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
- 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
- Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Advagraf Capsule, extended release 3 mg Oral Astellas Pharma Inc 2010-04-05 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 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 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 0.5 mg Oral Astellas Pharma Inc 2008-04-09 Not applicable Canada Advagraf Capsule, extended release 5 mg Oral Astellas Pharma Europe Bv 2007-04-23 Not applicable EU - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Ach-tacrolimus Capsule 0.5 mg Oral Accord Healthcare Limited Not applicable Not applicable Canada Ach-tacrolimus Capsule 1 mg Oral Accord Healthcare Limited Not applicable Not applicable Canada Ach-tacrolimus Capsule 5 mg Oral Accord Healthcare Limited Not applicable Not applicable Canada Apo-tacrolimus Capsule 5 mg Oral Apotex Corporation Not applicable Not applicable Canada Apo-tacrolimus Capsule 1 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 2018-01-06 US Hecoria Capsule 1 mg/1 Oral Novartis 2011-12-20 2018-01-06 US Hecoria Capsule .5 mg/1 Oral Novartis 2011-12-20 2018-01-06 US Jamp-tacrolimus Capsule 1 mg Oral Jamp Pharma Corporation Not applicable Not applicable Canada - Categories
- Antineoplastic and Immunomodulating Agents
- Calcineurin Inhibitor Immunosuppressant
- Calcineurin Inhibitors
- Combined Inhibitors of CYP3A4 and P-glycoprotein
- CYP3A Substrates (Sensitive)
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 CYP3A7 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- Enzyme Inhibitors
- Hyperglycemia-Associated Agents
- Immunologic Factors
- Immunosuppressive Agents
- Lactones
- Macrolides
- Misc. Skin and Mucous Membrane Agents
- 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 (4R)-limonene (4R)-limonene may increase the nephrotoxic activities of Tacrolimus. Investigational 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 Tacrolimus may increase the immunosuppressive activities of 2-Methoxyethanol. Experimental 2,4-thiazolidinedione The therapeutic efficacy of 2,4-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 Tacrolimus may increase the immunosuppressive activities of Abatacept. Approved Abetimus Tacrolimus may increase the immunosuppressive activities of Abetimus. Investigational Acarbose The therapeutic efficacy of Acarbose can be decreased when used in combination with Tacrolimus. Approved, Investigational Aceclofenac Aceclofenac may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Acemetacin Acemetacin may increase the nephrotoxic activities of Tacrolimus. Approved, Experimental, Investigational Acetohexamide The therapeutic efficacy of Acetohexamide can be decreased when used in combination with Tacrolimus. Approved, Investigational, Withdrawn Acetylsalicylic acid Acetylsalicylic acid may increase the nephrotoxic activities of Tacrolimus. Approved, Vet Approved Acteoside Tacrolimus may increase the immunosuppressive activities of Acteoside. Investigational Adalimumab Tacrolimus may increase the immunosuppressive activities of Adalimumab. Approved Adapalene Adapalene may increase the nephrotoxic activities of Tacrolimus. Approved Adefovir Tacrolimus may increase the immunosuppressive activities of Adefovir. Investigational Afatinib The serum concentration of Afatinib can be decreased when it is combined with Tacrolimus. Approved Afelimomab Tacrolimus may increase the immunosuppressive activities of Afelimomab. Investigational AICA ribonucleotide The therapeutic efficacy of AICA ribonucleotide can be decreased when used in combination with Tacrolimus. Experimental, Investigational Alaproclate The metabolism of Tacrolimus can be decreased when combined with Alaproclate. Experimental Alclofenac Alclofenac may increase the nephrotoxic activities of Tacrolimus. Approved, Withdrawn Alefacept Tacrolimus may increase the immunosuppressive activities of Alefacept. Approved, Investigational, Withdrawn Alemtuzumab Tacrolimus may increase the immunosuppressive activities of Alemtuzumab. Approved, Investigational Alicaforsen Tacrolimus may increase the immunosuppressive activities of Alicaforsen. Investigational Allicin The therapeutic efficacy of Allicin can be decreased when used in combination with Tacrolimus. Investigational Alminoprofen Alminoprofen may increase the nephrotoxic activities of Tacrolimus. Experimental Alogliptin The metabolism of Tacrolimus can be decreased when combined with Alogliptin. Approved Alpha-1-proteinase inhibitor The metabolism of Tacrolimus can be decreased when combined with Alpha-1-proteinase inhibitor. Approved Altretamine Tacrolimus may increase the immunosuppressive activities of Altretamine. Approved Amiloride The risk or severity of hyperkalemia can be increased when Amiloride is combined with Tacrolimus. Approved Amiodarone The metabolism of Tacrolimus can be decreased when combined with Amiodarone. Approved, Investigational 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, Investigational 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, Investigational Amsacrine Tacrolimus may increase the immunosuppressive activities of Amsacrine. Approved, Investigational Anakinra Tacrolimus may increase the immunosuppressive activities of Anakinra. Approved Andrographolide Andrographolide 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 Anthrax immune globulin human The risk or severity of adverse effects can be increased when Tacrolimus is combined with Anthrax immune globulin human. Approved Antilymphocyte immunoglobulin (horse) Tacrolimus may increase the immunosuppressive activities of Antilymphocyte immunoglobulin (horse). Approved, Investigational Antipyrine Antipyrine may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Antithrombin III human The metabolism of Tacrolimus can be decreased when combined with Antithrombin III human. Approved Antithymocyte immunoglobulin (rabbit) Tacrolimus may increase the immunosuppressive activities of Antithymocyte immunoglobulin (rabbit). Approved Apalutamide The serum concentration of Tacrolimus can be decreased when it is combined with Apalutamide. Approved, Investigational Apixaban The metabolism of Tacrolimus can be decreased when combined with Apixaban. Approved Apocynin Apocynin may increase the nephrotoxic activities of Tacrolimus. Investigational Apremilast Tacrolimus may increase the immunosuppressive activities of Apremilast. 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, Investigational, Withdrawn Argatroban The metabolism of Tacrolimus can be decreased when combined with Argatroban. Approved, Investigational Artemether The metabolism of Tacrolimus can be decreased when combined with Artemether. Approved Asunaprevir The metabolism of Tacrolimus can be decreased when combined with Asunaprevir. Approved, Investigational, Withdrawn Atazanavir The metabolism of Tacrolimus can be decreased when combined with Atazanavir. Approved, Investigational Atomoxetine The metabolism of Tacrolimus can be decreased when combined with Atomoxetine. Approved Atorvastatin The risk or severity of adverse effects can be increased when Tacrolimus is combined with Atorvastatin. Approved Azacitidine Tacrolimus may increase the immunosuppressive activities of Azacitidine. Approved, Investigational Azapropazone Azapropazone may increase the nephrotoxic activities of Tacrolimus. Withdrawn Azathioprine Tacrolimus may increase the immunosuppressive activities of Azathioprine. 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 Bacillus calmette-guerin substrain connaught live antigen The risk or severity of adverse effects can be increased when Tacrolimus is combined with Bacillus calmette-guerin substrain connaught live antigen. Approved, Investigational Bacillus calmette-guerin substrain tice live antigen The risk or severity of adverse effects can be increased when Tacrolimus is combined with Bacillus calmette-guerin substrain tice live antigen. 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 Tacrolimus may increase the immunosuppressive activities of Basiliximab. Approved, Investigational Batimastat The metabolism of Tacrolimus can be decreased when combined with Batimastat. Experimental BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Tacrolimus. Investigational Begelomab Tacrolimus may increase the immunosuppressive activities of Begelomab. Experimental, Investigational Belatacept Tacrolimus may increase the immunosuppressive activities of Belatacept. Approved, Investigational Belimumab Tacrolimus may increase the immunosuppressive activities of Belimumab. Approved Bempedoic acid The therapeutic efficacy of Bempedoic acid can be decreased when used in combination with Tacrolimus. Investigational Benazepril The metabolism of Tacrolimus can be decreased when combined with Benazepril. Approved, Investigational Bendazac Bendazac may increase the nephrotoxic activities of Tacrolimus. Experimental Benorilate Benorilate may increase the nephrotoxic activities of Tacrolimus. Experimental Benoxaprofen Benoxaprofen may increase the nephrotoxic activities of Tacrolimus. Withdrawn Benzamidine The metabolism of Tacrolimus can be decreased when combined with Benzamidine. Experimental Benznidazole Tacrolimus may increase the immunosuppressive activities of Benznidazole. Approved, Investigational Benzoic Acid The metabolism of Tacrolimus can be decreased when combined with Benzoic Acid. Approved, Investigational Benzydamine Benzydamine may increase the nephrotoxic activities of Tacrolimus. Approved Betamethasone Tacrolimus may increase the immunosuppressive activities of Betamethasone. Approved, Vet Approved Bevonium Bevonium may increase the nephrotoxic activities of Tacrolimus. Experimental Bifonazole The metabolism of Tacrolimus can be decreased when combined with Bifonazole. Approved, Investigational Bivalirudin The metabolism of Tacrolimus can be decreased when combined with Bivalirudin. Approved, Investigational Bleomycin Tacrolimus may increase the immunosuppressive activities of Bleomycin. Approved, Investigational Blinatumomab Tacrolimus may increase the immunosuppressive activities of Blinatumomab. Approved, Investigational Boceprevir The serum concentration of Tacrolimus can be increased when it is combined with Boceprevir. Approved, 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 Brefeldin A The metabolism of Tacrolimus can be decreased when combined with Brefeldin A. Experimental Brentuximab vedotin Tacrolimus may increase the immunosuppressive activities of Brentuximab vedotin. Approved, Investigational Briakinumab Tacrolimus may increase the immunosuppressive activities of Briakinumab. Investigational Brigatinib The serum concentration of Tacrolimus can be decreased when it is combined with Brigatinib. Approved, Investigational Brodalumab Tacrolimus may increase the immunosuppressive activities of Brodalumab. Approved, Investigational Bromfenac Bromfenac may increase the nephrotoxic activities of Tacrolimus. Approved Bromocriptine The risk or severity of adverse effects can be increased when Bromocriptine is combined with Tacrolimus. Approved, Investigational Bucillamine Bucillamine may increase the nephrotoxic activities of Tacrolimus. Investigational Budesonide Tacrolimus may increase the immunosuppressive activities of Budesonide. Approved Bufexamac Bufexamac may increase the nephrotoxic activities of Tacrolimus. Approved, Experimental Buformin The therapeutic efficacy of Buformin can be decreased when used in combination with Tacrolimus. Investigational, Withdrawn Bumadizone Bumadizone may increase the nephrotoxic activities of Tacrolimus. Experimental Busulfan Tacrolimus may increase the immunosuppressive activities of 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 Tacrolimus may increase the immunosuppressive activities of Cabazitaxel. Approved Cabergoline The risk or severity of adverse effects can be increased when Cabergoline is combined with Tacrolimus. Approved Camostat The metabolism of Tacrolimus can be decreased when combined with Camostat. Experimental Canagliflozin The therapeutic efficacy of Canagliflozin can be decreased when used in combination with Tacrolimus. Approved Canakinumab Tacrolimus may increase the immunosuppressive activities of Canakinumab. Approved, Investigational 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 Tacrolimus may increase the immunosuppressive activities of Capecitabine. Approved, Investigational Capric acid The metabolism of Tacrolimus can be decreased when combined with Capric acid. Experimental Captopril The metabolism of Tacrolimus can be decreased when combined with Captopril. Approved Carbamazepine The metabolism of Tacrolimus can be increased when combined with Carbamazepine. Approved, Investigational Carbaspirin calcium Carbaspirin calcium may increase the nephrotoxic activities of Tacrolimus. Experimental, Investigational Carbomycin The serum concentration of Tacrolimus can be increased when it is combined with Carbomycin. Vet Approved Carboplatin Tacrolimus may increase the immunosuppressive activities of Carboplatin. Approved Carbutamide The therapeutic efficacy of Carbutamide can be decreased when used in combination with Tacrolimus. Experimental Carmustine Tacrolimus may increase the immunosuppressive activities of Carmustine. Approved, Investigational Carprofen Carprofen may increase the nephrotoxic activities of Tacrolimus. Approved, Vet Approved, Withdrawn Caspofungin The serum concentration of Tacrolimus can be decreased when it is combined with Caspofungin. Approved Castanospermine Tacrolimus may increase the immunosuppressive activities of Castanospermine. 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 increased when it is combined with Tacrolimus. Approved, Withdrawn Certolizumab pegol Tacrolimus may increase the immunosuppressive activities of Certolizumab pegol. Approved Cerulenin The metabolism of Tacrolimus can be decreased when combined with Cerulenin. Approved Chlorambucil Tacrolimus may increase the immunosuppressive activities of Chlorambucil. Approved Chloramphenicol The serum concentration of Tacrolimus can be increased when it is combined with Chloramphenicol. Approved, Vet Approved Chloroquine Chloroquine may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational, Vet Approved Chloroxine The metabolism of Tacrolimus can be decreased when combined with Chloroxine. Approved Chlorpropamide The therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Tacrolimus. Approved, Investigational Cholesterol The metabolism of Tacrolimus can be decreased when combined with Cholesterol. Approved, Experimental, Investigational Choline magnesium trisalicylate Choline magnesium trisalicylate 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, Investigational Cilazapril The metabolism of Tacrolimus can be decreased when combined with Cilazapril. Approved Cinacalcet The serum concentration of Tacrolimus can be decreased when it is combined with Cinacalcet. Approved Cisplatin Tacrolimus may increase the immunosuppressive activities of Cisplatin. Approved Citalopram The metabolism of Tacrolimus can be decreased when combined with Citalopram. Approved Cladribine Tacrolimus may increase the immunosuppressive activities of Cladribine. Approved, Investigational 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, Investigational Clevidipine The serum concentration of Tacrolimus can be increased when it is combined with Clevidipine. Approved, Investigational Clofarabine Tacrolimus may increase the immunosuppressive activities of Clofarabine. Approved, Investigational Clomipramine The metabolism of Tacrolimus can be decreased when combined with Clomipramine. Approved, Investigational, Vet Approved Clonixin Clonixin may increase the nephrotoxic activities of Tacrolimus. Approved Clostridium tetani toxoid antigen (formaldehyde inactivated) The risk or severity of adverse effects can be increased when Tacrolimus is combined with Clostridium tetani toxoid antigen (formaldehyde inactivated). 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 Colchicine The serum concentration of Colchicine can be increased when it is combined with Tacrolimus. Approved Conivaptan The serum concentration of Conivaptan can be increased when it is combined with Tacrolimus. Approved, Investigational Cordycepin The metabolism of Tacrolimus can be decreased when combined with Cordycepin. Investigational Corticotropin Tacrolimus may increase the immunosuppressive activities of Corticotropin. Approved, Investigational, Vet Approved Cortisone acetate Tacrolimus may increase the immunosuppressive activities of Cortisone acetate. Approved, Investigational Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated) The risk or severity of adverse effects can be increased when Tacrolimus is combined with Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated). Approved Crizotinib The serum concentration of Tacrolimus can be increased when it is combined with Crizotinib. Approved Curcumin Curcumin may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Cyclophosphamide Tacrolimus may increase the immunosuppressive activities of Cyclophosphamide. Approved, Investigational Cyclosporine Tacrolimus may increase the nephrotoxic activities of Cyclosporine. Approved, Investigational, Vet Approved Cytarabine Tacrolimus may increase the immunosuppressive activities of Cytarabine. Approved, Investigational Dabigatran etexilate The serum concentration of Dabigatran etexilate can be decreased when it is combined with Tacrolimus. Approved Dabrafenib The serum concentration of Tacrolimus can be decreased when it is combined with Dabrafenib. Approved, Investigational Dacarbazine Tacrolimus may increase the immunosuppressive activities of Dacarbazine. Approved, Investigational Daclizumab Tacrolimus may increase the immunosuppressive activities of Daclizumab. Investigational, Withdrawn Dactinomycin Tacrolimus may increase the immunosuppressive activities of Dactinomycin. Approved, Investigational Danazol The serum concentration of Tacrolimus can be increased when it is combined with Danazol. 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 Darexaban. 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 Tacrolimus may increase the immunosuppressive activities of Dasatinib. Approved, Investigational Daunorubicin Tacrolimus may increase the immunosuppressive activities of Daunorubicin. Approved Deferasirox The serum concentration of Tacrolimus can be decreased when it is combined with Deferasirox. Approved, Investigational Deflazacort Tacrolimus may increase the immunosuppressive activities of Deflazacort. Approved, Investigational Delanzomib The metabolism of Tacrolimus can be decreased when combined with Delanzomib. Investigational Delapril The metabolism of Tacrolimus can be decreased when combined with Delapril. Experimental 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 Tacrolimus may increase the immunosuppressive activities of Deoxyspergualin. Investigational Dexamethasone Tacrolimus may increase the immunosuppressive activities of Dexamethasone. Approved, Investigational, Vet Approved Dexlansoprazole The serum concentration of Tacrolimus can be increased when it is combined with Dexlansoprazole. Approved, Investigational Dexrabeprazole The serum concentration of Tacrolimus can be increased when it is combined with Dexrabeprazole. Experimental Dichlorophene The metabolism of Tacrolimus can be decreased when combined with Dichlorophene. Vet Approved Diclofenac Diclofenac may increase the nephrotoxic activities of Tacrolimus. Approved, Vet Approved Difenpiramide Difenpiramide may increase the nephrotoxic activities of Tacrolimus. Experimental Diflunisal Diflunisal may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Dihydroergocornine The risk or severity of adverse effects can be increased when Dihydroergocornine is combined with Tacrolimus. Approved Dihydroergocristine The risk or severity of adverse effects can be increased when Dihydroergocristine is combined with Tacrolimus. Approved, Experimental Dihydroergocryptine The risk or severity of adverse effects can be increased when Dihydroergocryptine is combined with Tacrolimus. Experimental Dihydroergotamine The risk or severity of adverse effects can be increased when Dihydroergotamine is combined with Tacrolimus. Approved, Investigational Diltiazem The metabolism of Tacrolimus can be decreased when combined with Diltiazem. Approved, Investigational Dimethyl fumarate Tacrolimus may increase the immunosuppressive activities of Dimethyl fumarate. Approved, Investigational Dinutuximab Tacrolimus may increase the immunosuppressive activities of Dinutuximab. Approved, Investigational Docetaxel Tacrolimus may increase the immunosuppressive activities of Docetaxel. Approved, Investigational Doxifluridine Tacrolimus may increase the immunosuppressive activities of Doxifluridine. Investigational Doxorubicin Tacrolimus may increase the immunosuppressive activities of Doxorubicin. Approved, Investigational Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Tacrolimus. Approved, Investigational Doxycycline The metabolism of Tacrolimus can be decreased when combined with Doxycycline. Approved, Investigational, Vet Approved Dronedarone Tacrolimus may increase the QTc-prolonging activities of Dronedarone. Approved Droxicam Droxicam may increase the nephrotoxic activities of Tacrolimus. Withdrawn Dulaglutide The therapeutic efficacy of Dulaglutide can be decreased when used in combination with Tacrolimus. Approved, Investigational Duvelisib Duvelisib may increase the nephrotoxic activities of Tacrolimus. Investigational E-6201 E-6201 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 Tacrolimus may increase the immunosuppressive activities of Eculizumab. Approved, Investigational Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Tacrolimus. Approved Efalizumab Tacrolimus may increase the immunosuppressive activities of 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, Investigational Elafin The metabolism of Tacrolimus can be decreased when combined with Elafin. 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 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 Epigallocatechin Gallate The metabolism of Tacrolimus can be decreased when combined with Epigallocatechin Gallate. Investigational Epirizole Epirizole may increase the nephrotoxic activities of Tacrolimus. Approved Epirubicin Tacrolimus may increase the immunosuppressive activities of Epirubicin. Approved Eplerenone Eplerenone may increase the hyperkalemic activities of Tacrolimus. Approved Ergonovine The risk or severity of adverse effects can be increased when Ergonovine is combined with Tacrolimus. Approved Ergotamine The risk or severity of adverse effects can be increased when Ergotamine is combined with Tacrolimus. Approved 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, Investigational, Vet Approved Escitalopram The metabolism of Tacrolimus can be decreased when combined with Escitalopram. Approved, Investigational Esomeprazole The serum concentration of Tacrolimus can be increased when it is combined with Esomeprazole. Approved, Investigational Estramustine Tacrolimus may increase the immunosuppressive activities of Estramustine. Approved, Investigational Etanercept Tacrolimus may increase the immunosuppressive activities of Etanercept. 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 Ethenzamide Ethenzamide may increase the nephrotoxic activities of Tacrolimus. Experimental Etodolac Etodolac may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational, Vet Approved Etofenamate Etofenamate may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Etoposide Tacrolimus may increase the immunosuppressive activities of Etoposide. Approved Etoricoxib Etoricoxib may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Evening primrose oil Evening primrose oil may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Everolimus Tacrolimus may increase the immunosuppressive activities of Everolimus. 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 Faldaprevir The metabolism of Tacrolimus can be decreased when combined with Faldaprevir. Investigational Felbinac Felbinac may increase the nephrotoxic activities of Tacrolimus. Experimental 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. Approved, Illicit, Investigational, Withdrawn Fenofibrate Tacrolimus may increase the nephrotoxic activities of Fenofibrate. Approved Fenoprofen Fenoprofen may increase the nephrotoxic activities of Tacrolimus. Approved Fentiazac Fentiazac may increase the nephrotoxic activities of Tacrolimus. Experimental Fenticonazole The metabolism of Tacrolimus can be decreased when combined with Fenticonazole. Experimental Feprazone Feprazone may increase the nephrotoxic activities of Tacrolimus. Experimental Ferulic acid Ferulic acid may increase the nephrotoxic activities of Tacrolimus. Experimental Fingolimod Tacrolimus may increase the immunosuppressive activities of Fingolimod. Approved, Investigational Floctafenine Floctafenine may increase the nephrotoxic activities of Tacrolimus. Approved, Withdrawn Floxuridine Tacrolimus may increase the immunosuppressive activities of Floxuridine. Approved Fluconazole The serum concentration of Tacrolimus can be increased when it is combined with Fluconazole. Approved, Investigational Flucytosine The metabolism of Tacrolimus can be decreased when combined with Flucytosine. Approved, Investigational Fludarabine Tacrolimus may increase the immunosuppressive activities of Fludarabine. Approved Fludrocortisone Tacrolimus may increase the immunosuppressive activities of Fludrocortisone. Approved, Investigational Flunixin Flunixin may increase the nephrotoxic activities of Tacrolimus. Vet Approved Flunoxaprofen Flunoxaprofen may increase the nephrotoxic activities of Tacrolimus. Experimental Fluorouracil Tacrolimus may increase the immunosuppressive activities of Fluorouracil. Approved Fluoxetine The metabolism of Tacrolimus can be decreased when combined with Fluoxetine. Approved, Vet Approved Flurbiprofen Flurbiprofen may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Flutrimazole The metabolism of Tacrolimus can be decreased when combined with Flutrimazole. Experimental Fluvastatin The serum concentration of Fluvastatin can be increased 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 serum concentration of Tacrolimus can be decreased when it is combined with Fosphenytoin. Approved, Investigational Fusidic Acid The serum concentration of Tacrolimus can be increased when it is combined with Fusidic Acid. Approved, Investigational 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 Tacrolimus may increase the immunosuppressive activities of Gallium nitrate. Approved, Investigational Geldanamycin The metabolism of Tacrolimus can be decreased when combined with Geldanamycin. Experimental, Investigational Gemcitabine Tacrolimus may increase the immunosuppressive activities of Gemcitabine. Approved Gemtuzumab ozogamicin Tacrolimus may increase the immunosuppressive activities of Gemtuzumab ozogamicin. Approved, Investigational GI-5005 The risk or severity of adverse effects can be increased when Tacrolimus is combined with GI-5005. Investigational Glatiramer Acetate Tacrolimus may increase the immunosuppressive activities of Glatiramer Acetate. Approved, Investigational Glibornuride The therapeutic efficacy of Glibornuride can be decreased when used in combination with Tacrolimus. Investigational, Withdrawn Gliclazide The therapeutic efficacy of Gliclazide can be decreased when used in combination with Tacrolimus. Approved Glimepiride Tacrolimus may increase the immunosuppressive activities of Glimepiride. Approved Glipizide The therapeutic efficacy of Glipizide can be decreased when used in combination with Tacrolimus. Approved, Investigational Gliquidone The therapeutic efficacy of Gliquidone can be decreased when used in combination with Tacrolimus. Approved, Investigational Glyburide The therapeutic efficacy of Glyburide can be decreased when used in combination with Tacrolimus. 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 Tacrolimus may increase the immunosuppressive activities of Golimumab. Approved Griseofulvin The metabolism of Tacrolimus can be decreased when combined with Griseofulvin. Approved, Investigational, Vet Approved GS 0573 Tacrolimus may increase the immunosuppressive activities of GS 0573. Investigational Guacetisal Guacetisal may increase the nephrotoxic activities of Tacrolimus. Experimental Gusperimus Tacrolimus may increase the immunosuppressive activities of Gusperimus. Investigational Hachimycin The metabolism of Tacrolimus can be decreased when combined with Hachimycin. Experimental Haloprogin The metabolism of Tacrolimus can be decreased when combined with Haloprogin. Approved, Withdrawn Hepatitis A Vaccine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Hepatitis A Vaccine. Approved Hepatitis B Vaccine (Recombinant) The risk or severity of adverse effects can be increased when Tacrolimus is combined with Hepatitis B Vaccine (Recombinant). Approved, Withdrawn Hexetidine The metabolism of Tacrolimus can be decreased when combined with Hexetidine. Approved, Investigational Higenamine Higenamine may increase the nephrotoxic activities of Tacrolimus. Investigational Human C1-esterase inhibitor Tacrolimus may increase the immunosuppressive activities of Human C1-esterase inhibitor. Approved Human rabies virus immune globulin The risk or severity of adverse effects can be increased when Tacrolimus is combined with Human rabies virus immune globulin. Approved Hydrocortisone Tacrolimus may increase the immunosuppressive activities of Hydrocortisone. Approved, Vet Approved Hydroxyurea Tacrolimus may increase the immunosuppressive activities of Hydroxyurea. Approved Hypericin Tacrolimus may increase the immunosuppressive activities of Hypericin. Investigational Ibritumomab tiuxetan Tacrolimus may increase the immunosuppressive activities of Ibritumomab tiuxetan. Approved, Investigational Ibrutinib The serum concentration of Ibrutinib can be increased when it is combined with Tacrolimus. Approved Ibuprofen Ibuprofen may increase the nephrotoxic activities of Tacrolimus. Approved Ibuproxam Ibuproxam may increase the nephrotoxic activities of Tacrolimus. Withdrawn Icatibant Tacrolimus may increase the immunosuppressive activities of Icatibant. Approved, Investigational Idarubicin Tacrolimus may increase the immunosuppressive activities of Idarubicin. Approved Idelalisib The serum concentration of Tacrolimus can be increased when it is combined with Idelalisib. Approved Idraparinux The metabolism of Tacrolimus can be decreased when combined with Idraparinux. Investigational Ifosfamide Tacrolimus may increase the immunosuppressive activities of Ifosfamide. Approved Imatinib Tacrolimus may increase the immunosuppressive activities of Imatinib. Approved Imidapril The metabolism of Tacrolimus can be decreased when combined with Imidapril. Investigational Imidazole salicylate Imidazole salicylate may increase the nephrotoxic activities of Tacrolimus. Experimental Imiquimod Tacrolimus may increase the immunosuppressive activities of Imiquimod. Approved, Investigational 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 Indobufen Indobufen may increase the nephrotoxic activities of Tacrolimus. Investigational Indomethacin Indomethacin may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Indoprofen Indoprofen may increase the nephrotoxic activities of Tacrolimus. Withdrawn Infliximab Tacrolimus may increase the immunosuppressive activities of 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 Human The therapeutic efficacy of Insulin Human can be decreased when used in combination with Tacrolimus. Approved, Investigational 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 Tacrolimus may increase the immunosuppressive activities of Irinotecan. Approved, Investigational Isavuconazole The serum concentration of Tacrolimus can be increased when it is combined with Isavuconazole. 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, Investigational, Withdrawn Isoxicam Isoxicam may increase the nephrotoxic activities of Tacrolimus. Withdrawn Isradipine The serum concentration of Tacrolimus can be increased when it is combined with Isradipine. 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 Ixazomib The metabolism of Tacrolimus can be decreased when combined with Ixazomib. Approved, Investigational Japanese encephalitis virus strain sa 14-14-2 antigen (formaldehyde inactivated) The risk or severity of adverse effects can be increased when Tacrolimus is combined with Japanese encephalitis virus strain sa 14-14-2 antigen (formaldehyde inactivated). Approved Josamycin The serum concentration of Tacrolimus can be increased when it is combined with Josamycin. Approved, Investigational Kebuzone Kebuzone may increase the nephrotoxic activities of Tacrolimus. Experimental 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 Tacrolimus may increase the immunosuppressive activities of L-Phenylalanine. Approved, Investigational, Nutraceutical Lansoprazole The serum concentration of Tacrolimus can be increased when it is combined with Lansoprazole. Approved, Investigational Ledipasvir The serum concentration of Ledipasvir can be decreased when it is combined with Tacrolimus. Approved Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Tacrolimus. Approved Leflunomide Tacrolimus may increase the immunosuppressive activities of Leflunomide. Approved, Investigational Lenalidomide Tacrolimus may increase the immunosuppressive activities of Lenalidomide. Approved Lepirudin The metabolism of Tacrolimus can be decreased when combined with Lepirudin. Approved Letaxaban The metabolism of Tacrolimus can be decreased when combined with Letaxaban. 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, Investigational Linagliptin The serum concentration of Linagliptin can be decreased when it is combined with Tacrolimus. 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 Lisofylline Tacrolimus may increase the immunosuppressive activities of Lisofylline. Investigational Lisuride The risk or severity of adverse effects can be increased when Lisuride is combined with Tacrolimus. Approved, Investigational Lomustine Tacrolimus may increase the immunosuppressive activities of Lomustine. Approved, Investigational Lonazolac Lonazolac may increase the nephrotoxic activities of Tacrolimus. Experimental Lopinavir The metabolism of Tacrolimus can be decreased when combined with Lopinavir. Approved Lornoxicam Lornoxicam may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Lorpiprazole The serum concentration of Tacrolimus can be increased when it is combined with Lorpiprazole. Approved Lovastatin The serum concentration of Lovastatin can be increased when it is combined with Tacrolimus. Approved, Investigational Loxoprofen Loxoprofen may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational 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 Lysergic Acid Diethylamide The risk or severity of adverse effects can be increased when Lysergic Acid Diethylamide is combined with Tacrolimus. Illicit, Investigational, Withdrawn Magnesium salicylate Magnesium salicylate may increase the nephrotoxic activities of Tacrolimus. Approved Masoprocol Masoprocol may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Mechlorethamine Tacrolimus may increase the immunosuppressive activities of Mechlorethamine. Approved, Investigational 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 Melagatran The metabolism of Tacrolimus can be decreased when combined with Melagatran. Experimental Meloxicam Meloxicam may increase the nephrotoxic activities of Tacrolimus. Approved, Vet Approved Melphalan Tacrolimus may increase the immunosuppressive activities of Melphalan. Approved Mepartricin The metabolism of Tacrolimus can be decreased when combined with Mepartricin. Experimental Mepolizumab Tacrolimus may increase the immunosuppressive activities of Mepolizumab. Approved, Investigational Mercaptopurine Tacrolimus may increase the immunosuppressive activities of Mercaptopurine. Approved Mesalazine Mesalazine may increase the nephrotoxic activities of Tacrolimus. Approved Metamizole The risk or severity of myelosuppression can be increased when Metamizole is combined with Tacrolimus. Approved, Investigational, Withdrawn Metergoline The risk or severity of adverse effects can be increased when Metergoline is combined with Tacrolimus. Experimental Metformin The therapeutic efficacy of Metformin can be decreased when used in combination with Tacrolimus. Approved Methotrexate Tacrolimus may increase the immunosuppressive activities of Methotrexate. Approved Methylergometrine The risk or severity of adverse effects can be increased when Methylergometrine is combined with Tacrolimus. Approved Methylprednisolone Tacrolimus may increase the immunosuppressive activities of Methylprednisolone. Approved, Vet Approved Methysergide The risk or severity of adverse effects can be increased when Methysergide is combined with Tacrolimus. Approved Mevastatin The metabolism of Tacrolimus can be decreased when combined with Mevastatin. Experimental 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 Mifamurtide The therapeutic efficacy of Mifamurtide can be decreased when used in combination with Tacrolimus. Approved, Experimental Mifepristone Mifepristone may increase the QTc-prolonging activities of Tacrolimus. 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, Investigational Miltefosine The metabolism of Tacrolimus can be decreased when combined with Miltefosine. Approved, Investigational Mitiglinide The therapeutic efficacy of Mitiglinide can be decreased when used in combination with Tacrolimus. Approved, Investigational Mitomycin Tacrolimus may increase the immunosuppressive activities of Mitomycin. Approved Mitotane The serum concentration of Tacrolimus can be decreased when it is combined with Mitotane. Approved Mitoxantrone Tacrolimus may increase the immunosuppressive activities of Mitoxantrone. Approved, Investigational Mizoribine Tacrolimus may increase the immunosuppressive activities of Mizoribine. Investigational Moexipril The metabolism of Tacrolimus can be decreased when combined with Moexipril. Approved Mofebutazone Mofebutazone may increase the nephrotoxic activities of Tacrolimus. Experimental Monensin The metabolism of Tacrolimus can be decreased when combined with Monensin. Vet Approved Muromonab Tacrolimus may increase the immunosuppressive activities of Muromonab. Approved, Investigational Mycophenolate mofetil Tacrolimus may increase the immunosuppressive activities of Mycophenolate mofetil. Approved, Investigational Mycophenolic acid Tacrolimus may increase the immunosuppressive activities of Mycophenolic acid. 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 Nafamostat Tacrolimus may increase the immunosuppressive activities of Nafamostat. Approved, Investigational Naftifine The metabolism of Tacrolimus can be decreased when combined with Naftifine. Approved Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Tacrolimus. Approved Naproxen Naproxen may increase the nephrotoxic activities of Tacrolimus. Approved, Vet Approved 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 Tacrolimus may increase the immunosuppressive activities of Nelarabine. Approved, Investigational Nelfinavir The metabolism of Tacrolimus can be decreased when combined with Nelfinavir. Approved Nepafenac Nepafenac may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Netupitant The serum concentration of Tacrolimus can be increased when it is combined with Netupitant. Approved, Investigational Nevirapine The metabolism of Tacrolimus can be increased when combined with Nevirapine. Approved Nicardipine The serum concentration of Tacrolimus can be increased when it is combined with Nicardipine. Approved, Investigational Nicergoline The risk or severity of adverse effects can be increased when Nicergoline is combined with Tacrolimus. Approved, Investigational Nifedipine The serum concentration of Tacrolimus can be increased when it is combined with Nifedipine. Approved Nifenazone Nifenazone may increase the nephrotoxic activities of Tacrolimus. Experimental Niflumic Acid Niflumic Acid may increase the nephrotoxic activities of Tacrolimus. Approved Nifuratel The metabolism of Tacrolimus can be decreased when combined with Nifuratel. Experimental Nikkomycin Z The metabolism of Tacrolimus can be decreased when combined with Nikkomycin Z. Investigational Nilotinib Tacrolimus may increase the immunosuppressive activities of Nilotinib. Approved, Investigational Nimesulide Nimesulide may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational, Withdrawn Nimodipine The serum concentration of Tacrolimus can be increased when it is combined with Nimodipine. Approved, Investigational 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 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 Nystatin The metabolism of Tacrolimus can be decreased when combined with Nystatin. Approved, Vet Approved Obinutuzumab Tacrolimus may increase the immunosuppressive activities of Obinutuzumab. Approved, Investigational Ocrelizumab Ocrelizumab may increase the immunosuppressive activities of Tacrolimus. Approved, Investigational Olanzapine The metabolism of Tacrolimus can be decreased when combined with Olanzapine. 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, Investigational Omeprazole The serum concentration of Tacrolimus can be increased when it is combined with Omeprazole. Approved, Investigational, Vet Approved Omoconazole The metabolism of Tacrolimus can be decreased when combined with Omoconazole. Experimental 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 Tacrolimus may increase the immunosuppressive activities of 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. Approved, Withdrawn Paclitaxel Tacrolimus may increase the immunosuppressive activities of Paclitaxel. Approved, Vet Approved Pafuramidine The metabolism of Tacrolimus can be decreased when combined with Pafuramidine. Investigational Palbociclib Tacrolimus may increase the immunosuppressive activities of Palbociclib. Approved, Investigational Panobinostat Tacrolimus may increase the immunosuppressive activities of Panobinostat. Approved, Investigational Pantoprazole The serum concentration of Tacrolimus can be increased when it is combined with Pantoprazole. Approved Paquinimod Tacrolimus may increase the immunosuppressive activities of Paquinimod. Investigational 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, Investigational Paroxetine The metabolism of Tacrolimus can be decreased when combined with Paroxetine. Approved, Investigational Parthenolide Parthenolide may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Tacrolimus. Approved Pegaspargase Tacrolimus may increase the immunosuppressive activities of Pegaspargase. Approved, Investigational Pemetrexed Tacrolimus may increase the immunosuppressive activities of Pemetrexed. Approved, Investigational Pentamidine The metabolism of Tacrolimus can be decreased when combined with Pentamidine. Approved, Investigational Pentobarbital The metabolism of Tacrolimus can be increased when combined with Pentobarbital. Approved, Investigational, Vet Approved Pentostatin Tacrolimus may increase the immunosuppressive activities of Pentostatin. Approved, Investigational Pergolide The risk or severity of adverse effects can be increased when Pergolide is combined with Tacrolimus. Approved, Investigational, Vet Approved, Withdrawn Perindopril The metabolism of Tacrolimus can be decreased when combined with Perindopril. Approved Phenformin The therapeutic efficacy of Phenformin can be decreased when used in combination with Tacrolimus. Approved, Investigational, Withdrawn Phenobarbital The metabolism of Tacrolimus can be increased when combined with Phenobarbital. Approved, Investigational Phenylbutazone Phenylbutazone may increase the nephrotoxic activities of Tacrolimus. 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 Pioglitazone The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Tacrolimus. Approved, Investigational Pirarubicin Tacrolimus may increase the immunosuppressive activities of Pirarubicin. Investigational Pirfenidone Tacrolimus may increase the immunosuppressive activities of Pirfenidone. Approved, Investigational Piroxicam Piroxicam may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Pirprofen Pirprofen may increase the nephrotoxic activities of Tacrolimus. Experimental Pitavastatin The serum concentration of Pitavastatin can be increased when it is combined with Tacrolimus. Approved Pitolisant The serum concentration of Tacrolimus can be decreased when it is combined with Pitolisant. Approved, Investigational Pomalidomide Tacrolimus may increase the immunosuppressive activities of Pomalidomide. Approved Posaconazole The serum concentration of Tacrolimus can be increased when it is combined with Posaconazole. Approved, Investigational, Vet Approved Pralatrexate Tacrolimus may increase the immunosuppressive activities of Pralatrexate. Approved, Investigational Pramlintide The therapeutic efficacy of Pramlintide can be decreased when used in combination with Tacrolimus. Approved, Investigational Pranoprofen Pranoprofen may increase the nephrotoxic activities of Tacrolimus. Experimental, Investigational Pravastatin The serum concentration of Pravastatin can be increased when it is combined with Tacrolimus. Approved Prednisolone Tacrolimus may increase the immunosuppressive activities of Prednisolone. Approved, Vet Approved Prednisone Tacrolimus may increase the immunosuppressive activities of Prednisone. 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 Procarbazine Tacrolimus may increase the immunosuppressive activities of Procarbazine. Approved, Investigational Proglumetacin Proglumetacin may increase the nephrotoxic activities of Tacrolimus. Experimental Propacetamol Propacetamol may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Propyphenazone Propyphenazone may increase the nephrotoxic activities of Tacrolimus. Experimental Proquazone Proquazone may increase the nephrotoxic activities of Tacrolimus. Experimental 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 Pyrrolnitrin The metabolism of Tacrolimus can be decreased when combined with Pyrrolnitrin. Experimental Quinapril The metabolism of Tacrolimus can be decreased when combined with Quinapril. Approved, Investigational 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 virus inactivated antigen, A. Approved, Investigational Rabies virus inactivated antigen, A The therapeutic efficacy of Rabies virus inactivated antigen, A can be decreased when used in combination with Tacrolimus. Approved, Investigational 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 Ranolazine The serum concentration of Tacrolimus can be increased when it is combined with Ranolazine. Approved, Investigational 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 Resveratrol Resveratrol may increase the nephrotoxic activities of Tacrolimus. Approved, Experimental, Investigational Ribociclib The serum concentration of Tacrolimus can be increased when it is combined with Ribociclib. Approved, Investigational Rifabutin The serum concentration of Tacrolimus can be decreased when it is combined with Rifabutin. Approved, Investigational Rifampicin The serum concentration of Tacrolimus can be decreased when it is combined with Rifampicin. Approved Rifapentine The serum concentration of Tacrolimus can be decreased when it is combined with Rifapentine. Approved, Investigational Rifaximin The serum concentration of Tacrolimus can be decreased when it is combined with Rifaximin. Approved, Investigational Rilonacept Tacrolimus may increase the immunosuppressive activities of Rilonacept. Approved, Investigational Rilpivirine The serum concentration of Rilpivirine can be increased when it is combined with Tacrolimus. Approved Rindopepimut The risk or severity of adverse effects can be increased when Tacrolimus is combined with Rindopepimut. Investigational Ritonavir The serum concentration of Tacrolimus can be increased when it is combined with Ritonavir. Approved, Investigational Rituximab Tacrolimus may increase the immunosuppressive activities of Rituximab. Approved Rivaroxaban The metabolism of Tacrolimus can be decreased when combined with Rivaroxaban. Approved Rofecoxib Rofecoxib may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational, Withdrawn Roflumilast Roflumilast may increase the immunosuppressive activities of Tacrolimus. Approved Rosiglitazone The therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Tacrolimus. Approved, Investigational Rosuvastatin The serum concentration of Rosuvastatin can be increased when it is combined with Tacrolimus. Approved Rotavirus Vaccine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Rotavirus Vaccine. Approved Rubella virus vaccine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Rubella virus vaccine. Approved, Investigational Rucaparib The metabolism of Tacrolimus can be decreased when combined with Rucaparib. Approved, Investigational Ruxolitinib Tacrolimus may increase the immunosuppressive activities of Ruxolitinib. Approved S-3304 The metabolism of Tacrolimus can be decreased when combined with S-3304. Investigational 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, Investigational, Vet Approved Salmonella typhi ty2 vi polysaccharide antigen The risk or severity of adverse effects can be increased when Tacrolimus is combined with Salmonella typhi ty2 vi polysaccharide antigen. Approved Salmonella typhi ty21a live antigen The risk or severity of adverse effects can be increased when Tacrolimus is combined with Salmonella typhi ty21a live antigen. 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 Sarilumab The therapeutic efficacy of Tacrolimus can be decreased when used in combination with Sarilumab. Approved, Investigational Saxagliptin The metabolism of Tacrolimus can be decreased when combined with Saxagliptin. Approved Secukinumab Tacrolimus may increase the immunosuppressive activities of Secukinumab. Approved Semapimod Tacrolimus may increase the immunosuppressive activities of Semapimod. Investigational Seocalcitol Tacrolimus may increase the immunosuppressive activities of Seocalcitol. Experimental, Investigational Seratrodast Seratrodast may increase the nephrotoxic activities of Tacrolimus. Approved Serrapeptase Serrapeptase may increase the nephrotoxic activities of Tacrolimus. Investigational Sertaconazole The metabolism of Tacrolimus can be decreased when combined with Sertaconazole. Approved, Investigational Sertraline The metabolism of Tacrolimus can be decreased when 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 Tacrolimus may increase the immunosuppressive activities of Siltuximab. Approved, Investigational Simeprevir The metabolism of Tacrolimus can be decreased when combined with Simeprevir. Approved Simvastatin The serum concentration of Simvastatin can be increased when it is combined with Tacrolimus. 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, Investigational Sirolimus The risk or severity of adverse effects can be increased when Tacrolimus is combined with Sirolimus. Approved, Investigational Sitagliptin The metabolism of Tacrolimus can be decreased when combined with Sitagliptin. Approved, Investigational Sivelestat The metabolism of Tacrolimus can be decreased when combined with Sivelestat. 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 Tacrolimus may increase the immunosuppressive activities of Sorafenib. Approved, Investigational Sotagliflozin The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Tacrolimus. Investigational Spirapril The metabolism of Tacrolimus can be decreased when combined with Spirapril. Approved Spironolactone The risk or severity of hyperkalemia can be increased when Spironolactone is combined with Tacrolimus. 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. Approved, Investigational, Nutraceutical Stepronin Tacrolimus may increase the immunosuppressive activities of Stepronin. Approved Stiripentol The serum concentration of Tacrolimus can be increased when it is combined with Stiripentol. Approved Streptozocin Tacrolimus may increase the immunosuppressive activities of Streptozocin. Approved, Investigational Sulconazole The metabolism of Tacrolimus can be decreased when combined with Sulconazole. Approved Sulfasalazine Sulfasalazine may increase the nephrotoxic activities of Tacrolimus. 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, Investigational Sulodexide The therapeutic efficacy of Sulodexide can be decreased when used in combination with Tacrolimus. Approved, Investigational Sunitinib Tacrolimus may increase the immunosuppressive activities of Sunitinib. Approved, Investigational Suprofen Suprofen may increase the nephrotoxic activities of Tacrolimus. Approved, Withdrawn Suxibuzone Suxibuzone may increase the nephrotoxic activities of Tacrolimus. Experimental Tarenflurbil Tarenflurbil may increase the nephrotoxic activities of Tacrolimus. Investigational Tavaborole The metabolism of Tacrolimus can be decreased when combined with Tavaborole. Approved, Investigational Tecemotide The risk or severity of adverse effects can be increased when Tacrolimus is combined with Tecemotide. Investigational Telaprevir The serum concentration of Tacrolimus can be increased when it is combined with Telaprevir. Approved, Withdrawn Telithromycin The serum concentration of Tacrolimus can be increased when it is combined with Telithromycin. Approved Temocapril The metabolism of Tacrolimus can be decreased when combined with Temocapril. Experimental, Investigational Temozolomide Tacrolimus may increase the immunosuppressive activities of Temozolomide. Approved, Investigational Temsirolimus The risk or severity of adverse effects can be increased when Tacrolimus is combined with Temsirolimus. Approved Tenidap Tenidap may increase the nephrotoxic activities of Tacrolimus. Experimental Teniposide Tacrolimus may increase the immunosuppressive activities of Teniposide. Approved Tenoxicam Tenoxicam may increase the nephrotoxic activities of Tacrolimus. Approved Tepoxalin Tacrolimus may increase the immunosuppressive activities of Tepoxalin. Vet 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 Terguride The risk or severity of adverse effects can be increased when Terguride is combined with Tacrolimus. Experimental Teriflunomide Tacrolimus may increase the immunosuppressive activities of Teriflunomide. Approved TG4010 The risk or severity of adverse effects can be increased when Tacrolimus is combined with TG4010. Investigational Thalidomide Tacrolimus may increase the immunosuppressive activities of Thalidomide. Approved, Investigational, Withdrawn Thiorphan The metabolism of Tacrolimus can be decreased when combined with Thiorphan. Experimental Thiotepa Tacrolimus may increase the immunosuppressive activities of Thiotepa. Approved, Investigational 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 Ticlopidine The metabolism of Tacrolimus can be decreased when combined with Ticlopidine. 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 Tacrolimus may increase the immunosuppressive activities of Tioguanine. Approved Tipranavir The metabolism of Tacrolimus can be decreased when combined with Tipranavir. Approved, Investigational Tocilizumab Tacrolimus may increase the immunosuppressive activities of Tocilizumab. Approved Tofacitinib Tacrolimus may increase the immunosuppressive activities of Tofacitinib. Approved, Investigational Tolazamide The therapeutic efficacy of Tolazamide can be decreased when used in combination with Tacrolimus. Approved, Investigational Tolbutamide The therapeutic efficacy of Tolbutamide can be decreased when used in combination with Tacrolimus. Approved, Investigational Tolciclate The metabolism of Tacrolimus can be decreased when combined with Tolciclate. Experimental Tolfenamic Acid Tolfenamic Acid may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational Tolmetin Tolmetin may increase the nephrotoxic activities of Tacrolimus. Approved Tolnaftate The metabolism of Tacrolimus can be decreased when combined with Tolnaftate. Approved, Investigational, Vet Approved Tolvaptan The serum concentration of Tolvaptan can be increased when it is combined with Tacrolimus. Approved Topotecan The serum concentration of Topotecan can be increased when it is combined with Tacrolimus. Approved, Investigational Tositumomab Tacrolimus may increase the immunosuppressive activities of Tositumomab. Approved, Investigational Trabectedin Tacrolimus may increase the immunosuppressive activities of 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 Tacrolimus may increase the immunosuppressive activities of Trastuzumab emtansine. Approved, Investigational Trazodone The metabolism of Tacrolimus can be decreased when combined with Trazodone. Approved, Investigational Tretinoin Tacrolimus may increase the immunosuppressive activities of Tretinoin. Approved, Investigational, Nutraceutical Triamcinolone Tacrolimus may increase the immunosuppressive activities of Triamcinolone. Approved, Vet Approved Triamterene The risk or severity of hyperkalemia can be increased when Triamterene is combined with Tacrolimus. Approved Tribenoside Tribenoside may increase the nephrotoxic activities of Tacrolimus. Experimental Trimetrexate The metabolism of Tacrolimus can be decreased when combined with Trimetrexate. Approved, Investigational Triptolide Tacrolimus may increase the immunosuppressive activities of Triptolide. Investigational Trofosfamide Tacrolimus may increase the immunosuppressive activities of Trofosfamide. Investigational Troglitazone The therapeutic efficacy of Troglitazone can be decreased when used in combination with Tacrolimus. Investigational, 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, Investigational Ulinastatin The metabolism of Tacrolimus can be decreased when combined with Ulinastatin. Investigational Ustekinumab Tacrolimus may increase the immunosuppressive activities of Ustekinumab. Approved, Investigational Valdecoxib Valdecoxib may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational, Withdrawn Varicella Zoster Vaccine (Live/Attenuated) The risk or severity of adverse effects can be increased when Tacrolimus is combined with Varicella Zoster Vaccine (Live/Attenuated). Approved Vedolizumab Tacrolimus may increase the immunosuppressive activities of Vedolizumab. Approved Vemurafenib The serum concentration of Tacrolimus can be increased when it is combined with Vemurafenib. 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 Tacrolimus may increase the immunosuppressive activities of 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 Vinblastine Tacrolimus may increase the immunosuppressive activities of Vinblastine. Approved Vincristine The serum concentration of Vincristine can be decreased when it is combined with Tacrolimus. Approved, Investigational Vincristine Tacrolimus may increase the immunosuppressive activities of Vincristine. Approved, Investigational Vindesine Tacrolimus may increase the immunosuppressive activities of Vindesine. Approved, Investigational Vinorelbine Tacrolimus may increase the immunosuppressive activities of Vinorelbine. Approved, Investigational Voclosporin Tacrolimus may increase the immunosuppressive activities of Voclosporin. Investigational Voglibose The therapeutic efficacy of Voglibose can be decreased when used in combination with Tacrolimus. 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, Investigational Ximelagatran The metabolism of Tacrolimus can be decreased when combined with Ximelagatran. Approved, Investigational, Withdrawn Yellow Fever Vaccine The risk or severity of adverse effects can be increased when Tacrolimus is combined with Yellow Fever Vaccine. Approved, Investigational Z-Val-Ala-Asp fluoromethyl ketone The metabolism of Tacrolimus can be decreased when combined with Z-Val-Ala-Asp fluoromethyl ketone. Experimental Zaltoprofen Zaltoprofen may increase the nephrotoxic activities of Tacrolimus. Approved, Investigational 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 Ziprasidone The metabolism of Tacrolimus can be decreased when combined with Ziprasidone. Approved Zofenopril The metabolism of Tacrolimus can be decreased when combined with Zofenopril. Experimental 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
- Kino T, Hatanaka H, Hashimoto M, Nishiyama M, Goto T, Okuhara M, Kohsaka M, Aoki H, Imanaka H: FK-506, a novel immunosuppressant isolated from a Streptomyces. I. Fermentation, isolation, and physico-chemical and biological characteristics. J Antibiot (Tokyo). 1987 Sep;40(9):1249-55. [PubMed:2445721]
- 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
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- 445643
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- Wikipedia
- Tacrolimus
- ATC Codes
- D11AH01 — Tacrolimus
- D11AH — Agents for dermatitis, excluding corticosteroids
- D11A — OTHER DERMATOLOGICAL PREPARATIONS
- D11 — OTHER DERMATOLOGICAL PREPARATIONS
- D — DERMATOLOGICALS
- AHFS Codes
- 92:44.00 — Immunosuppressive Agents
- 84:92.00 — Misc. Skin and Mucous Membrane Agents
- PDB Entries
- 1bkf / 1fkf / 1fkj / 1q6i / 1tco / 1yat / 2fke / 2vn1 / 3ihz / 3o5r … show 15 more
- 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
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- Kaiser Foundation Hospital
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- Neuman Distributors Inc.
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- 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 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 .3 mg/g Ointment Topical 0.03 % Ointment Topical 0.1 % Ointment Topical 1 mg/g Capsule Oral .5 mg/1 Capsule Oral 1 mg/1 Capsule Oral 5 mg/1 Capsule, gelatin coated Oral .5 mg/1 Capsule, gelatin coated Oral 5 mg/1 - 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 US9757362 No 2004-08-30 2024-08-30 US US9763920 No 2004-08-30 2024-08-30 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 MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) 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 April 17, 2018 01:01