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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyTacrolimus
Targets (1)
Enzymes (3)
Carriers (2)
Transporters (2)
Identification
- Name
- Tacrolimus
- Accession Number
- DB00864 (APRD00276, EXPT01437)
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Description
Tacrolimus (also FK-506 or Fujimycin) is an immunosuppressive drug whose main use is after organ transplant to reduce the activity of the patient's immune system and so the risk of organ rejection. It is also used in a topical preparation in the treatment of severe atopic dermatitis, severe refractory uveitis after bone marrow transplants, and the skin condition vitiligo. It was discovered in 1984 from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis. Tacrolimus is chemically known as a macrolide. It reduces peptidyl-prolyl isomerase activity by binding to the immunophilin FKBP-12 (FK506 binding protein) creating a new complex. This FKBP12-FK506 complex interacts with and inhibits calcineurin thus inhibiting both T-lymphocyte signal transduction and IL-2 transcription.
- Structure
Structure for DB00864 (Tacrolimus)
- Synonyms
- Anhydrous tacrolimus
- Tacrolimus anhydrous
- Tacrolimus, anhydrous
- External IDs
- FK-506 / FK5 / K506
- Product Ingredients
Ingredient UNII CAS InChI Key Tacrolimus hydrate WM0HAQ4WNM 109581-93-3 NWJQLQGQZSIBAF-MSLXHMNKSA-N - Product Images
- Approved Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Ach-tacrolimus Capsule 1 mg Oral Accord Healthcare Limited Not applicable Not applicable Canada 
Ach-tacrolimus Capsule 0.5 mg Oral Accord Healthcare Limited Not applicable Not applicable Canada Ach-tacrolimus Capsule 5 mg Oral Accord Healthcare Limited Not applicable Not applicable Canada Advagraf Capsule, extended release 5 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU 
Advagraf Capsule, extended release 1 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU Advagraf Capsule, extended release 3 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU Advagraf Capsule, extended release 3 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU Advagraf Capsule, extended release 0.5 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU Advagraf Capsule, extended release 0.5 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU Advagraf Capsule, extended release 5 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU Advagraf Capsule, extended release 5 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU Advagraf Capsule, extended release 3 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU Advagraf Capsule, extended release 0.5 mg Oral Astellas Pharma Inc 2008-04-09 Not applicable Canada Advagraf Capsule, extended release 3 mg Oral Astellas Pharma Inc 2010-04-05 Not applicable Canada Advagraf Capsule, extended release 1 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU Advagraf Capsule, extended release 1 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU Advagraf Capsule, extended release 5 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU Advagraf Capsule, extended release 5 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU Advagraf Capsule, extended release 1 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU Advagraf Capsule, extended release 3 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU Advagraf Capsule, extended release 1 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU Advagraf Capsule, extended release 0.5 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU Advagraf Capsule, extended release 1 mg Oral Astellas Pharma Inc 2008-04-09 Not applicable Canada Advagraf Capsule, extended release 1 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU Advagraf Capsule, extended release 1 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU Advagraf Capsule, extended release 0.5 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU Advagraf Capsule, extended release 3 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU Advagraf Capsule, extended release 5 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU Advagraf Capsule, extended release 0.5 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU Advagraf Capsule, extended release 3 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU Advagraf Capsule, extended release 5 mg Oral Astellas Pharma Inc 2008-04-09 Not applicable Canada Advagraf Capsule, extended release 1 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU Advagraf Capsule, extended release 0.5 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU Astagraf XL Capsule, coated, extended release .5 mg/1 Oral Astellas Pharma Inc 2013-07-19 Not applicable US 
Astagraf XL Capsule, coated, extended release 1 mg/1 Oral Astellas Pharma Inc 2013-07-19 Not applicable US Astagraf XL Capsule, coated, extended release 5 mg/1 Oral Astellas Pharma Inc 2013-07-19 Not applicable US Envarsus Tablet, extended release 1 mg Oral Chiesi Farmaceutici S.P.A. 2014-07-18 Not applicable EU Envarsus Tablet, extended release 4 mg Oral Chiesi Farmaceutici S.P.A. 2014-07-18 Not applicable EU Envarsus Tablet, extended release 4 mg Oral Chiesi Farmaceutici S.P.A. 2014-07-18 Not applicable EU Envarsus Tablet, extended release 0.75 mg Oral Chiesi Farmaceutici S.P.A. 2014-07-18 Not applicable EU Envarsus Tablet, extended release 1 mg Oral Chiesi Farmaceutici S.P.A. 2014-07-18 Not applicable EU Envarsus Tablet, extended release 0.75 mg Oral Chiesi Farmaceutici S.P.A. 2014-07-18 Not applicable EU Envarsus Tablet, extended release 1 mg Oral Chiesi Farmaceutici S.P.A. 2014-07-18 Not applicable EU Envarsus Tablet, extended release 4 mg Oral Chiesi Farmaceutici S.P.A. 2014-07-18 Not applicable EU Envarsus Tablet, extended release 0.75 mg Oral Chiesi Farmaceutici S.P.A. 2014-07-18 Not applicable EU Envarsus XR Tablet, extended release 1 mg/1 Oral Veloxis Pharmaceuticals 2015-09-01 Not applicable US Envarsus XR Tablet, extended release 4 mg/1 Oral Veloxis Pharmaceuticals 2015-09-01 Not applicable US Envarsus XR Tablet, extended release .75 mg/1 Oral Veloxis Pharmaceuticals 2015-09-01 Not applicable US Jamp-tacrolimus Capsule 1 mg Oral Jamp Pharma Corporation Not applicable Not applicable Canada Jamp-tacrolimus Capsule 5 mg Oral Jamp Pharma Corporation Not applicable Not applicable Canada Jamp-tacrolimus Capsule 0.5 mg Oral Jamp Pharma Corporation Not applicable Not applicable Canada Modigraf Granule 0.2 mg Oral Astellas Pharma Europe Bv 2009-05-15 Not applicable EU Modigraf Granule 1 mg Oral Astellas Pharma Europe Bv 2009-05-15 Not applicable EU Prograf Capsule 1 mg Oral Astellas Pharma Inc 1996-08-14 Not applicable Canada Prograf Capsule, gelatin coated 1 mg/1 Oral Astellas Pharma Inc 1994-04-08 Not applicable US Prograf Capsule, gelatin coated 1 mg/1 Oral Rebel Distributors 1994-04-08 Not applicable US Prograf Capsule 5 mg Oral Astellas Pharma Inc 1996-08-14 Not applicable Canada Prograf Solution 5 mg Intravenous Astellas Pharma Inc 1996-08-14 Not applicable Canada Prograf Capsule, gelatin coated 5 mg/1 Oral Astellas Pharma Inc 1994-04-08 Not applicable US Prograf Capsule, gelatin coated .5 mg/1 Oral Astellas Pharma Inc 1998-08-24 Not applicable US 
Prograf Capsule, gelatin coated 1 mg/1 Oral Cardinal Health 1994-04-08 Not applicable US Prograf Capsule 0.5 mg Oral Astellas Pharma Inc 2001-04-02 Not applicable Canada Prograf Injection, solution 5 mg/mL Intravenous Astellas Pharma Inc 1994-04-08 Not applicable US Prograf Capsule, gelatin coated 1 mg/1 Oral Aphena Pharma Solutions Tennessee, Inc. 1994-04-08 Not applicable US 
Protopic Ointment 0.1 % Cutaneous Leo Pharma 2002-02-28 Not applicable EU Protopic Ointment 0.03 % Cutaneous Leo Pharma 2002-02-28 Not applicable EU Protopic Ointment .3 mg/g Topical Astellas Pharma Inc 2000-12-08 Not applicable US Protopic Ointment 0.03 % Topical Leo Pharma 2001-09-06 Not applicable Canada Protopic Ointment 1 mg/g Topical Physicians Total Care, Inc. 2008-05-08 Not applicable US Protopic Ointment 0.1 % Cutaneous Leo Pharma 2002-02-28 Not applicable EU Protopic Ointment .3 mg/g Topical Leo Pharma 2000-12-08 Not applicable US Protopic Ointment 0.03 % Cutaneous Leo Pharma 2002-02-28 Not applicable EU Protopic Ointment 1 mg/g Topical Astellas Pharma Inc 2000-12-08 Not applicable US Protopic Ointment 0.03 % Cutaneous Leo Pharma 2002-02-28 Not applicable EU Protopic Ointment 1 mg/g Topical Leo Pharma 2000-12-08 Not applicable US Protopic Ointment 0.1 % Cutaneous Leo Pharma 2002-02-28 Not applicable EU Protopic Ointment 0.1 % Topical Leo Pharma 2001-09-06 Not applicable Canada Ran-tacrolimus Capsule 5 mg Oral Ranbaxy Inc. Not applicable Not applicable Canada Sandoz Tacrolimus Capsule 1 mg Oral Sandoz Canada Incorporated 2013-11-25 Not applicable Canada Sandoz Tacrolimus Capsule 5 mg Oral Sandoz Canada Incorporated 2013-11-25 Not applicable Canada Sandoz Tacrolimus Capsule 0.5 mg Oral Sandoz Canada Incorporated 2014-06-11 Not applicable Canada Tacrolimus Ointment .3 mg/g Topical Perrigo New York Inc. 2014-11-20 Not applicable US Tacrolimus Ointment 1 mg/g Topical Perrigo New York Inc. 2014-11-20 Not applicable US - Approved Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Apo-tacrolimus Capsule 1 mg Oral Apotex Corporation Not applicable Not applicable Canada Apo-tacrolimus Capsule 5 mg Oral Apotex Corporation Not applicable Not applicable Canada Apo-tacrolimus Capsule 0.5 mg Oral Apotex Corporation Not applicable Not applicable Canada Hecoria Capsule .5 mg/1 Oral Novartis 2011-12-20 Not applicable US Hecoria Capsule 1 mg/1 Oral Novartis 2011-12-20 Not applicable US Hecoria Capsule 5 mg/1 Oral Novartis 2011-12-20 Not applicable US Tacrolimus Capsule 1 mg/1 Oral A S Medication Solutions 2011-09-30 2017-06-20 US Tacrolimus Capsule, gelatin coated .5 mg/1 Oral Panacea Biotec Ltd 2016-02-26 Not applicable US Tacrolimus Capsule, gelatin coated .5 mg/1 Oral Kremers Urban 2015-07-30 Not applicable US Tacrolimus Capsule 5 mg/1 Oral Sandoz 2012-01-15 Not applicable US Tacrolimus Capsule 1 mg/1 Oral Sandoz 2009-08-10 Not applicable US Tacrolimus Capsule 1 mg/1 Oral Golden State Medical Supply 2015-11-18 Not applicable US Tacrolimus Capsule .5 mg/1 Oral Mylan Institutional 2010-11-15 Not applicable US Tacrolimus Capsule, gelatin coated 5 mg/1 Oral Bionpharma Inc. 2016-02-26 Not applicable US Tacrolimus Capsule .5 mg/1 Oral Major 2010-05-14 Not applicable US Tacrolimus Capsule, gelatin coated 1 mg/1 Oral Bionpharma Inc. 2016-02-26 Not applicable US Tacrolimus Capsule 1 mg/1 Oral Cardinal Health 2009-08-10 Not applicable US Tacrolimus Capsule 1 mg/1 Oral Mylan Pharmaceuticals 2010-09-17 Not applicable US Tacrolimus Ointment 1 mg/g Topical E. Fougera & CO., A division of Fougera Pharmaceuticals Inc. 2014-09-09 Not applicable US Tacrolimus Capsule 5 mg/1 Oral Strides Shasun Limited 2014-08-13 Not applicable US Tacrolimus Capsule 1 mg/1 Oral Cardinal Health 2010-11-01 Not applicable US Tacrolimus Capsule, gelatin coated 1 mg/1 Oral bryant ranch prepack 2012-10-30 Not applicable US Tacrolimus Capsule 5 mg/1 Oral Accord Healthcare Limited 2011-08-31 Not applicable US 
Tacrolimus Capsule 1 mg/1 Oral Sandoz 2012-01-15 Not applicable US Tacrolimus Capsule 5 mg/1 Oral Watson Pharmaceuticals 2010-07-06 Not applicable US Tacrolimus Capsule 5 mg/1 Oral Amerincan Health Packaging 2013-07-17 Not applicable US Tacrolimus Capsule 5 mg/1 Oral Ingenus Pharmaceuticals Llc 2012-09-28 Not applicable US Tacrolimus Capsule 1 mg/1 Oral Cardinal Health 2011-06-15 Not applicable US Tacrolimus Capsule 1 mg/1 Oral Dr Reddy's Laboratories 2010-05-14 Not applicable US Tacrolimus Capsule .5 mg/1 Oral Strides Shasun Limited 2014-08-13 Not applicable US Tacrolimus Capsule, gelatin coated 1 mg/1 Oral Panacea Biotec Ltd 2016-02-26 Not applicable US Tacrolimus Capsule, gelatin coated 1 mg/1 Oral Kremers Urban 2015-07-30 Not applicable US Tacrolimus Capsule .5 mg/1 Oral Accord Healthcare Limited 2011-08-31 Not applicable US 
Tacrolimus Capsule 5 mg/1 Oral Sandoz 2009-08-10 Not applicable US Tacrolimus Capsule 5 mg/1 Oral Golden State Medical Supply 2015-11-18 Not applicable US Tacrolimus Capsule 1 mg/1 Oral Mylan Institutional 2010-11-01 Not applicable US Tacrolimus Capsule 1 mg/1 Oral Cardinal Health 2009-08-10 Not applicable US Tacrolimus Capsule 5 mg/1 Oral Major 2010-05-14 Not applicable US Tacrolimus Capsule .5 mg/1 Oral Ingenus Pharmaceuticals Llc 2012-09-28 Not applicable US Tacrolimus Capsule 5 mg/1 Oral Mylan Pharmaceuticals 2010-09-17 Not applicable US Tacrolimus Ointment .3 mg/g Topical E. Fougera & CO., A division of Fougera Pharmaceuticals Inc. 2014-09-09 Not applicable US Tacrolimus Capsule .5 mg/1 Oral Amerincan Health Packaging 2013-07-17 Not applicable US Tacrolimus Capsule .5 mg/1 Oral Sandoz 2009-08-10 Not applicable US Tacrolimus Capsule .5 mg/1 Oral Golden State Medical Supply 2015-11-18 Not applicable US Tacrolimus Capsule 5 mg/1 Oral Mylan Institutional 2010-11-01 Not applicable US Tacrolimus Capsule .5 mg/1 Oral Cardinal Health 2011-06-15 Not applicable US Tacrolimus Capsule 5 mg/1 Oral Dr Reddy's Laboratories 2010-05-14 Not applicable US Tacrolimus Capsule 1 mg/1 Oral Cardinal Health 2013-07-17 Not applicable US Tacrolimus Capsule .5 mg/1 Oral Mylan Pharmaceuticals 2010-09-17 Not applicable US Tacrolimus Capsule 1 mg/1 Oral Strides Shasun Limited 2014-08-13 Not applicable US Tacrolimus Capsule, gelatin coated 5 mg/1 Oral Panacea Biotec Ltd 2016-02-26 Not applicable US Tacrolimus Capsule, gelatin coated 5 mg/1 Oral Kremers Urban 2015-07-30 Not applicable US Tacrolimus Capsule 1 mg/1 Oral Accord Healthcare Limited 2011-08-31 Not applicable US 
Tacrolimus Capsule .5 mg/1 Oral Sandoz 2012-01-15 Not applicable US Tacrolimus Capsule, gelatin coated .5 mg/1 Oral Bionpharma Inc. 2016-02-26 Not applicable US Tacrolimus Capsule 1 mg/1 Oral Amerincan Health Packaging 2013-07-17 Not applicable US Tacrolimus Capsule 1 mg/1 Oral Ingenus Pharmaceuticals Llc 2012-09-28 Not applicable US Tacrolimus Capsule 1 mg/1 Oral Major 2015-01-05 Not applicable US Tacrolimus Capsule .5 mg/1 Oral Dr Reddy's Laboratories 2010-05-14 Not applicable US Tacrolimus Capsule 1 mg/1 Oral Kaiser Foundations Hospitals 2010-12-10 Not applicable US - Approved Over the Counter Products
- Not Available
- Unapproved/Other Products
- Not Available
- International/Other Brands
- Not Available
- Brand mixtures
- Not Available
- Categories
- Antineoplastic and Immunomodulating Agents
- Calcineurin Inhibitors
- Combined Inhibitors of CYP3A4 and P-glycoprotein
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Substrates
- Enzyme Inhibitors
- Hyperglycemia-Associated Agents
- Immunologic Factors
- Immunosuppressive Agents
- Lactones
- Macrolides
- Myelosuppressive Agents
- P-glycoprotein/ABCB1 Inducers
- P-glycoprotein/ABCB1 Inhibitors
- P-glycoprotein/ABCB1 Substrates
- Polyketides
- UNII
- Y5L2157C4J
- CAS number
- 104987-11-3
- Weight
- Average: 804.0182
Monoisotopic: 803.481976677 - Chemical Formula
- C44H69NO12
- InChI Key
- QJJXYPPXXYFBGM-LFZNUXCKSA-N
- InChI
- InChI=1S/C44H69NO12/c1-10-13-31-19-25(2)18-26(3)20-37(54-8)40-38(55-9)22-28(5)44(52,57-40)41(49)42(50)45-17-12-11-14-32(45)43(51)56-39(29(6)34(47)24-35(31)48)27(4)21-30-15-16-33(46)36(23-30)53-7/h10,19,21,26,28-34,36-40,46-47,52H,1,11-18,20,22-24H2,2-9H3/b25-19+,27-21+/t26-,28+,29+,30-,31+,32-,33+,34-,36+,37-,38-,39+,40+,44+/m0/s1
- IUPAC Name
- (1R,9S,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-1,14-dihydroxy-12-[(1E)-1-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-17-(prop-2-en-1-yl)-11,28-dioxa-4-azatricyclo[22.3.1.0⁴,⁹]octacos-18-ene-2,3,10,16-tetrone
- SMILES
- CO[[email protected]@H]1C[[email protected]@H](CC[[email protected]]1O)\C=C(/C)[[email protected]]1OC(=O)[[email protected]@H]2CCCCN2C(=O)C(=O)[[email protected]]2(O)O[[email protected]@H]([[email protected]](C[[email protected]]2C)OC)[[email protected]](C[[email protected]@H](C)C\C(C)=C\[[email protected]@H](CC=C)C(=O)C[[email protected]](O)[[email protected]]1C)OC
Pharmacology
- Indication
For use after allogenic organ transplant to reduce the activity of the patient's immune system and so the risk of organ rejection. It was first approved by the FDA in 1994 for use in liver transplantation, this has been extended to include kidney, heart, small bowel, pancreas, lung, trachea, skin, cornea, and limb transplants. It has also been used in a topical preparation in the treatment of severe atopic dermatitis.
- Structured Indications
- Graft Versus Host Disease (GVHD)
- Heart Transplant Rejection
- Kidney Transplant Rejection
- Liver Transplant Rejection
- Oral Lichen Planus
- Psoriasis
- Pyoderma Gangrenosum
- Rheumatoid Arthritis
- Severe Atopic Dermatitis
- Vitiligo
- Moderate Atopic dermatitis
- Refractory Atopic dermatitis
- Refractory Rheumatoid arthritis
- Severe Rheumatoid arthritis
- Pharmacodynamics
Tacrolimus is a macrolide antibiotic. It acts by reducing peptidyl-prolyl isomerase activity by binding to the immunophilin FKBP-12 (FK506 binding protein) creating a new complex. This inhibits both T-lymphocyte signal transduction and IL-2 transcription. Although this activity is similar to cyclosporine studies have shown that the incidence of acute rejection is reduced by tacrolimus use over cyclosporine. Tacrolimus has also been shown to be effective in the topical treatment of eczema, particularly atopic eczema. It suppresses inflammation in a similar way to steroids, but is not as powerful. An important dermatological advantage of tacrolimus is that it can be used directly on the face; topical steroids cannot be used on the face, as they thin the skin dramatically there. On other parts of the body, topical steroid are generally a better treatment.
- Mechanism of action
The mechanism of action of tacrolimus in atopic dermatitis is not known. While the following have been observed, the clinical significance of these observations in atopic dermatitis is not known. It has been demonstrated that tacrolimus inhibits T-lymphocyte activation by first binding to an intracellular protein, FKBP-12. A complex of tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin is then formed and the phosphatase activity of calcineurin is inhibited. This prevents the dephosphorylation and translocation of nuclear factor of activated T-cells (NF-AT), a nuclear component thought to initiate gene transcription for the formation of lymphokines. Tacrolimus also inhibits the transcription for genes which encode IL-3, IL-4, IL-5, GM-CSF, and TNF-, all of which are involved in the early stages of T-cell activation. Additionally, tacrolimus has been shown to inhibit the release of pre-formed mediators from skin mast cells and basophils, and to downregulate the expression of FceRI on Langerhans cells.
Target Actions Organism APeptidyl-prolyl cis-trans isomerase FKBP1A inhibitorHuman - Absorption
Absorption of tacrolimus from the gastrointestinal tract after oral administration is incomplete and variable. The absolute bioavailability in adult kidney transplant patients is 17±10%; in adults liver transplant patients is 22±6%; in healthy subjects is 18±5%. The absolute bioavailability in pediatric liver transplant patients was 31±24%. Tacrolimus maximum blood concentrations (Cmax) and area under the curve (AUC) appeared to increase in a dose-proportional fashion in 18 fasted healthy volunteers receiving a single oral dose of 3, 7, and 10 mg. When given without food, the rate and extent of absorption were the greatest. The time of the meal also affected bioavailability. When given immediately after a meal, mean Cmax was reduced 71%, and mean AUC was reduced 39%, relative to the fasted condition. When administered 1.5 hours following the meal, mean Cmax was reduced 63%, and mean AUC was reduced 39%, relative to the fasted condition.
- Volume of distribution
- 2.6 ± 2.1 L/kg [pediatric liver transplant patients]
- 1.07 ± 0.20 L/kg [patients with renal impairment, 0.02 mg/kg/4 hr dose, IV]
- 3.1 ± 1.6 L/kg [Mild Hepatic Impairment, 0.02 mg/kg/4 hr dose, IV]
- 3.7 ± 4.7 L/kg [Mild Hepatic Impairment, 7.7 mg dose, PO]
- 3.9 ± 1.0 L/kg [Severe hepatic impairment, 0.02 mg/kg/4 hr dose, IV]
- 3.1 ± 3.4 L/kg [Severe hepatic impairment, 8 mg dose, PO]
- Protein binding
~99% bound to human plasma protein, primarily to albumin and alpha-1-acid glycoprotein. This is independent of concentration over a range of 5-50 ng/mL.
- Metabolism
Hepatic, extensive, primarily by CYP3A4. The major metabolite identified in incubations with human liver microsomes is 13-demethyl tacrolimus. In in vitro studies, a 31-demethyl metabolite has been reported to have the same activity as tacrolimus.
- Route of elimination
In man, less than 1% of the dose administered is excreted unchanged in urine. When administered IV, fecal elimination accounted for 92.6±30.7%, urinary elimination accounted for 2.3±1.1%.
- Half life
The elimination half life in adult healthy volunteers, kidney transplant patients, liver transplants patients, and heart transplant patients are approximately 35, 19, 12, 24 hours, respectively. The elimination half life in pediatric liver transplant patients was 11.5±3.8 hours, in pediatric kidney transplant patients was 10.2±5.0 (range 3.4-25) hours.
- Clearance
- 0.040 L/hr/kg [healthy subjects, IV]
- 0.172 ± 0.088 L/hr/kg [healthy subjects, oral]
- 0.083 L/hr/kg [adult kidney transplant patients, IV]
- 0.053 L/hr/kg [adult liver transplant patients, IV]
- 0.051 L/hr/kg [adult heart transplant patients, IV]
- 0.138 ± 0.071 L/hr/kg [pediatric liver transplant patients]
- 0.12 ± 0.04 (range 0.06-0.17) L/hr/kg [pediatric kidney transplant patients]
- 0.038 ± 0.014 L/hr/kg [patients with renal impairment, 0.02 mg/kg/4 hr dose, IV]
- 0.042 ± 0.02 L/hr/kg [Mild Hepatic Impairment, 0.02 mg/kg/4 hr dose, IV]
- 0.034 ± 0.019 L/hr/kg [Mild Hepatic Impairment, 7.7 mg dose, PO]
- 0.017 ± 0.013 L/hr/kg [Severe hepatic impairment, 0.02 mg/kg/4 hr dose, IV]
- 0.016 ± 0.011 L/hr/kg [Severe hepatic impairment, 8 mg dose, PO]
- Toxicity
Side effects can be severe and include blurred vision, liver and kidney problems (it is nephrotoxic), seizures, tremors, hypertension, hypomagnesemia, diabetes mellitus, hyperkalemia, itching, insomnia, confusion. LD50=134-194 mg/kg (rat).
- Affected organisms
- Humans and other mammals
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
Interacting Gene/Enzyme Allele name Genotype(s) Defining Change(s) Type(s) Description Details Multidrug resistance protein 1 --- (T;T) / (G;T) T Allele (G2677T) ADR Directly Studied The presence of this genotype in ABCB1 may indicate an increased risk of drug-induced neurotoxicity when treated with tacrolimus. Details Cytochrome P450 3A5 CYP3A5*1 Not Available Functional gene Effect Directly Studied Patients with this genotype in CYP3A5 are extensive metabolizers and require higer doses of tacrolimus to attain the therapeutic effect. Details
Interactions
- Drug Interactions
Drug Interaction Drug group 1,10-Phenanthroline The metabolism of Tacrolimus can be decreased when combined with 1,10-Phenanthroline. Experimental 2-HYDROXY-1,4-NAPHTHOQUINONE The metabolism of Tacrolimus can be decreased when combined with 2-HYDROXY-1,4-NAPHTHOQUINONE. Experimental 2-mercaptobenzothiazole The metabolism of Tacrolimus can be decreased when combined with 2-mercaptobenzothiazole. Vet Approved 2-Methoxyethanol The risk or severity of adverse effects can be increased when Tacrolimus is combined with 2-Methoxyethanol. Experimental 2,4-thiazolidinedione The therapeutic efficacy of Thiazolidinedione can be decreased when used in combination with Tacrolimus. Investigational 3,4-Dichloroisocoumarin The metabolism of Tacrolimus can be decreased when combined with 3,4-Dichloroisocoumarin. Experimental 4-(2-Aminoethyl)Benzenesulfonyl Fluoride The metabolism of Tacrolimus can be decreased when combined with 4-(2-AMINOETHYL)BENZENESULFONYL FLUORIDE. Experimental Abatacept The risk or severity of adverse effects can be increased when Tacrolimus is combined with Abatacept. Approved abetimus The risk or severity of adverse effects can be increased when Tacrolimus is combined with abetimus. Investigational Acarbose The therapeutic efficacy of Acarbose can be decreased when used in combination with Tacrolimus. Approved, Investigational Acebutolol The serum concentration of Acebutolol can be decreased when it is combined with Tacrolimus. Approved Aceclofenac Aceclofenac may increase the nephrotoxic activities of Tacrolimus. Approved Acetaminophen The serum concentration of Acetaminophen can be decreased when it is combined with Tacrolimus. Approved Acetohexamide The therapeutic efficacy of Acetohexamide can be decreased when used in combination with Tacrolimus. Withdrawn Acetylsalicylic acid The serum concentration of Acetylsalicylic acid can be decreased when it is combined with Tacrolimus. Approved, Vet Approved Acetylsalicylic acid Acetylsalicylic acid may increase the nephrotoxic activities of Tacrolimus. Approved, Vet Approved Acteoside The risk or severity of adverse effects can be increased when Tacrolimus is combined with Acteoside. Investigational Adalimumab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Adalimumab. Approved Adapalene Adapalene may increase the nephrotoxic activities of Tacrolimus. Approved Adefovir Dipivoxil The risk or severity of adverse effects can be increased when Tacrolimus is combined with Adefovir Dipivoxil. Approved, Investigational Afatinib The serum concentration of Afatinib can be decreased when it is combined with Tacrolimus. Approved Afelimomab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Afelimomab. Investigational AICA ribonucleotide The therapeutic efficacy of Aicar can be decreased when used in combination with Tacrolimus. Experimental Albendazole The serum concentration of Tacrolimus can be increased when it is combined with Albendazole. Approved, Vet Approved Aldosterone The serum concentration of Tacrolimus can be decreased when it is combined with Aldosterone. Experimental Alectinib The serum concentration of Tacrolimus can be increased when it is combined with Alectinib. Approved Alefacept The risk or severity of adverse effects can be increased when Tacrolimus is combined with Alefacept. Approved, Withdrawn Alemtuzumab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Alemtuzumab. Approved, Investigational Alfentanil The serum concentration of Tacrolimus can be increased when it is combined with Alfentanil. Approved, Illicit Alicaforsen The risk or severity of adverse effects can be increased when Tacrolimus is combined with alicaforsen. Investigational Alitretinoin The serum concentration of Alitretinoin can be decreased when it is combined with Tacrolimus. Approved, Investigational Alogliptin The metabolism of Tacrolimus can be decreased when combined with Alogliptin. Approved Alogliptin The therapeutic efficacy of Alogliptin can be decreased when used in combination with Tacrolimus. Approved Alpha-1-proteinase inhibitor The metabolism of Tacrolimus can be decreased when combined with Alpha-1-proteinase inhibitor. Approved Altretamine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Altretamine. Approved Amantadine The serum concentration of Tacrolimus can be increased when it is combined with Amantadine. Approved Ambrisentan The serum concentration of Ambrisentan can be decreased when it is combined with Tacrolimus. Approved, Investigational Amiloride Amiloride may increase the hyperkalemic activities of Tacrolimus. Approved Aminohippuric acid The serum concentration of Tacrolimus can be increased when it is combined with Aminohippuric acid. Approved Amiodarone The metabolism of Tacrolimus can be decreased when combined with Amiodarone. Approved, Investigational Amitriptyline The serum concentration of Amitriptyline can be decreased when it is combined with Tacrolimus. Approved Amlodipine The serum concentration of Tacrolimus can be increased when it is combined with Amlodipine. Approved Amorolfine The metabolism of Tacrolimus can be decreased when combined with Amorolfine. Approved Amoxapine The metabolism of Tacrolimus can be decreased when combined with Amoxapine. Approved Amphotericin B The metabolism of Tacrolimus can be decreased when combined with Amphotericin B. Approved, Investigational Amprenavir The metabolism of Tacrolimus can be decreased when combined with Amprenavir. Approved Amprenavir The serum concentration of Tacrolimus can be decreased when it is combined with Amprenavir. Approved Amsacrine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Amsacrine. Approved Amsacrine The serum concentration of Tacrolimus can be increased when it is combined with Amsacrine. Approved Anakinra The risk or severity of adverse effects can be increased when Tacrolimus is combined with Anakinra. Approved Andrographolide HMPL-004 may increase the nephrotoxic activities of Tacrolimus. Investigational Anidulafungin The metabolism of Tacrolimus can be decreased when combined with Anidulafungin. Approved, Investigational Anisodamine Anisodamine may increase the nephrotoxic activities of Tacrolimus. Investigational Antipyrine Antipyrine may increase the nephrotoxic activities of Tacrolimus. Approved Antithrombin III human The metabolism of Tacrolimus can be decreased when combined with Antithrombin III human. Approved Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Tacrolimus is combined with Anti-thymocyte Globulin (Rabbit). Approved Apixaban The metabolism of Tacrolimus can be decreased when combined with Apixaban. Approved Apixaban The serum concentration of Apixaban can be decreased when it is combined with Tacrolimus. Approved Apocynin Acetovanillone may increase the nephrotoxic activities of Tacrolimus. Investigational Apremilast The risk or severity of adverse effects can be increased when Tacrolimus is combined with Apremilast. Approved, Investigational Apremilast Apremilast may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Aprepitant The serum concentration of Tacrolimus can be increased when it is combined with Aprepitant. Approved, Investigational Aprotinin The metabolism of Tacrolimus can be decreased when combined with Aprotinin. Approved, Withdrawn Argatroban The metabolism of Tacrolimus can be decreased when combined with Argatroban. Approved, Investigational Arsenic trioxide The serum concentration of Arsenic trioxide can be decreased when it is combined with Tacrolimus. Approved, Investigational Artemether The metabolism of Tacrolimus can be decreased when combined with Artemether. Approved Astemizole The serum concentration of Tacrolimus can be increased when it is combined with Astemizole. Approved, Withdrawn Asunaprevir The metabolism of Tacrolimus can be decreased when combined with Asunaprevir. Approved, Investigational Atazanavir The metabolism of Tacrolimus can be decreased when combined with Atazanavir. Approved, Investigational Atenolol The serum concentration of Atenolol can be decreased when it is combined with Tacrolimus. Approved Atomoxetine The metabolism of Tacrolimus can be decreased when combined with Atomoxetine. Approved Atorvastatin The serum concentration of Tacrolimus can be increased when it is combined with Atorvastatin. Approved Axitinib The serum concentration of Axitinib can be decreased when it is combined with Tacrolimus. Approved, Investigational Azacitidine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Azacitidine. Approved, Investigational Azapropazone Azapropazone may increase the nephrotoxic activities of Tacrolimus. Withdrawn Azathioprine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Azathioprine. Approved Azelastine The serum concentration of Tacrolimus can be increased when it is combined with Azelastine. Approved Azelastine Azelastine may increase the nephrotoxic activities of Tacrolimus. Approved Azithromycin The serum concentration of Tacrolimus can be increased when it is combined with Azithromycin. Approved Bafilomycin A1 The metabolism of Tacrolimus can be decreased when combined with Bafilomycin A1. Experimental Balaglitazone The therapeutic efficacy of Balaglitazone can be decreased when used in combination with Tacrolimus. Investigational Balsalazide Balsalazide may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Basiliximab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Basiliximab. Approved, Investigational Batimastat The metabolism of Tacrolimus can be decreased when combined with Batimastat. Experimental BCG vaccine The therapeutic efficacy of Bcg can be decreased when used in combination with Tacrolimus. Investigational Belatacept The risk or severity of adverse effects can be increased when Tacrolimus is combined with Belatacept. Approved Belimumab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Belimumab. Approved Benazepril The metabolism of Tacrolimus can be decreased when combined with Benazepril. Approved, Investigational Benoxaprofen Benoxaprofen may increase the nephrotoxic activities of Tacrolimus. Withdrawn Benzamidine The metabolism of Tacrolimus can be decreased when combined with Benzamidine. Experimental Benznidazole The risk or severity of adverse effects can be increased when Tacrolimus is combined with Benznidazole. Approved Benzocaine The serum concentration of Tacrolimus can be increased when it is combined with Benzocaine. Approved Benzoic Acid The metabolism of Tacrolimus can be decreased when combined with Benzoic Acid. Approved Bepridil The serum concentration of Tacrolimus can be increased when it is combined with Bepridil. Approved, Withdrawn Betamethasone The risk or severity of adverse effects can be increased when Tacrolimus is combined with Betamethasone. Approved, Vet Approved Betamethasone The serum concentration of Betamethasone can be decreased when it is combined with Tacrolimus. Approved, Vet Approved Betulinic Acid Betulinic Acid may increase the nephrotoxic activities of Tacrolimus. Investigational Bexarotene The serum concentration of Tacrolimus can be decreased when it is combined with Bexarotene. Approved, Investigational Bifonazole The metabolism of Tacrolimus can be decreased when combined with Bifonazole. Approved Biperiden The serum concentration of Tacrolimus can be increased when it is combined with Biperiden. Approved Bivalirudin The metabolism of Tacrolimus can be decreased when combined with Bivalirudin. Approved, Investigational Bleomycin The risk or severity of adverse effects can be increased when Tacrolimus is combined with Bleomycin. Approved Blinatumomab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Blinatumomab. Approved Boceprevir The metabolism of Tacrolimus can be decreased when combined with Boceprevir. Withdrawn Boceprevir The serum concentration of Tacrolimus can be increased when it is combined with Boceprevir. Withdrawn Bortezomib The metabolism of Tacrolimus can be decreased when combined with Bortezomib. Approved, Investigational Bosentan The serum concentration of Tacrolimus can be decreased when it is combined with Bosentan. Approved, Investigational Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Tacrolimus. Approved Brentuximab vedotin The risk or severity of adverse effects can be increased when Tacrolimus is combined with Brentuximab vedotin. Approved Brentuximab vedotin The serum concentration of Brentuximab vedotin can be decreased when it is combined with Tacrolimus. Approved Briakinumab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Briakinumab. Investigational Brodalumab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Amg 827. Approved, Investigational Bromfenac Bromfenac may increase the nephrotoxic activities of Tacrolimus. Approved Bromocriptine The serum concentration of Bromocriptine can be decreased when it is combined with Tacrolimus. Approved, Investigational Bucillamine Bucillamine may increase the nephrotoxic activities of Tacrolimus. Investigational Budesonide The risk or severity of adverse effects can be increased when Tacrolimus is combined with Budesonide. Approved Buformin The therapeutic efficacy of Buformin can be decreased when used in combination with Tacrolimus. Withdrawn Buprenorphine The serum concentration of Tacrolimus can be increased when it is combined with Buprenorphine. Approved, Illicit, Investigational, Vet Approved Buspirone The serum concentration of Tacrolimus can be increased when it is combined with Buspirone. Approved, Investigational Busulfan The risk or severity of adverse effects can be increased when Tacrolimus is combined with Busulfan. Approved, Investigational Butenafine The metabolism of Tacrolimus can be decreased when combined with Butenafine. Approved Butoconazole The metabolism of Tacrolimus can be decreased when combined with Butoconazole. Approved Cabazitaxel The risk or severity of adverse effects can be increased when Tacrolimus is combined with Cabazitaxel. Approved Cabazitaxel The serum concentration of Cabazitaxel can be decreased when it is combined with Tacrolimus. Approved Caffeine The serum concentration of Caffeine can be decreased when it is combined with Tacrolimus. Approved Camptothecin The serum concentration of Camptothecin can be decreased when it is combined with Tacrolimus. Experimental Canagliflozin The serum concentration of Canagliflozin can be decreased when it is combined with Tacrolimus. Approved Canakinumab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Canakinumab. Approved, Investigational Candesartan The serum concentration of Tacrolimus can be increased when it is combined with Candesartan. Approved Candicidin The metabolism of Tacrolimus can be decreased when combined with Candicidin. Withdrawn Candoxatril The metabolism of Tacrolimus can be decreased when combined with Candoxatril. Experimental Candoxatrilat The metabolism of Tacrolimus can be decreased when combined with Candoxatrilat. Experimental Capecitabine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Capecitabine. Approved, Investigational Capric acid The metabolism of Tacrolimus can be decreased when combined with Decanoic Acid. Experimental Captopril The metabolism of Tacrolimus can be decreased when combined with Captopril. Approved Captopril The serum concentration of Tacrolimus can be increased when it is combined with Captopril. Approved Carbamazepine The metabolism of Tacrolimus can be increased when combined with Carbamazepine. Approved, Investigational Carbomycin The serum concentration of Tacrolimus can be increased when it is combined with Carbomycin. Vet Approved Carboplatin The risk or severity of adverse effects can be increased when Tacrolimus is combined with Carboplatin. Approved Carfilzomib The serum concentration of Carfilzomib can be decreased when it is combined with Tacrolimus. Approved Carmustine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Carmustine. Approved Carprofen Carprofen may increase the nephrotoxic activities of Tacrolimus. Approved, Vet Approved, Withdrawn Carvedilol The serum concentration of Tacrolimus can be increased when it is combined with Carvedilol. Approved, Investigational Caspofungin The metabolism of Tacrolimus can be decreased when combined with Caspofungin. Approved Caspofungin The serum concentration of Tacrolimus can be increased when it is combined with Caspofungin. Approved Caspofungin The serum concentration of Tacrolimus can be decreased when it is combined with Caspofungin. Approved Castanospermine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Castanospermine. Experimental Castanospermine The therapeutic efficacy of Castanospermine can be decreased when used in combination with Tacrolimus. Experimental Castanospermine Castanospermine may increase the nephrotoxic activities of Tacrolimus. Experimental Celecoxib Celecoxib may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Ceritinib The serum concentration of Tacrolimus can be increased when it is combined with Ceritinib. Approved Cerivastatin The serum concentration of Cerivastatin can be decreased when it is combined with Tacrolimus. Withdrawn Certolizumab pegol The risk or severity of adverse effects can be increased when Tacrolimus is combined with Certolizumab pegol. Approved Cerulenin The metabolism of Tacrolimus can be decreased when combined with Cerulenin. Approved Chlorambucil The risk or severity of adverse effects can be increased when Tacrolimus is combined with Chlorambucil. Approved Chloramphenicol The serum concentration of Tacrolimus can be increased when it is combined with Chloramphenicol. Approved, Vet Approved Chloroquine The serum concentration of Tacrolimus can be increased when it is combined with Chloroquine. Approved, Vet Approved Chloroquine Chloroquine may increase the nephrotoxic activities of Tacrolimus. Approved, Vet Approved Chloroxine The metabolism of Tacrolimus can be decreased when combined with Chloroxine. Approved Chlorpromazine The serum concentration of Chlorpromazine can be decreased when it is combined with Tacrolimus. Approved, Vet Approved Chlorpropamide The serum concentration of Tacrolimus can be increased when it is combined with Chlorpropamide. Approved Chlorprothixene The serum concentration of Tacrolimus can be increased when it is combined with Chlorprothixene. Approved, Withdrawn Cholesterol The serum concentration of Tacrolimus can be increased when it is combined with Cholesterol. Experimental Cholic Acid The serum concentration of Tacrolimus can be decreased when it is combined with Cholic Acid. Approved Choline magnesium trisalicylate Trisalicylate-choline may increase the nephrotoxic activities of Tacrolimus. Approved Chymostatin The metabolism of Tacrolimus can be decreased when combined with Chymostatin. Experimental Ciclopirox The metabolism of Tacrolimus can be decreased when combined with Ciclopirox. Approved, Investigational Ciglitazone The therapeutic efficacy of Ciglitazone can be decreased when used in combination with Tacrolimus. Experimental Cilastatin The metabolism of Tacrolimus can be decreased when combined with Cilastatin. Approved Cilazapril The metabolism of Tacrolimus can be decreased when combined with Cilazapril. Approved Cilazapril The serum concentration of Tacrolimus can be increased when it is combined with Cilazapril. Approved Cimetidine The serum concentration of Tacrolimus can be decreased when it is combined with Cimetidine. Approved Cinacalcet The serum concentration of Tacrolimus can be decreased when it is combined with Cinacalcet. Approved Ciprofloxacin The serum concentration of Ciprofloxacin can be decreased when it is combined with Tacrolimus. Approved, Investigational Cisplatin The risk or severity of adverse effects can be increased when Tacrolimus is combined with Cisplatin. Approved Cisplatin The serum concentration of Cisplatin can be decreased when it is combined with Tacrolimus. Approved Citalopram The metabolism of Tacrolimus can be decreased when combined with Citalopram. Approved Citalopram The serum concentration of Citalopram can be decreased when it is combined with Tacrolimus. Approved Cladribine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Cladribine. Approved, Investigational Clarithromycin The metabolism of Tacrolimus can be decreased when combined with Clarithromycin. Approved Clarithromycin The serum concentration of Tacrolimus can be increased when it is combined with Clarithromycin. Approved Clemastine The metabolism of Tacrolimus can be decreased when combined with Clemastine. Approved Clevidipine The serum concentration of Tacrolimus can be increased when it is combined with Clevidipine. Approved Clobazam The serum concentration of Clobazam can be decreased when it is combined with Tacrolimus. Approved, Illicit Clofarabine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Clofarabine. Approved, Investigational Clofazimine The serum concentration of Tacrolimus can be increased when it is combined with Clofazimine. Approved, Investigational Clomifene The serum concentration of Clomifene can be decreased when it is combined with Tacrolimus. Approved, Investigational Clomipramine The metabolism of Tacrolimus can be decreased when combined with Clomipramine. Approved, Vet Approved Clomipramine The serum concentration of Tacrolimus can be increased when it is combined with Clomipramine. Approved, Vet Approved Clonidine The serum concentration of Clonidine can be decreased when it is combined with Tacrolimus. Approved Clonixin Clonixin may increase the nephrotoxic activities of Tacrolimus. Approved Clopidogrel The serum concentration of Clopidogrel can be decreased when it is combined with Tacrolimus. Approved, Nutraceutical Clotrimazole The metabolism of Tacrolimus can be decreased when combined with Clotrimazole. Approved, Vet Approved Clotrimazole The serum concentration of Tacrolimus can be increased when it is combined with Clotrimazole. Approved, Vet Approved Clozapine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Clozapine. Approved Cobicistat The metabolism of Tacrolimus can be decreased when combined with Cobicistat. Approved Cobimetinib The serum concentration of Cobimetinib can be decreased when it is combined with Tacrolimus. Approved Colchicine The serum concentration of Colchicine can be increased when it is combined with Tacrolimus. Approved Colforsin The serum concentration of Tacrolimus can be increased when it is combined with Colforsin. Experimental Conivaptan The serum concentration of Tacrolimus can be increased when it is combined with Conivaptan. Approved, Investigational Conjugated estrogens The serum concentration of Conjugated Equine Estrogens can be decreased when it is combined with Tacrolimus. Approved Cordycepin The metabolism of Tacrolimus can be decreased when combined with Cordycepin. Investigational Corticotropin The risk or severity of adverse effects can be increased when Tacrolimus is combined with Corticotropin. Approved, Vet Approved Cortisone acetate The risk or severity of adverse effects can be increased when Tacrolimus is combined with Cortisone acetate. Approved Crizotinib The serum concentration of Tacrolimus can be increased when it is combined with Crizotinib. Approved Crizotinib The metabolism of Tacrolimus can be decreased when combined with Crizotinib. Approved Curcumin Curcumin may increase the nephrotoxic activities of Tacrolimus. Investigational Cyclophosphamide The risk or severity of adverse effects can be increased when Tacrolimus is combined with Cyclophosphamide. Approved, Investigational Cyclophosphamide The serum concentration of Tacrolimus can be increased when it is combined with Cyclophosphamide. Approved, Investigational Cyclosporine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Cyclosporine. Approved, Investigational, Vet Approved Cyclosporine Tacrolimus may increase the nephrotoxic activities of Cyclosporine. Approved, Investigational, Vet Approved Cyclosporine The metabolism of Tacrolimus can be decreased when combined with Cyclosporine. Approved, Investigational, Vet Approved Cytarabine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Cytarabine. Approved, Investigational D-Limonene D-Limonene may increase the nephrotoxic activities of Tacrolimus. Investigational Dabigatran etexilate The serum concentration of Dabigatran etexilate can be decreased when it is combined with Tacrolimus. Approved Dabigatran etexilate The metabolism of Tacrolimus can be decreased when combined with Dabigatran etexilate. Approved Dabrafenib The serum concentration of Tacrolimus can be decreased when it is combined with Dabrafenib. Approved Dacarbazine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Dacarbazine. Approved, Investigational Daclatasvir The serum concentration of Tacrolimus can be increased when it is combined with Daclatasvir. Approved Daclizumab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Daclizumab. Approved, Investigational Dactinomycin The risk or severity of adverse effects can be increased when Tacrolimus is combined with Dactinomycin. Approved Dactinomycin The serum concentration of Dactinomycin can be decreased when it is combined with Tacrolimus. Approved Danazol The serum concentration of Tacrolimus can be increased when it is combined with Danazol. Approved Dapagliflozin The serum concentration of Dapagliflozin can be decreased when it is combined with Tacrolimus. Approved Dapoxetine The metabolism of Tacrolimus can be decreased when combined with Dapoxetine. Investigational Darexaban The metabolism of Tacrolimus can be decreased when combined with Ym150. Investigational Darunavir The metabolism of Tacrolimus can be decreased when combined with Darunavir. Approved Dasabuvir The serum concentration of Tacrolimus can be increased when it is combined with Dasabuvir. Approved Dasatinib The risk or severity of adverse effects can be increased when Tacrolimus is combined with Dasatinib. Approved, Investigational Dasatinib The serum concentration of Tacrolimus can be increased when it is combined with Dasatinib. Approved, Investigational Daunorubicin The risk or severity of adverse effects can be increased when Tacrolimus is combined with Daunorubicin. Approved Daunorubicin The serum concentration of Daunorubicin can be decreased when it is combined with Tacrolimus. Approved Debrisoquin The serum concentration of Debrisoquin can be decreased when it is combined with Tacrolimus. Approved Deferasirox The serum concentration of Tacrolimus can be decreased when it is combined with Deferasirox. Approved, Investigational Delavirdine The metabolism of Tacrolimus can be decreased when combined with Delavirdine. Approved Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Tacrolimus. Approved Deoxyspergualin The risk or severity of adverse effects can be increased when Tacrolimus is combined with Deoxyspergualin. Investigational Deoxyspergualin The therapeutic efficacy of Deoxyspergualin can be decreased when used in combination with Tacrolimus. Investigational Desipramine The serum concentration of Tacrolimus can be increased when it is combined with Desipramine. Approved Desloratadine The serum concentration of Tacrolimus can be increased when it is combined with Desloratadine. Approved, Investigational Dexamethasone The risk or severity of adverse effects can be increased when Tacrolimus is combined with Dexamethasone. Approved, Investigational, Vet Approved Dexamethasone The serum concentration of Tacrolimus can be decreased when it is combined with Dexamethasone. Approved, Investigational, Vet Approved Dexlansoprazole The serum concentration of Tacrolimus can be increased when it is combined with TAK-390MR. Approved Dextromethorphan The serum concentration of Tacrolimus can be increased when it is combined with Dextromethorphan. Approved Diazepam The serum concentration of Diazepam can be decreased when it is combined with Tacrolimus. Approved, Illicit, Vet Approved Diclofenac The serum concentration of Tacrolimus can be increased when it is combined with Diclofenac. Approved, Vet Approved Diclofenac Diclofenac may increase the nephrotoxic activities of Tacrolimus. Approved, Vet Approved Diethylstilbestrol The serum concentration of Diethylstilbestrol can be decreased when it is combined with Tacrolimus. Approved Diflunisal Diflunisal may increase the nephrotoxic activities of Tacrolimus. Approved Digitoxin The serum concentration of Digitoxin can be decreased when it is combined with Tacrolimus. Approved Digoxin The serum concentration of Tacrolimus can be decreased when it is combined with Digoxin. Approved Dihydroergotamine The metabolism of Tacrolimus can be decreased when combined with Dihydroergotamine. Approved Dihydrotestosterone The serum concentration of Dihydrotestosterone can be decreased when it is combined with Tacrolimus. Illicit Diltiazem The metabolism of Tacrolimus can be decreased when combined with Diltiazem. Approved Dimethyl fumarate The risk or severity of adverse effects can be increased when Tacrolimus is combined with Dimethyl fumarate. Approved, Investigational Dinutuximab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Dinutuximab. Approved Dipyridamole The serum concentration of Dipyridamole can be decreased when it is combined with Tacrolimus. Approved Docetaxel The risk or severity of adverse effects can be increased when Tacrolimus is combined with Docetaxel. Approved, Investigational Docetaxel The serum concentration of Docetaxel can be decreased when it is combined with Tacrolimus. Approved, Investigational Domperidone The serum concentration of Domperidone can be decreased when it is combined with Tacrolimus. Approved, Investigational, Vet Approved Doxazosin The serum concentration of Tacrolimus can be increased when it is combined with Doxazosin. Approved Doxepin The serum concentration of Tacrolimus can be increased when it is combined with Doxepin. Approved Doxifluridine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Doxifluridine. Investigational Doxorubicin The risk or severity of adverse effects can be increased when Tacrolimus is combined with Doxorubicin. Approved, Investigational Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Tacrolimus. Approved, Investigational Doxorubicin The serum concentration of Doxorubicin can be decreased when it is combined with Tacrolimus. Approved, Investigational Doxycycline The metabolism of Tacrolimus can be decreased when combined with Doxycycline. Approved, Investigational, Vet Approved Dronabinol The serum concentration of Tacrolimus can be increased when it is combined with Dronabinol. Approved, Illicit Dronedarone Tacrolimus may increase the QTc-prolonging activities of Dronedarone. Approved Dronedarone The metabolism of Tacrolimus can be decreased when combined with Dronedarone. Approved Droxicam Droxicam may increase the nephrotoxic activities of Tacrolimus. Approved Dulaglutide The therapeutic efficacy of Dulaglutide can be decreased when used in combination with Tacrolimus. Approved Duvelisib Duvelisib may increase the nephrotoxic activities of Tacrolimus. Investigational E-6201 E6201 may increase the nephrotoxic activities of Tacrolimus. Investigational Ebselen Ebselen may increase the nephrotoxic activities of Tacrolimus. Investigational Ecabet The metabolism of Tacrolimus can be decreased when combined with Ecabet. Approved, Investigational Econazole The metabolism of Tacrolimus can be decreased when combined with Econazole. Approved Eculizumab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Eculizumab. Approved, Investigational Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Tacrolimus. Approved Edoxaban The metabolism of Tacrolimus can be decreased when combined with Edoxaban. Approved Efalizumab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Efalizumab. Approved, Investigational Efavirenz The serum concentration of Tacrolimus can be decreased when it is combined with Efavirenz. Approved, Investigational Efinaconazole The metabolism of Tacrolimus can be decreased when combined with Efinaconazole. Approved Efonidipine The serum concentration of Tacrolimus can be increased when it is combined with Efonidipine. Approved Elafin The metabolism of Tacrolimus can be decreased when combined with Elafin. Investigational Elbasvir The serum concentration of Tacrolimus can be increased when it is combined with Elbasvir. Approved Eletriptan The serum concentration of Eletriptan can be decreased when it is combined with Tacrolimus. Approved, Investigational Empagliflozin The therapeutic efficacy of Empagliflozin can be decreased when used in combination with Tacrolimus. Approved Enalapril The metabolism of Tacrolimus can be decreased when combined with Enalapril. Approved, Vet Approved Enalapril The serum concentration of Tacrolimus can be increased when it is combined with Enalapril. Approved, Vet Approved Enalaprilat The metabolism of Tacrolimus can be decreased when combined with Enalaprilat. Approved Enalkiren The metabolism of Tacrolimus can be decreased when combined with Enalkiren. Experimental Enzalutamide The serum concentration of Tacrolimus can be decreased when it is combined with Enzalutamide. Approved Epinastine The serum concentration of Epinastine can be decreased when it is combined with Tacrolimus. Approved, Investigational Epirizole Epirizole may increase the nephrotoxic activities of Tacrolimus. Approved Epirubicin The risk or severity of adverse effects can be increased when Tacrolimus is combined with Epirubicin. Approved Eplerenone Eplerenone may increase the hyperkalemic activities of Tacrolimus. Approved Ergonovine The serum concentration of Tacrolimus can be increased when it is combined with Ergonovine. Approved Ergotamine The serum concentration of Tacrolimus can be increased when it is combined with Ergotamine. Approved Erlotinib The serum concentration of Erlotinib can be decreased when it is combined with Tacrolimus. Approved, Investigational Ertapenem The serum concentration of Tacrolimus can be increased when it is combined with Ertapenem. Approved, Investigational Erythromycin The serum concentration of Tacrolimus can be increased when it is combined with Erythromycin. Approved, Vet Approved Erythromycin The metabolism of Tacrolimus can be decreased when combined with Erythromycin. Approved, Vet Approved Escitalopram The metabolism of Tacrolimus can be decreased when combined with Escitalopram. Approved, Investigational Eslicarbazepine acetate The serum concentration of Tacrolimus can be decreased when it is combined with Eslicarbazepine acetate. Approved Esomeprazole The serum concentration of Tacrolimus can be increased when it is combined with Esomeprazole. Approved, Investigational Estradiol The serum concentration of Estradiol can be decreased when it is combined with Tacrolimus. Approved, Investigational, Vet Approved Estramustine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Estramustine. Approved Estramustine The serum concentration of Tacrolimus can be increased when it is combined with Estramustine. Approved Estriol The serum concentration of Estriol can be decreased when it is combined with Tacrolimus. Approved, Vet Approved Estrone The serum concentration of Estrone can be decreased when it is combined with Tacrolimus. Approved Etanercept The risk or severity of adverse effects can be increased when Tacrolimus is combined with Etanercept. Approved, Investigational Etanercept Etanercept may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Ethanol Ethanol can cause an increase in the absorption of Tacrolimus resulting in an increased serum concentration and potentially a worsening of adverse effects. Approved Ethinyl Estradiol The serum concentration of Ethinyl Estradiol can be decreased when it is combined with Tacrolimus. Approved Etodolac Etodolac may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational, Vet Approved Etofenamate Etofenamate may increase the nephrotoxic activities of Tacrolimus. Approved Etoperidone The metabolism of Tacrolimus can be decreased when combined with Etoperidone. Approved Etoposide The risk or severity of adverse effects can be increased when Tacrolimus is combined with Etoposide. Approved Etoposide The serum concentration of Etoposide can be decreased when it is combined with Tacrolimus. Approved Etoricoxib Etoricoxib may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Etravirine The serum concentration of Tacrolimus can be decreased when it is combined with Etravirine. Approved Evening primrose oil Evening primrose oil may increase the nephrotoxic activities of Tacrolimus. Approved Everolimus The risk or severity of adverse effects can be increased when Tacrolimus is combined with Everolimus. Approved Everolimus The serum concentration of Everolimus can be increased when it is combined with Tacrolimus. Approved Exenatide The therapeutic efficacy of Exenatide can be decreased when used in combination with Tacrolimus. Approved, Investigational exisulind exisulind may increase the nephrotoxic activities of Tacrolimus. Investigational Ezetimibe The serum concentration of Ezetimibe can be decreased when it is combined with Tacrolimus. Approved Faldaprevir The metabolism of Tacrolimus can be decreased when combined with Bi201335. Investigational Felodipine The serum concentration of Tacrolimus can be increased when it is combined with Felodipine. Approved, Investigational Fenbufen Fenbufen may increase the nephrotoxic activities of Tacrolimus. Approved Fenfluramine The metabolism of Tacrolimus can be decreased when combined with Fenfluramine. Illicit, Withdrawn Fenofibrate Tacrolimus may increase the nephrotoxic activities of Fenofibrate. Approved Fenoprofen Fenoprofen may increase the nephrotoxic activities of Tacrolimus. Approved Fentanyl The serum concentration of Tacrolimus can be increased when it is combined with Fentanyl. Approved, Illicit, Investigational, Vet Approved Fesoterodine The serum concentration of Fesoterodine can be decreased when it is combined with Tacrolimus. Approved Fexofenadine The serum concentration of Fexofenadine can be decreased when it is combined with Tacrolimus. Approved Fidaxomicin The serum concentration of Fidaxomicin can be decreased when it is combined with Tacrolimus. Approved Fingolimod The risk or severity of adverse effects can be increased when Tacrolimus is combined with Fingolimod. Approved, Investigational Fingolimod Tacrolimus may increase the immunosuppressive activities of Fingolimod. Approved, Investigational Floctafenine Floctafenine may increase the nephrotoxic activities of Tacrolimus. Approved, Withdrawn Floxuridine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Floxuridine. Approved Fluconazole The metabolism of Tacrolimus can be decreased when combined with Fluconazole. Approved Fluconazole The serum concentration of Tacrolimus can be increased when it is combined with Fluconazole. Approved Flucytosine The metabolism of Tacrolimus can be decreased when combined with Flucytosine. Approved Fludarabine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Fludarabine. Approved Fludrocortisone The risk or severity of adverse effects can be increased when Tacrolimus is combined with Fludrocortisone. Approved Flunixin Flunixin may increase the nephrotoxic activities of Tacrolimus. Vet Approved Fluorouracil The risk or severity of adverse effects can be increased when Tacrolimus is combined with Fluorouracil. Approved Fluoxetine The metabolism of Tacrolimus can be decreased when combined with Fluoxetine. Approved, Vet Approved Fluoxetine The serum concentration of Tacrolimus can be increased when it is combined with Fluoxetine. Approved, Vet Approved Flupentixol The serum concentration of Tacrolimus can be increased when it is combined with Flupentixol. Approved, Withdrawn Fluphenazine The serum concentration of Tacrolimus can be increased when it is combined with Fluphenazine. Approved Flurazepam The serum concentration of Tacrolimus can be increased when it is combined with Flurazepam. Approved, Illicit Flurbiprofen Flurbiprofen may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Fluticasone furoate The serum concentration of Fluticasone furoate can be decreased when it is combined with Tacrolimus. Approved Fluvoxamine The metabolism of Tacrolimus can be decreased when combined with Fluvoxamine. Approved, Investigational Fosamprenavir The metabolism of Tacrolimus can be decreased when combined with Fosamprenavir. Approved Fosaprepitant The serum concentration of Tacrolimus can be increased when it is combined with Fosaprepitant. Approved Foscarnet Foscarnet may increase the nephrotoxic activities of Tacrolimus. Approved Fosinopril The metabolism of Tacrolimus can be decreased when combined with Fosinopril. Approved Fosphenytoin The metabolism of Tacrolimus can be increased when combined with Fosphenytoin. Approved Fosphenytoin The serum concentration of Tacrolimus can be decreased when it is combined with Fosphenytoin. Approved Fusidic Acid The serum concentration of Tacrolimus can be increased when it is combined with Fusidic Acid. Approved G17DT The risk or severity of adverse effects can be increased when Tacrolimus is combined with G17DT. Investigational Gabexate The metabolism of Tacrolimus can be decreased when combined with Gabexate. Investigational Gallium nitrate The risk or severity of adverse effects can be increased when Tacrolimus is combined with Gallium nitrate. Approved, Investigational Gefitinib The serum concentration of Gefitinib can be decreased when it is combined with Tacrolimus. Approved, Investigational Geldanamycin The metabolism of Tacrolimus can be decreased when combined with Geldanamycin. Experimental Gemcitabine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Gemcitabine. Approved Gemcitabine The serum concentration of Gemcitabine can be decreased when it is combined with Tacrolimus. Approved Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Tacrolimus is combined with Gemtuzumab ozogamicin. Approved Genistein The serum concentration of Tacrolimus can be increased when it is combined with Genistein. Investigational GI-5005 The risk or severity of adverse effects can be increased when Tacrolimus is combined with GI-5005. Investigational Glatiramer Acetate The risk or severity of adverse effects can be increased when Tacrolimus is combined with Glatiramer Acetate. Approved, Investigational Glibornuride The therapeutic efficacy of Glibornuride can be decreased when used in combination with Tacrolimus. Withdrawn Gliclazide The therapeutic efficacy of Gliclazide can be decreased when used in combination with Tacrolimus. Approved Glimepiride The risk or severity of adverse effects can be increased when Tacrolimus is combined with Glimepiride. Approved Glimepiride The therapeutic efficacy of Glimepiride can be decreased when used in combination with Tacrolimus. Approved Glipizide The therapeutic efficacy of Glipizide can be decreased when used in combination with Tacrolimus. Approved Gliquidone The therapeutic efficacy of Gliquidone can be decreased when used in combination with Tacrolimus. Approved Glyburide The serum concentration of Tacrolimus can be increased when it is combined with Glyburide. Approved Glyphosate The metabolism of Tacrolimus can be decreased when combined with Glyphosate. Experimental GM6001 The metabolism of Tacrolimus can be decreased when combined with GM6001. Experimental Golimumab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Golimumab. Approved Gramicidin D The serum concentration of Tacrolimus can be increased when it is combined with Gramicidin D. Approved Grazoprevir The serum concentration of Grazoprevir can be decreased when it is combined with Tacrolimus. Approved Grepafloxacin The serum concentration of Grepafloxacin can be decreased when it is combined with Tacrolimus. Withdrawn Griseofulvin The metabolism of Tacrolimus can be decreased when combined with Griseofulvin. Approved, Vet Approved GS 0573 The risk or severity of adverse effects can be increased when Tacrolimus is combined with 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine. Investigational Gusperimus The risk or severity of adverse effects can be increased when Tacrolimus is combined with Gusperimus. Investigational Gusperimus The therapeutic efficacy of Gusperimus can be decreased when used in combination with Tacrolimus. Investigational Haloperidol The serum concentration of Haloperidol can be decreased when it is combined with Tacrolimus. Approved Haloprogin The metabolism of Tacrolimus can be decreased when combined with Haloprogin. Approved, Withdrawn Hexetidine The metabolism of Tacrolimus can be decreased when combined with Hexetidine. Approved Higenamine Higenamine may increase the nephrotoxic activities of Tacrolimus. Investigational Human C1-esterase inhibitor The risk or severity of adverse effects can be increased when Tacrolimus is combined with C1 Esterase Inhibitor (Human). Approved Hydrocortisone The risk or severity of adverse effects can be increased when Tacrolimus is combined with Hydrocortisone. Approved, Vet Approved Hydrocortisone The serum concentration of Hydrocortisone can be decreased when it is combined with Tacrolimus. Approved, Vet Approved Hydroxyurea The risk or severity of adverse effects can be increased when Tacrolimus is combined with Hydroxyurea. Approved Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Tacrolimus is combined with Ibritumomab tiuxetan. Approved Ibrutinib The risk or severity of adverse effects can be increased when Tacrolimus is combined with Ibrutinib. Approved Ibuprofen Ibuprofen may increase the nephrotoxic activities of Tacrolimus. Approved Ibuprofen The serum concentration of Ibuprofen can be decreased when it is combined with Tacrolimus. Approved Ibuproxam Ibuproxam may increase the nephrotoxic activities of Tacrolimus. Withdrawn Icatibant The risk or severity of adverse effects can be increased when Tacrolimus is combined with Icatibant. Approved Icatibant Icatibant may increase the nephrotoxic activities of Tacrolimus. Approved Idarubicin The risk or severity of adverse effects can be increased when Tacrolimus is combined with Idarubicin. Approved Idelalisib The serum concentration of Tacrolimus can be increased when it is combined with Idelalisib. Approved Idelalisib The risk or severity of adverse effects can be increased when Tacrolimus is combined with Idelalisib. Approved Idraparinux The metabolism of Tacrolimus can be decreased when combined with idraparinux. Investigational Ifosfamide The risk or severity of adverse effects can be increased when Tacrolimus is combined with Ifosfamide. Approved Imatinib The risk or severity of adverse effects can be increased when Tacrolimus is combined with Imatinib. Approved Imatinib The metabolism of Tacrolimus can be decreased when combined with Imatinib. Approved Imidapril The metabolism of Tacrolimus can be decreased when combined with Imidapril. Investigational Imipramine The serum concentration of Imipramine can be decreased when it is combined with Tacrolimus. Approved Imiquimod The risk or severity of adverse effects can be increased when Tacrolimus is combined with Imiquimod. Approved, Investigational Indacaterol The serum concentration of Indacaterol can be decreased when it is combined with Tacrolimus. Approved Indalpine The metabolism of Tacrolimus can be decreased when combined with Indalpine. Investigational, Withdrawn Indinavir The metabolism of Tacrolimus can be decreased when combined with Indinavir. Approved Indomethacin The serum concentration of Indomethacin can be decreased when it is combined with Tacrolimus. Approved, Investigational Indomethacin Indomethacin may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Indoprofen Indoprofen may increase the nephrotoxic activities of Tacrolimus. Withdrawn Infliximab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Infliximab. Approved INGN 201 The risk or severity of adverse effects can be increased when Tacrolimus is combined with INGN 201. Investigational INGN 225 The risk or severity of adverse effects can be increased when Tacrolimus is combined with INGN 225. Investigational Insulin Aspart The therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Tacrolimus. Approved Insulin Detemir The therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Tacrolimus. Approved Insulin Glargine The therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Tacrolimus. Approved Insulin Glulisine The therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Tacrolimus. Approved Insulin Lispro The therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Tacrolimus. Approved Insulin Pork The therapeutic efficacy of Insulin Pork can be decreased when used in combination with Tacrolimus. Approved Irinotecan The risk or severity of adverse effects can be increased when Tacrolimus is combined with Irinotecan. Approved, Investigational Irinotecan The serum concentration of Irinotecan can be decreased when it is combined with Tacrolimus. Approved, Investigational Isavuconazonium The metabolism of Tacrolimus can be decreased when combined with Isavuconazonium. Approved, Investigational Isoconazole The metabolism of Tacrolimus can be decreased when combined with Isoconazole. Approved Isoflurophate The metabolism of Tacrolimus can be decreased when combined with Isoflurophate. Approved, Withdrawn Isoxicam Isoxicam may increase the nephrotoxic activities of Tacrolimus. Withdrawn Isradipine The metabolism of Tacrolimus can be decreased when combined with Isradipine. Approved Isradipine The serum concentration of Tacrolimus can be increased when it is combined with Isradipine. Approved Itraconazole The metabolism of Tacrolimus can be decreased when combined with Itraconazole. Approved, Investigational Itraconazole The serum concentration of Tacrolimus can be increased when it is combined with Itraconazole. Approved, Investigational Ivacaftor The serum concentration of Tacrolimus can be increased when it is combined with Ivacaftor. Approved Ivermectin The serum concentration of Ivermectin can be decreased when it is combined with Tacrolimus. Approved, Vet Approved Ixazomib The metabolism of Tacrolimus can be decreased when combined with Ixazomib. Approved Josamycin The serum concentration of Tacrolimus can be increased when it is combined with Josamycin. Approved Kebuzone Kebuzone may increase the nephrotoxic activities of Tacrolimus. Experimental Ketamine The serum concentration of Tacrolimus can be increased when it is combined with Ketamine. Approved, Vet Approved Ketazolam The serum concentration of Ketazolam can be decreased when it is combined with Tacrolimus. Approved Ketoconazole The metabolism of Tacrolimus can be decreased when combined with Ketoconazole. Approved, Investigational Ketoconazole The serum concentration of Tacrolimus can be increased when it is combined with Ketoconazole. Approved, Investigational Ketoprofen Ketoprofen may increase the nephrotoxic activities of Tacrolimus. Approved, Vet Approved Ketorolac Ketorolac may increase the nephrotoxic activities of Tacrolimus. Approved Kitasamycin The serum concentration of Tacrolimus can be increased when it is combined with Kitasamycin. Experimental L-Phenylalanine The risk or severity of adverse effects can be increased when Tacrolimus is combined with L-Phenylalanine. Approved, Nutraceutical Lamivudine The serum concentration of Lamivudine can be decreased when it is combined with Tacrolimus. Approved, Investigational Lamotrigine The serum concentration of Lamotrigine can be decreased when it is combined with Tacrolimus. Approved, Investigational Lansoprazole The serum concentration of Tacrolimus can be increased when it is combined with Lansoprazole. Approved, Investigational Lansoprazole The serum concentration of Lansoprazole can be decreased when it is combined with Tacrolimus. Approved, Investigational Lapatinib The serum concentration of Tacrolimus can be increased when it is combined with Lapatinib. Approved, Investigational Ledipasvir The serum concentration of Ledipasvir can be decreased when it is combined with Tacrolimus. Approved Leflunomide The risk or severity of adverse effects can be increased when Tacrolimus is combined with Leflunomide. Approved, Investigational Leflunomide Leflunomide may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Lenalidomide The risk or severity of adverse effects can be increased when Tacrolimus is combined with Lenalidomide. Approved Lenalidomide The serum concentration of Lenalidomide can be decreased when it is combined with Tacrolimus. Approved Lenvatinib The serum concentration of Lenvatinib can be decreased when it is combined with Tacrolimus. Approved Lepirudin The metabolism of Tacrolimus can be decreased when combined with Lepirudin. Approved Levetiracetam The serum concentration of Levetiracetam can be decreased when it is combined with Tacrolimus. Approved, Investigational Levofloxacin The serum concentration of Levofloxacin can be decreased when it is combined with Tacrolimus. Approved, Investigational Levofloxacin Levofloxacin may increase the QTc-prolonging activities of Tacrolimus. Approved, Investigational Levomilnacipran The metabolism of Tacrolimus can be decreased when combined with Levomilnacipran. Approved Levomilnacipran The serum concentration of Levomilnacipran can be decreased when it is combined with Tacrolimus. Approved Levothyroxine The serum concentration of Tacrolimus can be decreased when it is combined with Levothyroxine. Approved Lidocaine The serum concentration of Tacrolimus can be increased when it is combined with Lidocaine. Approved, Vet Approved Linagliptin The metabolism of Tacrolimus can be decreased when combined with Linagliptin. Approved Linagliptin The serum concentration of Linagliptin can be decreased when it is combined with Tacrolimus. Approved Liothyronine The serum concentration of Tacrolimus can be decreased when it is combined with Liothyronine. Approved, Vet Approved Liotrix The serum concentration of Tacrolimus can be decreased when it is combined with Liotrix. Approved Liraglutide The therapeutic efficacy of Liraglutide can be decreased when used in combination with Tacrolimus. Approved Lisinopril The metabolism of Tacrolimus can be decreased when combined with Lisinopril. Approved, Investigational Lisinopril The serum concentration of Tacrolimus can be increased when it is combined with Lisinopril. Approved, Investigational Lisofylline The risk or severity of adverse effects can be increased when Tacrolimus is combined with Lisofylline. Investigational Lisofylline Lisofylline may increase the nephrotoxic activities of Tacrolimus. Investigational Lomitapide The serum concentration of Tacrolimus can be increased when it is combined with Lomitapide. Approved Lomustine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Lomustine. Approved Loperamide The serum concentration of Loperamide can be decreased when it is combined with Tacrolimus. Approved Lopinavir The metabolism of Tacrolimus can be decreased when combined with Lopinavir. Approved Loratadine The serum concentration of Tacrolimus can be increased when it is combined with Loratadine. Approved Lornoxicam Lornoxicam may increase the nephrotoxic activities of Tacrolimus. Approved Losartan The serum concentration of Losartan can be decreased when it is combined with Tacrolimus. Approved Lovastatin The metabolism of Tacrolimus can be decreased when combined with Lovastatin. Approved, Investigational Loxoprofen Loxoprofen may increase the nephrotoxic activities of Tacrolimus. Approved Luliconazole The serum concentration of Tacrolimus can be increased when it is combined with Luliconazole. Approved Lumacaftor The serum concentration of Tacrolimus can be decreased when it is combined with Lumacaftor. Approved Lumiracoxib Lumiracoxib may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Magnesium salicylate Magnesium salicylate may increase the nephrotoxic activities of Tacrolimus. Approved Mannitol The serum concentration of Mannitol can be decreased when it is combined with Tacrolimus. Approved, Investigational Maprotiline The serum concentration of Tacrolimus can be increased when it is combined with Maprotiline. Approved Masoprocol Masoprocol may increase the nephrotoxic activities of Tacrolimus. Approved Mebendazole The serum concentration of Tacrolimus can be increased when it is combined with Mebendazole. Approved, Vet Approved Mechlorethamine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Mechlorethamine. Approved Meclofenamic acid Meclofenamic acid may increase the nephrotoxic activities of Tacrolimus. Approved, Vet Approved Mefenamic acid Mefenamic acid may increase the nephrotoxic activities of Tacrolimus. Approved Mefloquine The serum concentration of Tacrolimus can be increased when it is combined with Mefloquine. Approved Megestrol acetate The serum concentration of Tacrolimus can be increased when it is combined with Megestrol acetate. Approved, Vet Approved Meloxicam Meloxicam may increase the nephrotoxic activities of Tacrolimus. Approved, Vet Approved Melphalan The risk or severity of adverse effects can be increased when Tacrolimus is combined with Melphalan. Approved Mepolizumab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Mepolizumab. Approved, Investigational Meprobamate The serum concentration of Tacrolimus can be increased when it is combined with Meprobamate. Approved, Illicit Mercaptopurine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Mercaptopurine. Approved Mesalazine Mesalazine may increase the nephrotoxic activities of Tacrolimus. Approved Metamizole The risk or severity of adverse effects can be increased when Metamizole is combined with Tacrolimus. Withdrawn Metamizole Metamizole may increase the nephrotoxic activities of Tacrolimus. Withdrawn Metformin The therapeutic efficacy of Metformin can be decreased when used in combination with Tacrolimus. Approved Methadone The serum concentration of Tacrolimus can be increased when it is combined with Methadone. Approved Methotrexate The risk or severity of adverse effects can be increased when Tacrolimus is combined with Methotrexate. Approved Methotrexate The serum concentration of Methotrexate can be decreased when it is combined with Tacrolimus. Approved Methylprednisolone The risk or severity of adverse effects can be increased when Tacrolimus is combined with Methylprednisolone. Approved, Vet Approved Methylprednisolone The serum concentration of Methylprednisolone can be decreased when it is combined with Tacrolimus. Approved, Vet Approved Metoprolol The serum concentration of Metoprolol can be decreased when it is combined with Tacrolimus. Approved, Investigational Mevastatin The metabolism of Tacrolimus can be decreased when combined with Mevastatin. Experimental Mibefradil The serum concentration of Tacrolimus can be increased when it is combined with Mibefradil. Withdrawn Micafungin The metabolism of Tacrolimus can be decreased when combined with Micafungin. Approved, Investigational Miconazole The metabolism of Tacrolimus can be decreased when combined with Miconazole. Approved, Investigational, Vet Approved Miconazole The serum concentration of Tacrolimus can be increased when it is combined with Miconazole. Approved, Investigational, Vet Approved Midazolam The serum concentration of Midazolam can be decreased when it is combined with Tacrolimus. Approved, Illicit Mifepristone Mifepristone may increase the QTc-prolonging activities of Tacrolimus. Approved, Investigational Mifepristone The serum concentration of Tacrolimus can be increased when it is combined with Mifepristone. Approved, Investigational Miglitol The therapeutic efficacy of Miglitol can be decreased when used in combination with Tacrolimus. Approved Miglustat The therapeutic efficacy of Miglustat can be decreased when used in combination with Tacrolimus. Approved Milnacipran The metabolism of Tacrolimus can be decreased when combined with Milnacipran. Approved Miltefosine The metabolism of Tacrolimus can be decreased when combined with Miltefosine. Approved Mirabegron The serum concentration of Mirabegron can be decreased when it is combined with Tacrolimus. Approved Mitiglinide The therapeutic efficacy of Mitiglinide can be decreased when used in combination with Tacrolimus. Approved, Investigational Mitomycin The risk or severity of adverse effects can be increased when Tacrolimus is combined with Mitomycin. Approved Mitomycin The serum concentration of Tacrolimus can be increased when it is combined with Mitomycin. Approved Mitotane The serum concentration of Tacrolimus can be decreased when it is combined with Mitotane. Approved Mitoxantrone The risk or severity of adverse effects can be increased when Tacrolimus is combined with Mitoxantrone. Approved, Investigational Mitoxantrone The serum concentration of Mitoxantrone can be decreased when it is combined with Tacrolimus. Approved, Investigational Mizoribine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Mizoribine. Investigational Mizoribine Mizoribine may increase the nephrotoxic activities of Tacrolimus. Investigational Modafinil The serum concentration of Tacrolimus can be decreased when it is combined with Modafinil. Approved, Investigational Moexipril The metabolism of Tacrolimus can be decreased when combined with Moexipril. Approved Monensin The metabolism of Tacrolimus can be decreased when combined with Monensin. Vet Approved Morphine The serum concentration of Morphine can be decreased when it is combined with Tacrolimus. Approved, Investigational Muromonab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Muromonab. Approved, Investigational Mycophenolate mofetil The risk or severity of adverse effects can be increased when Tacrolimus is combined with Mycophenolate mofetil. Approved, Investigational Mycophenolate mofetil The serum concentration of Mycophenolate mofetil can be decreased when it is combined with Tacrolimus. Approved, Investigational Mycophenolate mofetil Mycophenolate mofetil may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Mycophenolic acid The risk or severity of adverse effects can be increased when Tacrolimus is combined with Mycophenolic acid. Approved Mycophenolic acid Mycophenolic acid may increase the nephrotoxic activities of Tacrolimus. Approved Myxothiazol The metabolism of Tacrolimus can be decreased when combined with Myxothiazol. Experimental N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-Proline The metabolism of Tacrolimus can be decreased when combined with N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-Proline. Experimental Nabumetone Nabumetone may increase the nephrotoxic activities of Tacrolimus. Approved Nadolol The serum concentration of Nadolol can be decreased when it is combined with Tacrolimus. Approved Nafamostat The risk or severity of adverse effects can be increased when Tacrolimus is combined with Nafamostat. Approved, Investigational Nafamostat The metabolism of Tacrolimus can be decreased when combined with Nafamostat. Approved, Investigational Nafcillin The serum concentration of Tacrolimus can be decreased when it is combined with Nafcillin. Approved Naftifine The metabolism of Tacrolimus can be decreased when combined with Naftifine. Approved Naftifine Naftifine may increase the nephrotoxic activities of Tacrolimus. Approved Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Tacrolimus. Approved Naloxone The serum concentration of Naloxone can be decreased when it is combined with Tacrolimus. Approved, Vet Approved Naltrexone The serum concentration of Tacrolimus can be increased when it is combined with Naltrexone. Approved, Investigational, Vet Approved Naproxen Naproxen may increase the nephrotoxic activities of Tacrolimus. Approved, Vet Approved Naringenin The serum concentration of Tacrolimus can be increased when it is combined with Naringenin. Experimental Natalizumab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Natalizumab. Approved, Investigational Natamycin The metabolism of Tacrolimus can be decreased when combined with Natamycin. Approved Nateglinide The therapeutic efficacy of Nateglinide can be decreased when used in combination with Tacrolimus. Approved, Investigational Nefazodone The metabolism of Tacrolimus can be decreased when combined with Nefazodone. Approved, Withdrawn Nelarabine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Nelarabine. Approved, Investigational Nelfinavir The metabolism of Tacrolimus can be decreased when combined with Nelfinavir. Approved Neostigmine The serum concentration of Tacrolimus can be increased when it is combined with Neostigmine. Approved, Vet Approved Nepafenac Nepafenac may increase the nephrotoxic activities of Tacrolimus. Approved Netupitant The serum concentration of Tacrolimus can be increased when it is combined with Netupitant. Approved Nevirapine The metabolism of Tacrolimus can be increased when combined with Nevirapine. Approved Nicardipine The serum concentration of Nicardipine can be decreased when it is combined with Tacrolimus. Approved Nicardipine The serum concentration of Tacrolimus can be increased when it is combined with Nicardipine. Approved Nifedipine The serum concentration of Tacrolimus can be decreased when it is combined with Nifedipine. Approved Nifedipine The serum concentration of Tacrolimus can be increased when it is combined with Nifedipine. Approved Niflumic Acid Niflumic Acid may increase the nephrotoxic activities of Tacrolimus. Approved Nilotinib The risk or severity of adverse effects can be increased when Tacrolimus is combined with Nilotinib. Approved, Investigational Nilotinib The metabolism of Tacrolimus can be decreased when combined with Nilotinib. Approved, Investigational Nimesulide Nimesulide may increase the nephrotoxic activities of Tacrolimus. Approved, Withdrawn Nimodipine The serum concentration of Tacrolimus can be increased when it is combined with Nimodipine. Approved Nintedanib The serum concentration of Nintedanib can be increased when it is combined with Tacrolimus. Approved Nisoldipine The serum concentration of Tacrolimus can be increased when it is combined with Nisoldipine. Approved Nitrazepam The serum concentration of Tacrolimus can be increased when it is combined with Nitrazepam. Approved Nitrendipine The serum concentration of Tacrolimus can be increased when it is combined with Nitrendipine. Approved Nitroaspirin The metabolism of Tacrolimus can be decreased when combined with Nitroaspirin. Investigational Nitroxoline The metabolism of Tacrolimus can be decreased when combined with Nitroxoline. Approved Nizatidine The serum concentration of Nizatidine can be decreased when it is combined with Tacrolimus. Approved Norethisterone The serum concentration of Tacrolimus can be decreased when it is combined with Norethisterone. Approved Nystatin The metabolism of Tacrolimus can be decreased when combined with Nystatin. Approved, Vet Approved Obinutuzumab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Obinutuzumab. Approved Olanzapine The metabolism of Tacrolimus can be decreased when combined with Olanzapine. Approved, Investigational Olanzapine The serum concentration of Olanzapine can be decreased when it is combined with Tacrolimus. Approved, Investigational Olaparib The metabolism of Tacrolimus can be decreased when combined with Olaparib. Approved Oleandomycin The serum concentration of Tacrolimus can be increased when it is combined with Oleandomycin. Vet Approved Olopatadine Olopatadine may increase the nephrotoxic activities of Tacrolimus. Approved Olsalazine Olsalazine may increase the nephrotoxic activities of Tacrolimus. Approved Omapatrilat The metabolism of Tacrolimus can be decreased when combined with Omapatrilat. Investigational Ombitasvir The serum concentration of Tacrolimus can be increased when it is combined with Ombitasvir. Approved Ombitasvir The serum concentration of Ombitasvir can be decreased when it is combined with Tacrolimus. Approved Omeprazole The serum concentration of Tacrolimus can be increased when it is combined with Omeprazole. Approved, Investigational, Vet Approved Orgotein Orgotein may increase the nephrotoxic activities of Tacrolimus. Vet Approved Osimertinib The serum concentration of Tacrolimus can be increased when it is combined with Osimertinib. Approved Otamixaban The metabolism of Tacrolimus can be decreased when combined with Otamixaban. Investigational Oxaliplatin The risk or severity of adverse effects can be increased when Tacrolimus is combined with Oxaliplatin. Approved, Investigational Oxaprozin Oxaprozin may increase the nephrotoxic activities of Tacrolimus. Approved Oxiconazole The metabolism of Tacrolimus can be decreased when combined with Oxiconazole. Approved Oxyphenbutazone Oxyphenbutazone may increase the nephrotoxic activities of Tacrolimus. Withdrawn P-Nitrophenol The serum concentration of Tacrolimus can be increased when it is combined with P-Nitrophenol. Experimental Paclitaxel The risk or severity of adverse effects can be increased when Tacrolimus is combined with Paclitaxel. Approved, Vet Approved Paclitaxel The serum concentration of Paclitaxel can be decreased when it is combined with Tacrolimus. Approved, Vet Approved pafuramidine The metabolism of Tacrolimus can be decreased when combined with pafuramidine. Investigational Palbociclib The risk or severity of adverse effects can be increased when Tacrolimus is combined with Palbociclib. Approved Palbociclib The serum concentration of Tacrolimus can be increased when it is combined with Palbociclib. Approved Palmitic Acid The serum concentration of Tacrolimus can be increased when it is combined with Palmitic Acid. Experimental Panobinostat The risk or severity of adverse effects can be increased when Tacrolimus is combined with Panobinostat. Approved, Investigational Panobinostat The serum concentration of Panobinostat can be decreased when it is combined with Tacrolimus. Approved, Investigational Pantoprazole The serum concentration of Tacrolimus can be increased when it is combined with Pantoprazole. Approved Parecoxib Parecoxib may increase the nephrotoxic activities of Tacrolimus. Approved Paritaprevir The serum concentration of Tacrolimus can be increased when it is combined with Paritaprevir. Approved Paroxetine The metabolism of Tacrolimus can be decreased when combined with Paroxetine. Approved, Investigational Paroxetine The serum concentration of Tacrolimus can be increased when it is combined with Paroxetine. Approved, Investigational Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Tacrolimus. Approved Pazopanib The risk or severity of adverse effects can be increased when Tacrolimus is combined with Pazopanib. Approved Pegaspargase The risk or severity of adverse effects can be increased when Tacrolimus is combined with Pegaspargase. Approved, Investigational Pemetrexed The risk or severity of adverse effects can be increased when Tacrolimus is combined with Pemetrexed. Approved, Investigational Pentamidine The metabolism of Tacrolimus can be decreased when combined with Pentamidine. Approved Pentobarbital The metabolism of Tacrolimus can be increased when combined with Pentobarbital. Approved, Vet Approved Pentostatin The risk or severity of adverse effects can be increased when Tacrolimus is combined with Pentostatin. Approved, Investigational Perindopril The metabolism of Tacrolimus can be decreased when combined with Perindopril. Approved Perindopril The serum concentration of Tacrolimus can be increased when it is combined with Perindopril. Approved Phenformin The therapeutic efficacy of Phenformin can be decreased when used in combination with Tacrolimus. Approved, Withdrawn Phenobarbital The metabolism of Tacrolimus can be increased when combined with Phenobarbital. Approved Phenylbutazone Phenylbutazone may increase the nephrotoxic activities of Tacrolimus. Approved, Vet Approved Phenytoin The metabolism of Tacrolimus can be increased when combined with Phenytoin. Approved, Vet Approved Phenytoin The serum concentration of Tacrolimus can be decreased when it is combined with Phenytoin. Approved, Vet Approved Phosphoramidon The metabolism of Tacrolimus can be decreased when combined with Phosphoramidon. Experimental Pimecrolimus The risk or severity of adverse effects can be increased when Pimecrolimus is combined with Tacrolimus. Approved, Investigational Pimecrolimus Pimecrolimus may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Pimozide The serum concentration of Tacrolimus can be increased when it is combined with Pimozide. Approved Pioglitazone The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Tacrolimus. Approved, Investigational Pirarubicin The risk or severity of adverse effects can be increased when Tacrolimus is combined with Pirarubicin. Investigational Pirfenidone Pirfenidone may increase the nephrotoxic activities of Tacrolimus. Investigational Pirfenidone The risk or severity of adverse effects can be increased when Tacrolimus is combined with Pirfenidone. Investigational Piroxicam Piroxicam may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Pitavastatin The serum concentration of Pitavastatin can be decreased when it is combined with Tacrolimus. Approved Platelet Activating Factor The serum concentration of Tacrolimus can be decreased when it is combined with Platelet Activating Factor. Experimental Pomalidomide The risk or severity of adverse effects can be increased when Tacrolimus is combined with Pomalidomide. Approved Pomalidomide The serum concentration of Pomalidomide can be decreased when it is combined with Tacrolimus. Approved Ponatinib The serum concentration of Ponatinib can be decreased when it is combined with Tacrolimus. Approved Posaconazole The metabolism of Tacrolimus can be decreased when combined with Posaconazole. Approved, Investigational, Vet Approved Posaconazole The serum concentration of Tacrolimus can be increased when it is combined with Posaconazole. Approved, Investigational, Vet Approved Pralatrexate The risk or severity of adverse effects can be increased when Tacrolimus is combined with Pralatrexate. Approved Pramlintide The therapeutic efficacy of Pramlintide can be decreased when used in combination with Tacrolimus. Approved, Investigational Pravastatin The serum concentration of Pravastatin can be decreased when it is combined with Tacrolimus. Approved Prazosin The serum concentration of Prazosin can be decreased when it is combined with Tacrolimus. Approved Prednisolone The risk or severity of adverse effects can be increased when Tacrolimus is combined with Prednisolone. Approved, Vet Approved Prednisolone The serum concentration of Prednisolone can be decreased when it is combined with Tacrolimus. Approved, Vet Approved Prednisone The risk or severity of adverse effects can be increased when Tacrolimus is combined with Prednisone. Approved, Vet Approved Prednisone The serum concentration of Prednisone can be decreased when it is combined with Tacrolimus. Approved, Vet Approved Primidone The metabolism of Tacrolimus can be increased when combined with Primidone. Approved, Vet Approved Prinomastat The metabolism of Tacrolimus can be decreased when combined with Prinomastat. Investigational Probenecid The serum concentration of Tacrolimus can be increased when it is combined with Probenecid. Approved Procarbazine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Procarbazine. Approved Progesterone The serum concentration of Tacrolimus can be decreased when it is combined with Progesterone. Approved, Vet Approved Promethazine The serum concentration of Tacrolimus can be increased when it is combined with Promethazine. Approved Propacetamol Propacetamol may increase the nephrotoxic activities of Tacrolimus. Approved Propafenone The serum concentration of Tacrolimus can be increased when it is combined with Propafenone. Approved Propranolol The serum concentration of Propranolol can be decreased when it is combined with Tacrolimus. Approved, Investigational Protriptyline The serum concentration of Tacrolimus can be increased when it is combined with Protriptyline. Approved Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Tacrolimus. Approved PTC299 PTC299 may increase the nephrotoxic activities of Tacrolimus. Investigational Quercetin The serum concentration of Tacrolimus can be increased when it is combined with Quercetin. Experimental Quetiapine The serum concentration of Quetiapine can be decreased when it is combined with Tacrolimus. Approved Quinacrine The serum concentration of Tacrolimus can be increased when it is combined with Quinacrine. Approved Quinapril The metabolism of Tacrolimus can be decreased when combined with Quinapril. Approved, Investigational Quinidine The serum concentration of Quinidine can be decreased when it is combined with Tacrolimus. Approved Quinine The serum concentration of Quinine can be decreased when it is combined with Tacrolimus. Approved Rabeprazole The serum concentration of Tacrolimus can be increased when it is combined with Rabeprazole. Approved, Investigational Rabies virus inactivated antigen, A The risk or severity of adverse effects can be increased when Tacrolimus is combined with Rabies vaccine. Approved Rabies virus inactivated antigen, A The therapeutic efficacy of Rabies vaccine can be decreased when used in combination with Tacrolimus. Approved Racecadotril The metabolism of Tacrolimus can be decreased when combined with Racecadotril. Investigational Radicicol The metabolism of Tacrolimus can be decreased when combined with Radicicol. Experimental Ramipril The metabolism of Tacrolimus can be decreased when combined with Ramipril. Approved Ranitidine The serum concentration of Ranitidine can be decreased when it is combined with Tacrolimus. Approved Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Tacrolimus. Approved, Investigational Reboxetine The serum concentration of Tacrolimus can be increased when it is combined with Reboxetine. Approved, Investigational Regorafenib The serum concentration of Tacrolimus can be increased when it is combined with Regorafenib. Approved Remikiren The metabolism of Tacrolimus can be decreased when combined with Remikiren. Approved Repaglinide The therapeutic efficacy of Repaglinide can be decreased when used in combination with Tacrolimus. Approved, Investigational Reserpine The serum concentration of Tacrolimus can be decreased when it is combined with Reserpine. Approved Resveratrol Resveratrol may increase the nephrotoxic activities of Tacrolimus. Experimental, Investigational Rifabutin The metabolism of Tacrolimus can be increased when combined with Rifabutin. Approved Rifabutin The serum concentration of Tacrolimus can be decreased when it is combined with Rifabutin. Approved Rifampicin The metabolism of Tacrolimus can be increased when combined with Rifampicin. Approved Rifampicin The serum concentration of Tacrolimus can be decreased when it is combined with Rifampicin. Approved Rifapentine The metabolism of Tacrolimus can be increased when combined with Rifapentine. Approved Rifapentine The serum concentration of Tacrolimus can be decreased when it is combined with Rifapentine. Approved Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Tacrolimus. Approved, Investigational Rilonacept The risk or severity of adverse effects can be increased when Tacrolimus is combined with Rilonacept. Approved Rilpivirine The serum concentration of Tacrolimus can be increased when it is combined with Rilpivirine. Approved Rindopepimut The risk or severity of adverse effects can be increased when Tacrolimus is combined with CDX-110. Investigational Risperidone The serum concentration of Risperidone can be decreased when it is combined with Tacrolimus. Approved, Investigational Ritonavir The metabolism of Tacrolimus can be decreased when combined with Ritonavir. Approved, Investigational Ritonavir The serum concentration of Tacrolimus can be increased when it is combined with Ritonavir. Approved, Investigational Rituximab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Rituximab. Approved Rivaroxaban The metabolism of Tacrolimus can be decreased when combined with Rivaroxaban. Approved Rivaroxaban The serum concentration of Rivaroxaban can be decreased when it is combined with Tacrolimus. Approved Rofecoxib Rofecoxib may increase the nephrotoxic activities of Tacrolimus. Investigational, Withdrawn Roflumilast Roflumilast may increase the immunosuppressive activities of Tacrolimus. Approved Rolapitant The serum concentration of Tacrolimus can be increased when it is combined with Rolapitant. Approved Romidepsin The serum concentration of Romidepsin can be decreased when it is combined with Tacrolimus. Approved, Investigational Rosiglitazone The therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Tacrolimus. Approved, Investigational Ruxolitinib The risk or severity of adverse effects can be increased when Tacrolimus is combined with Ruxolitinib. Approved Salicylamide Salicylamide may increase the nephrotoxic activities of Tacrolimus. Approved Salicylhydroxamic Acid The metabolism of Tacrolimus can be decreased when combined with Salicylhydroxamic Acid. Experimental Salicylic acid The metabolism of Tacrolimus can be decreased when combined with Salicylic acid. Approved, Vet Approved Salicylic acid The serum concentration of Salicylic acid can be decreased when it is combined with Tacrolimus. Approved, Vet Approved Salicylic acid Salicylic acid may increase the nephrotoxic activities of Tacrolimus. Approved, Vet Approved Salsalate Salsalate may increase the nephrotoxic activities of Tacrolimus. Approved Saquinavir The metabolism of Tacrolimus can be decreased when combined with Saquinavir. Approved, Investigational Saxagliptin The metabolism of Tacrolimus can be decreased when combined with Saxagliptin. Approved Saxagliptin The therapeutic efficacy of Saxagliptin can be decreased when used in combination with Tacrolimus. Approved Scopolamine The serum concentration of Tacrolimus can be increased when it is combined with Scopolamine. Approved Secukinumab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Secukinumab. Approved Selegiline The serum concentration of Tacrolimus can be increased when it is combined with Selegiline. Approved, Investigational, Vet Approved Selexipag The serum concentration of Selexipag can be decreased when it is combined with Tacrolimus. Approved Seocalcitol The risk or severity of adverse effects can be increased when Tacrolimus is combined with Seocalcitol. Experimental Seratrodast Seratrodast may increase the nephrotoxic activities of Tacrolimus. Approved Sertaconazole The metabolism of Tacrolimus can be decreased when combined with Sertaconazole. Approved Sertraline The metabolism of Tacrolimus can be decreased when combined with Sertraline. Approved Sertraline The serum concentration of Tacrolimus can be increased when it is combined with Sertraline. Approved Sevelamer The serum concentration of Tacrolimus can be decreased when it is combined with Sevelamer. Approved Sildenafil The metabolism of Tacrolimus can be decreased when combined with Sildenafil. Approved, Investigational Silodosin The serum concentration of Silodosin can be increased when it is combined with Tacrolimus. Approved Siltuximab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Siltuximab. Approved Siltuximab The serum concentration of Tacrolimus can be decreased when it is combined with Siltuximab. Approved Simeprevir The metabolism of Tacrolimus can be decreased when combined with Simeprevir. Approved Simeprevir The serum concentration of Tacrolimus can be increased when it is combined with Simeprevir. Approved Simvastatin The serum concentration of Tacrolimus can be increased when it is combined with Simvastatin. Approved Sinefungin The metabolism of Tacrolimus can be decreased when combined with Sinefungin. Experimental Sipuleucel-T The therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Tacrolimus. Approved Sirolimus The risk or severity of adverse effects can be increased when Tacrolimus is combined with Sirolimus. Approved, Investigational Sirolimus The serum concentration of Tacrolimus can be decreased when it is combined with Sirolimus. Approved, Investigational Sitagliptin The metabolism of Tacrolimus can be decreased when combined with Sitagliptin. Approved, Investigational Sitagliptin The serum concentration of Sitagliptin can be decreased when it is combined with Tacrolimus. Approved, Investigational Sofosbuvir The serum concentration of Sofosbuvir can be decreased when it is combined with Tacrolimus. Approved Solithromycin The serum concentration of Tacrolimus can be increased when it is combined with Solithromycin. Investigational Sorafenib The risk or severity of adverse effects can be increased when Tacrolimus is combined with Sorafenib. Approved, Investigational Sorafenib The serum concentration of Sorafenib can be decreased when it is combined with Tacrolimus. Approved, Investigational Sparfloxacin The serum concentration of Sparfloxacin can be decreased when it is combined with Tacrolimus. Approved Sphingosine The serum concentration of Sphingosine can be decreased when it is combined with Tacrolimus. Experimental Spirapril The metabolism of Tacrolimus can be decreased when combined with Spirapril. Approved Spironolactone Spironolactone may increase the hyperkalemic activities of Tacrolimus. Approved Spironolactone The serum concentration of Tacrolimus can be increased when it is combined with Spironolactone. Approved SRP 299 The risk or severity of adverse effects can be increased when Tacrolimus is combined with SRP 299. Investigational SRT501 SRT501 may increase the nephrotoxic activities of Tacrolimus. Investigational St. John's Wort The serum concentration of Tacrolimus can be decreased when it is combined with St. John's Wort. Nutraceutical Staurosporine The serum concentration of Tacrolimus can be increased when it is combined with Staurosporine. Experimental Stepronin The risk or severity of adverse effects can be increased when Tacrolimus is combined with Stepronin. Approved Stiripentol The serum concentration of Tacrolimus can be increased when it is combined with Stiripentol. Approved Streptozocin The risk or severity of adverse effects can be increased when Tacrolimus is combined with Streptozocin. Approved Streptozocin The serum concentration of Tacrolimus can be decreased when it is combined with Streptozocin. Approved Sulconazole The metabolism of Tacrolimus can be decreased when combined with Sulconazole. Approved Sulfasalazine Sulfasalazine may increase the nephrotoxic activities of Tacrolimus. Approved Sulfinpyrazone The serum concentration of Tacrolimus can be increased when it is combined with Sulfinpyrazone. Approved Sulfisoxazole The metabolism of Tacrolimus can be decreased when combined with Sulfisoxazole. Approved, Vet Approved Sulindac Sulindac may increase the nephrotoxic activities of Tacrolimus. Approved Sulodexide The therapeutic efficacy of Sulodexide can be decreased when used in combination with Tacrolimus. Approved, Investigational Sumatriptan The serum concentration of Tacrolimus can be increased when it is combined with Sumatriptan. Approved, Investigational Sunitinib The risk or severity of adverse effects can be increased when Tacrolimus is combined with Sunitinib. Approved, Investigational Sunitinib The serum concentration of Tacrolimus can be increased when it is combined with Sunitinib. Approved, Investigational Suprofen Suprofen may increase the nephrotoxic activities of Tacrolimus. Approved, Withdrawn Tacrine The serum concentration of Tacrolimus can be increased when it is combined with Tacrine. Withdrawn Tamoxifen The serum concentration of Tamoxifen can be decreased when it is combined with Tacrolimus. Approved Taurocholic Acid The serum concentration of Taurocholic Acid can be decreased when it is combined with Tacrolimus. Experimental Tavaborole The metabolism of Tacrolimus can be decreased when combined with Tavaborole. Approved Technetium Tc-99m sestamibi The serum concentration of Technetium Tc-99m sestamibi can be decreased when it is combined with Tacrolimus. Approved Telaprevir The metabolism of Tacrolimus can be decreased when combined with Telaprevir. Withdrawn Telaprevir The serum concentration of Tacrolimus can be increased when it is combined with Telaprevir. Withdrawn Telithromycin The metabolism of Tacrolimus can be decreased when combined with Telithromycin. Approved Telithromycin The serum concentration of Tacrolimus can be increased when it is combined with Telithromycin. Approved Telmisartan The serum concentration of Tacrolimus can be increased when it is combined with Telmisartan. Approved, Investigational Temocapril The metabolism of Tacrolimus can be decreased when combined with Temocapril. Experimental, Investigational Temozolomide The risk or severity of adverse effects can be increased when Tacrolimus is combined with Temozolomide. Approved, Investigational Temsirolimus The risk or severity of adverse effects can be increased when Tacrolimus is combined with Temsirolimus. Approved Temsirolimus The serum concentration of Temsirolimus can be decreased when it is combined with Tacrolimus. Approved Teniposide The risk or severity of adverse effects can be increased when Tacrolimus is combined with Teniposide. Approved Tenoxicam Tenoxicam may increase the nephrotoxic activities of Tacrolimus. Approved Tepoxalin The risk or severity of adverse effects can be increased when Tacrolimus is combined with Tepoxalin. Vet Approved Tepoxalin Tepoxalin may increase the nephrotoxic activities of Tacrolimus. Vet Approved Terazosin The serum concentration of Tacrolimus can be increased when it is combined with Terazosin. Approved Terbinafine The metabolism of Tacrolimus can be decreased when combined with Terbinafine. Approved, Investigational, Vet Approved Terconazole The metabolism of Tacrolimus can be decreased when combined with Terconazole. Approved Terfenadine The serum concentration of Tacrolimus can be increased when it is combined with Terfenadine. Withdrawn Teriflunomide The risk or severity of adverse effects can be increased when Tacrolimus is combined with Teriflunomide. Approved Teriflunomide Teriflunomide may increase the nephrotoxic activities of Tacrolimus. Approved Tesmilifene The serum concentration of Tacrolimus can be decreased when it is combined with Tesmilifene. Investigational Testosterone The serum concentration of Tacrolimus can be increased when it is combined with Testosterone. Approved, Investigational TG4010 The risk or severity of adverse effects can be increased when Tacrolimus is combined with TG4010. Investigational Thalidomide The risk or severity of adverse effects can be increased when Tacrolimus is combined with Thalidomide. Approved, Investigational, Withdrawn Thiorphan The metabolism of Tacrolimus can be decreased when combined with Thiorphan. Experimental Thiotepa The risk or severity of adverse effects can be increased when Tacrolimus is combined with Thiotepa. Approved Thymol The metabolism of Tacrolimus can be decreased when combined with Thymol. Approved Tiaprofenic acid Tiaprofenic acid may increase the nephrotoxic activities of Tacrolimus. Approved Ticagrelor The serum concentration of Ticagrelor can be decreased when it is combined with Tacrolimus. Approved Ticlopidine The metabolism of Tacrolimus can be decreased when combined with Ticlopidine. Approved Timolol The serum concentration of Timolol can be decreased when it is combined with Tacrolimus. Approved Tinoridine Tinoridine may increase the nephrotoxic activities of Tacrolimus. Investigational Tioconazole The metabolism of Tacrolimus can be decreased when combined with Tioconazole. Approved Tioguanine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Tioguanine. Approved Tipranavir The metabolism of Tacrolimus can be decreased when combined with Tipranavir. Approved, Investigational Tocilizumab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Tocilizumab. Approved Tocilizumab The serum concentration of Tacrolimus can be decreased when it is combined with Tocilizumab. Approved Tofacitinib Tacrolimus may increase the immunosuppressive activities of Tofacitinib. Approved, Investigational Tofacitinib The risk or severity of adverse effects can be increased when Tacrolimus is combined with Tofacitinib. Approved, Investigational Tolazamide The therapeutic efficacy of Tolazamide can be decreased when used in combination with Tacrolimus. Approved Tolbutamide The therapeutic efficacy of Tolbutamide can be decreased when used in combination with Tacrolimus. Approved Tolfenamic Acid Tolfenamic Acid may increase the nephrotoxic activities of Tacrolimus. Approved Tolmetin Tolmetin may increase the nephrotoxic activities of Tacrolimus. Approved Tolnaftate The metabolism of Tacrolimus can be decreased when combined with Tolnaftate. Approved, Vet Approved Tolvaptan The serum concentration of Tolvaptan can be decreased when it is combined with Tacrolimus. Approved Topotecan The serum concentration of Topotecan can be increased when it is combined with Tacrolimus. Approved, Investigational Topotecan The risk or severity of adverse effects can be increased when Tacrolimus is combined with Topotecan. Approved, Investigational Toremifene The serum concentration of Toremifene can be decreased when it is combined with Tacrolimus. Approved, Investigational Tositumomab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Tositumomab. Approved Trabectedin The risk or severity of adverse effects can be increased when Tacrolimus is combined with Trabectedin. Approved, Investigational Trandolapril The metabolism of Tacrolimus can be decreased when combined with Trandolapril. Approved Tranilast Tranilast may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Trastuzumab Trastuzumab may increase the neutropenic activities of Tacrolimus. Approved, Investigational Trastuzumab emtansine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Trastuzumab emtansine. Approved Trastuzumab emtansine The serum concentration of Trastuzumab emtansine can be decreased when it is combined with Tacrolimus. Approved Trazodone The metabolism of Tacrolimus can be decreased when combined with Trazodone. Approved, Investigational Trazodone The serum concentration of Tacrolimus can be decreased when it is combined with Trazodone. Approved, Investigational Tretinoin The risk or severity of adverse effects can be increased when Tacrolimus is combined with Tretinoin. Approved, Investigational, Nutraceutical Triamcinolone The risk or severity of adverse effects can be increased when Tacrolimus is combined with Triamcinolone. Approved, Vet Approved Triamterene Triamterene may increase the hyperkalemic activities of Tacrolimus. Approved Trifluoperazine The serum concentration of Tacrolimus can be increased when it is combined with Trifluoperazine. Approved Triflupromazine The serum concentration of Tacrolimus can be increased when it is combined with Triflupromazine. Approved, Vet Approved Trimethoprim The serum concentration of Tacrolimus can be decreased when it is combined with Trimethoprim. Approved, Vet Approved Trimetrexate The metabolism of Tacrolimus can be decreased when combined with Trimetrexate. Approved, Investigational Trimipramine The serum concentration of Tacrolimus can be increased when it is combined with Trimipramine. Approved Trofosfamide The risk or severity of adverse effects can be increased when Tacrolimus is combined with Trofosfamide. Investigational Troglitazone The therapeutic efficacy of Troglitazone can be decreased when used in combination with Tacrolimus. Withdrawn Tylosin The serum concentration of Tacrolimus can be increased when it is combined with Tylosin. Vet Approved Ubenimex The metabolism of Tacrolimus can be decreased when combined with Ubenimex. Experimental Ulinastatin The metabolism of Tacrolimus can be decreased when combined with Ulinastatin. Investigational Ulipristal The serum concentration of Ulipristal can be decreased when it is combined with Tacrolimus. Approved Umeclidinium The serum concentration of Umeclidinium can be decreased when it is combined with Tacrolimus. Approved Ustekinumab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Ustekinumab. Approved, Investigational Valdecoxib Valdecoxib may increase the nephrotoxic activities of Tacrolimus. Investigational, Withdrawn Vecuronium The serum concentration of Vecuronium can be decreased when it is combined with Tacrolimus. Approved Vedolizumab The risk or severity of adverse effects can be increased when Tacrolimus is combined with Vedolizumab. Approved Venetoclax The serum concentration of Venetoclax can be decreased when it is combined with Tacrolimus. Approved Venlafaxine The metabolism of Tacrolimus can be decreased when combined with Venlafaxine. Approved Verapamil The metabolism of Tacrolimus can be decreased when combined with Verapamil. Approved Vilanterol The risk or severity of adverse effects can be increased when Tacrolimus is combined with Vilanterol. Approved Vilazodone The metabolism of Tacrolimus can be decreased when combined with Vilazodone. Approved Vildagliptin The metabolism of Tacrolimus can be decreased when combined with Vildagliptin. Approved, Investigational Vildagliptin The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Tacrolimus. Approved, Investigational Vinblastine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Vinblastine. Approved Vinblastine The serum concentration of Vinblastine can be decreased when it is combined with Tacrolimus. Approved Vincristine The serum concentration of Vincristine can be decreased when it is combined with Tacrolimus. Approved, Investigational Vincristine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Vincristine. Approved, Investigational Vindesine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Vindesine. Approved Vinorelbine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Vinorelbine. Approved, Investigational Vinorelbine The serum concentration of Tacrolimus can be increased when it is combined with Vinorelbine. Approved, Investigational Vismodegib The serum concentration of Vismodegib can be decreased when it is combined with Tacrolimus. Approved Voclosporin The risk or severity of adverse effects can be increased when Tacrolimus is combined with Lx211. Investigational Voglibose The therapeutic efficacy of Voglibose can be decreased when used in combination with Tacrolimus. Approved, Investigational Voriconazole The metabolism of Tacrolimus can be decreased when combined with Voriconazole. Approved, Investigational Voriconazole The serum concentration of Tacrolimus can be increased when it is combined with Voriconazole. Approved, Investigational Vortioxetine The metabolism of Tacrolimus can be decreased when combined with Vortioxetine. Approved Ximelagatran The metabolism of Tacrolimus can be decreased when combined with Ximelagatran. Approved, Investigational, Withdrawn Zaltoprofen Zaltoprofen may increase the nephrotoxic activities of Tacrolimus. Approved Zidovudine The serum concentration of Zidovudine can be decreased when it is combined with Tacrolimus. Approved Zileuton Zileuton may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational, Withdrawn Zimelidine The metabolism of Tacrolimus can be decreased when combined with Zimelidine. Withdrawn Zimelidine The serum concentration of Tacrolimus can be increased when it is combined with Zimelidine. Withdrawn Ziprasidone The metabolism of Tacrolimus can be decreased when combined with Ziprasidone. Approved Zomepirac Zomepirac may increase the nephrotoxic activities of Tacrolimus. Withdrawn - Food Interactions
- Food, especially food with a high-fat content, decreases the rate and extent of absorption.
- The time of the meal affects tacrolimus bioavailability. Take tacrolimus capsules consistently everyday either with or without food.
References
- Synthesis Reference
Pan Sup Chang, Hoon Cho, "Water soluble polymer-tacrolimus conjugated compounds and process for preparing the same." U.S. Patent US5922729, issued April, 1997.
US5922729- General References
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- Pritchard DI: Sourcing a chemical succession for cyclosporin from parasites and human pathogens. Drug Discov Today. 2005 May 15;10(10):688-91. [PubMed:15896681 ]
- Liu J, Farmer JD Jr, Lane WS, Friedman J, Weissman I, Schreiber SL: Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK506 complexes. Cell. 1991 Aug 23;66(4):807-15. [PubMed:1715244 ]
- Fukatsu S, Fukudo M, Masuda S, Yano I, Katsura T, Ogura Y, Oike F, Takada Y, Inui K: Delayed effect of grapefruit juice on pharmacokinetics and pharmacodynamics of tacrolimus in a living-donor liver transplant recipient. Drug Metab Pharmacokinet. 2006 Apr;21(2):122-5. [PubMed:16702731 ]
- Hanifin JM, Paller AS, Eichenfield L, Clark RA, Korman N, Weinstein G, Caro I, Jaracz E, Rico MJ: Efficacy and safety of tacrolimus ointment treatment for up to 4 years in patients with atopic dermatitis. J Am Acad Dermatol. 2005 Aug;53(2 Suppl 2):S186-94. [PubMed:16021174 ]
- External Links
- Human Metabolome Database
- HMDB15002
- KEGG Drug
- D00107
- KEGG Compound
- C01375
- PubChem Compound
- 445643
- PubChem Substance
- 46506004
- ChemSpider
- 393220
- BindingDB
- 50030448
- ChEBI
- 61049
- ChEMBL
- CHEMBL269732
- Therapeutic Targets Database
- DAP000162
- PharmGKB
- PA451578
- HET
- FK5
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Tacrolimus
- ATC Codes
- D11AH01 — Tacrolimus
- D11AH — Agents for dermatitis, excluding corticosteroids
- D11A — OTHER DERMATOLOGICAL PREPARATIONS
- D11 — OTHER DERMATOLOGICAL PREPARATIONS
- D — DERMATOLOGICALS
- AHFS Codes
- 84:92.00
- 92:00.00
- PDB Entries
- FDA label
- Download (144 KB)
- MSDS
- Download (54.9 KB)
Clinical Trials
- Clinical Trials
Pharmacoeconomics
- Manufacturers
- Astellas pharma us inc
- Dr reddys laboratories ltd
- Sandoz inc
- Watson laboratories inc
- Astellas Pharma US
- Packagers
- Astellas Pharma Inc.
- B&B Pharmaceuticals
- Cardinal Health
- Caremark LLC
- Doctor Reddys Laboratories Ltd.
- Kaiser Foundation Hospital
- Mckesson Corp.
- Murfreesboro Pharmaceutical Nursing Supply
- Neuman Distributors Inc.
- Physicians Total Care Inc.
- Rebel Distributors Corp.
- Sandoz
- Watson Pharmaceuticals
- Dosage forms
Form Route Strength Capsule, extended release Oral 0.5 mg Capsule, extended release Oral 1 mg Capsule, extended release Oral 3 mg Capsule, extended release Oral 5 mg Capsule, coated, extended release Oral .5 mg/1 Capsule, coated, extended release Oral 1 mg/1 Capsule, coated, extended release Oral 5 mg/1 Tablet, extended release Oral 0.75 mg Tablet, extended release Oral 1 mg Tablet, extended release Oral 4 mg Tablet, extended release Oral .75 mg/1 Tablet, extended release Oral 1 mg/1 Tablet, extended release Oral 4 mg/1 Capsule Oral .5 mg/1 Capsule Oral 1 mg/1 Capsule Oral 5 mg/1 Granule Oral 0.2 mg Granule Oral 1 mg Capsule Oral 0.5 mg Capsule Oral 1 mg Capsule Oral 5 mg Capsule, gelatin coated Oral 1 mg/1 Injection, solution Intravenous 5 mg/mL Solution Intravenous 5 mg Ointment Cutaneous 0.03 % Ointment Cutaneous 0.1 % Ointment Topical 0.03 % Ointment Topical 0.1 % Capsule, gelatin coated Oral .5 mg/1 Capsule, gelatin coated Oral 5 mg/1 Ointment Topical .3 mg/g Ointment Topical 1 mg/g - Prices
Unit description Cost Unit Tacrolimus micronized powder 2800.0USD g Protopic 0.1% Ointment 60 gm Tube 255.34USD tube Protopic 0.03% Ointment 60 gm Tube 251.17USD tube Prograf 5 mg/ml ampule 163.94USD ml Protopic 0.03% Ointment 30 gm Tube 132.99USD tube Protopic 0.1% Ointment 30 gm Tube 124.42USD tube Prograf 5 mg capsule 24.26USD capsule Tacrolimus anhydrous 5 mg cap 22.3USD each Prograf 1 mg capsule 4.85USD capsule Tacrolimus 1 mg capsule 4.64USD capsule Tacrolimus anhydrous 1 mg cap 4.46USD each Protopic 0.1% ointment 4.17USD g Protopic 0.03% ointment 4.09USD g Prograf 0.5 mg capsule 2.43USD capsule Tacrolimus anhydrous 0.5 mg cap 2.23USD each DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) US5665727 No 1994-09-09 2014-09-09 US US5260301 No 1994-02-28 2011-02-28 US CA2037408 No 2002-12-17 2011-03-01 Canada CA1338491 No 1996-07-30 2013-07-30 Canada US6884433 No 1999-03-25 2019-03-25 US US6576259 No 1999-03-25 2019-03-25 US US8551522 No 1999-03-25 2019-03-25 US US6440458 No 1999-03-25 2019-03-25 US US9161907 No 2004-08-30 2024-08-30 US US8889186 No 2004-08-30 2024-08-30 US US8623411 No 2004-08-30 2024-08-30 US US8486993 No 2004-08-30 2024-08-30 US US8889185 No 2004-08-30 2024-08-30 US US8664239 No 2008-05-30 2028-05-30 US US8586084 No 2004-08-30 2024-08-30 US US8685998 No 2008-05-30 2028-05-30 US US8623410 No 2004-08-30 2024-08-30 US US8617599 No 2004-08-30 2024-08-30 US US7994214 No 2004-08-30 2024-08-30 US US8591946 No 2004-08-30 2024-08-30 US US9549918 No 2008-05-30 2028-05-30 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 126 °C Not Available water solubility Insoluble FDA label logP 3.3 Not Available - Predicted Properties
Property Value Source Water Solubility 0.00402 mg/mL ALOGPS logP 3.19 ALOGPS logP 5.59 ChemAxon logS -5.3 ALOGPS pKa (Strongest Acidic) 9.96 ChemAxon pKa (Strongest Basic) -2.9 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 11 ChemAxon Hydrogen Donor Count 3 ChemAxon Polar Surface Area 178.36 Å2 ChemAxon Rotatable Bond Count 7 ChemAxon Refractivity 215.62 m3·mol-1 ChemAxon Polarizability 87.41 Å3 ChemAxon Number of Rings 4 ChemAxon Bioavailability 0 ChemAxon Rule of Five No ChemAxon Ghose Filter No ChemAxon Veber's Rule No ChemAxon MDDR-like Rule Yes ChemAxon - Predicted ADMET features
Property Value Probability Human Intestinal Absorption - 0.8264 Blood Brain Barrier - 0.9659 Caco-2 permeable - 0.5977 P-glycoprotein substrate Substrate 0.7862 P-glycoprotein inhibitor I Inhibitor 0.8687 P-glycoprotein inhibitor II Inhibitor 0.7974 Renal organic cation transporter Non-inhibitor 0.8135 CYP450 2C9 substrate Non-substrate 0.9116 CYP450 2D6 substrate Non-substrate 0.9116 CYP450 3A4 substrate Substrate 0.7435 CYP450 1A2 substrate Non-inhibitor 0.8874 CYP450 2C9 inhibitor Non-inhibitor 0.9053 CYP450 2D6 inhibitor Non-inhibitor 0.9402 CYP450 2C19 inhibitor Non-inhibitor 0.8969 CYP450 3A4 inhibitor Non-inhibitor 0.869 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9807 Ames test Non AMES toxic 0.6355 Carcinogenicity Non-carcinogens 0.9422 Biodegradation Not ready biodegradable 0.9698 Rat acute toxicity 2.7541 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9817 hERG inhibition (predictor II) Non-inhibitor 0.8733
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted LC-MS/MS Spectrum - 10V, Positive Predicted LC-MS/MS Not Available Predicted LC-MS/MS Spectrum - 20V, Positive Predicted LC-MS/MS Not Available Predicted LC-MS/MS Spectrum - 40V, Positive Predicted LC-MS/MS Not Available Predicted LC-MS/MS Spectrum - 10V, Negative Predicted LC-MS/MS Not Available Predicted LC-MS/MS Spectrum - 20V, Negative Predicted LC-MS/MS Not Available Predicted LC-MS/MS Spectrum - 40V, Negative Predicted LC-MS/MS Not Available
Taxonomy
- Description
- This compound belongs to the class of organic compounds known as macrolide lactams. These are cyclic polyketides containing both a cyclic amide and a cyclic ester group.
- Kingdom
- Organic compounds
- Super Class
- Phenylpropanoids and polyketides
- Class
- Macrolide lactams
- Sub Class
- Not Available
- Direct Parent
- Macrolide lactams
- Alternative Parents
- Alpha amino acid esters / Macrolides and analogues / Cyclohexanols / Piperidines / Oxanes / Tertiary carboxylic acid amides / Carboxylic acid esters / Cyclic alcohols and derivatives / Cyclic ketones / Hemiacetals show 10 more
- Substituents
- Macrolide lactam / Alpha-amino acid ester / Macrolide / Alpha-amino acid or derivatives / Cyclohexanol / Oxane / Piperidine / Cyclic alcohol / Tertiary carboxylic acid amide / Cyclic ketone show 24 more
- Molecular Framework
- Aliphatic heteropolycyclic compounds
- External Descriptors
- macrolide (CHEBI:61049 ) / Macrolides and lactone polyketides (C01375 ) / Macrolides and lactone polyketides (LMPK04000003 )
Targets
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Type i transforming growth factor beta receptor binding
- Specific Function
- Keeps in an inactive conformation TGFBR1, the TGF-beta type I serine/threonine kinase receptor, preventing TGF-beta receptor activation in absence of ligand. Recruites SMAD7 to ACVR1B which prevent...
- Gene Name
- FKBP1A
- Uniprot ID
- P62942
- Uniprot Name
- Peptidyl-prolyl cis-trans isomerase FKBP1A
- Molecular Weight
- 11950.665 Da
References
- Labrande C, Velly L, Canolle B, Guillet B, Masmejean F, Nieoullon A, Pisano P: Neuroprotective effects of tacrolimus (FK506) in a model of ischemic cortical cell cultures: role of glutamate uptake and FK506 binding protein 12 kDa. Neuroscience. 2006;137(1):231-9. Epub 2005 Nov 10. [PubMed:16289353 ]
- Masri M, Rizk S, Barbari A, Stephan A, Kamel G, Rost M: An assay for the determination of sirolimus levels in the lymphocyte of transplant patients. Transplant Proc. 2007 May;39(4):1204-6. [PubMed:17524933 ]
Enzymes
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
- Ekins S, Bravi G, Wikel JH, Wrighton SA: Three-dimensional-quantitative structure activity relationship analysis of cytochrome P-450 3A4 substrates. J Pharmacol Exp Ther. 1999 Oct;291(1):424-33. [PubMed:10490933 ]
- Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Oxygen binding
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
- Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Oxygen binding
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP3A7
- Uniprot ID
- P24462
- Uniprot Name
- Cytochrome P450 3A7
- Molecular Weight
- 57525.03 Da
References
- Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Carriers
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Not Available
- Specific Function
- Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...
- Gene Name
- ORM1
- Uniprot ID
- P02763
- Uniprot Name
- Alpha-1-acid glycoprotein 1
- Molecular Weight
- 23511.38 Da
Transporters
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitorInducer
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Schuetz EG, Beck WT, Schuetz JD: Modulators and substrates of P-glycoprotein and cytochrome P4503A coordinately up-regulate these proteins in human colon carcinoma cells. Mol Pharmacol. 1996 Feb;49(2):311-8. [PubMed:8632764 ]
- Saeki T, Ueda K, Tanigawara Y, Hori R, Komano T: Human P-glycoprotein transports cyclosporin A and FK506. J Biol Chem. 1993 Mar 25;268(9):6077-80. [PubMed:7681059 ]
- Wandel C, Kim RB, Kajiji S, Guengerich P, Wilkinson GR, Wood AJ: P-glycoprotein and cytochrome P-450 3A inhibition: dissociation of inhibitory potencies. Cancer Res. 1999 Aug 15;59(16):3944-8. [PubMed:10463589 ]
- Hashida T, Masuda S, Uemoto S, Saito H, Tanaka K, Inui K: Pharmacokinetic and prognostic significance of intestinal MDR1 expression in recipients of living-donor liver transplantation. Clin Pharmacol Ther. 2001 May;69(5):308-16. [PubMed:11371998 ]
- Collett A, Tanianis-Hughes J, Hallifax D, Warhurst G: Predicting P-glycoprotein effects on oral absorption: correlation of transport in Caco-2 with drug pharmacokinetics in wild-type and mdr1a(-/-) mice in vivo. Pharm Res. 2004 May;21(5):819-26. [PubMed:15180340 ]
- Quezada CA, Garrido WX, Gonzalez-Oyarzun MA, Rauch MC, Salas MR, San Martin RE, Claude AA, Yanez AJ, Slebe JC, Carcamo JG: Effect of tacrolimus on activity and expression of P-glycoprotein and ATP-binding cassette transporter A5 (ABCA5) proteins in hematoencephalic barrier cells. Biol Pharm Bull. 2008 Oct;31(10):1911-6. [PubMed:18827354 ]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Atpase activity, coupled to transmembrane movement of substances
- Specific Function
- May play a role in the processing of autolysosomes.
- Gene Name
- ABCA5
- Uniprot ID
- Q8WWZ7
- Uniprot Name
- ATP-binding cassette sub-family A member 5
- Molecular Weight
- 186505.825 Da
References
- Quezada CA, Garrido WX, Gonzalez-Oyarzun MA, Rauch MC, Salas MR, San Martin RE, Claude AA, Yanez AJ, Slebe JC, Carcamo JG: Effect of tacrolimus on activity and expression of P-glycoprotein and ATP-binding cassette transporter A5 (ABCA5) proteins in hematoencephalic barrier cells. Biol Pharm Bull. 2008 Oct;31(10):1911-6. [PubMed:18827354 ]
Drug created on June 13, 2005 07:24 / Updated on September 01, 2017 15:53