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Identification
NameTacrolimus
Accession NumberDB00864  (APRD00276, EXPT01437)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionTacrolimus (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
Thumb
Synonyms
Anhydrous tacrolimus
Tacrolimus anhydrous
Tacrolimus, anhydrous
External Identifiers
  • FK-506
  • FK5
  • K506
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ach-tacrolimusCapsule1 mgOralAccord Healthcare IncNot applicableNot applicableCanada
Ach-tacrolimusCapsule0.5 mgOralAccord Healthcare IncNot applicableNot applicableCanada
Ach-tacrolimusCapsule5 mgOralAccord Healthcare IncNot applicableNot applicableCanada
AdvagrafCapsule, extended release1 mgOralAstellas Pharma Canada Inc2008-04-09Not applicableCanada
AdvagrafCapsule, extended release1 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafCapsule, extended release1 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafCapsule, extended release3 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafCapsule, extended release5 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafCapsule, extended release3 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafCapsule, extended release0.5 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafCapsule, extended release0.5 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafCapsule, extended release5 mgOralAstellas Pharma Canada Inc2008-04-09Not applicableCanada
AdvagrafCapsule, extended release1 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafCapsule, extended release1 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafCapsule, extended release3 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafCapsule, extended release0.5 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafCapsule, extended release5 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafCapsule, extended release0.5 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafCapsule, extended release1 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafCapsule, extended release3 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafCapsule, extended release3 mgOralAstellas Pharma Canada Inc2010-04-05Not applicableCanada
AdvagrafCapsule, extended release1 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafCapsule, extended release0.5 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafCapsule, extended release5 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafCapsule, extended release5 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafCapsule, extended release0.5 mgOralAstellas Pharma Canada Inc2008-04-09Not applicableCanada
AdvagrafCapsule, extended release1 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafCapsule, extended release1 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafCapsule, extended release5 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafCapsule, extended release3 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafCapsule, extended release0.5 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafCapsule, extended release3 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafCapsule, extended release5 mgOralAstellas Pharma Europe B.V.2007-04-23Not applicableEu
Astagraf XLCapsule, coated, extended release1 mg/1OralAstellas Pharma US, Inc.2013-07-19Not applicableUs
Astagraf XLCapsule, coated, extended release5 mg/1OralAstellas Pharma US, Inc.2013-07-19Not applicableUs
Astagraf XLCapsule, coated, extended release.5 mg/1OralAstellas Pharma US, Inc.2013-07-19Not applicableUs
EnvarsusTablet, extended release4 mgOralChiesi Farmaceutici S.P.A.2014-07-18Not applicableEu
EnvarsusTablet, extended release0.75 mgOralChiesi Farmaceutici S.P.A.2014-07-18Not applicableEu
EnvarsusTablet, extended release1 mgOralChiesi Farmaceutici S.P.A.2014-07-18Not applicableEu
EnvarsusTablet, extended release4 mgOralChiesi Farmaceutici S.P.A.2014-07-18Not applicableEu
EnvarsusTablet, extended release0.75 mgOralChiesi Farmaceutici S.P.A.2014-07-18Not applicableEu
EnvarsusTablet, extended release1 mgOralChiesi Farmaceutici S.P.A.2014-07-18Not applicableEu
EnvarsusTablet, extended release0.75 mgOralChiesi Farmaceutici S.P.A.2014-07-18Not applicableEu
EnvarsusTablet, extended release4 mgOralChiesi Farmaceutici S.P.A.2014-07-18Not applicableEu
EnvarsusTablet, extended release1 mgOralChiesi Farmaceutici S.P.A.2014-07-18Not applicableEu
Envarsus XRTablet, extended release4 mg/1OralVeloxis Pharmaceuticals, Inc2015-09-01Not applicableUs
Envarsus XRTablet, extended release.75 mg/1OralVeloxis Pharmaceuticals, Inc2015-09-01Not applicableUs
Envarsus XRTablet, extended release1 mg/1OralVeloxis Pharmaceuticals, Inc2015-09-01Not applicableUs
ModigrafGranule0.2 mgOralAstellas Pharma Europe B.V.2009-05-15Not applicableEu
ModigrafGranule1 mgOralAstellas Pharma Europe B.V.2009-05-15Not applicableEu
PrografCapsule, gelatin coated.5 mg/1OralAstellas Pharma US, Inc.1998-08-24Not applicableUs
PrografSolution5 mgIntravenousAstellas Pharma Canada Inc1996-08-14Not applicableCanada
PrografCapsule, gelatin coated1 mg/1OralAstellas Pharma US, Inc.1994-04-08Not applicableUs
PrografCapsule0.5 mgOralAstellas Pharma Canada Inc2001-04-02Not applicableCanada
PrografCapsule, gelatin coated1 mg/1OralAphena Pharma Solutions Tennessee, Llc1994-04-08Not applicableUs
PrografCapsule5 mgOralAstellas Pharma Canada Inc1996-08-14Not applicableCanada
PrografCapsule, gelatin coated1 mg/1OralCardinal Health1994-04-08Not applicableUs
PrografInjection, solution5 mg/mLIntravenousAstellas Pharma US, Inc.1994-04-08Not applicableUs
PrografCapsule1 mgOralAstellas Pharma Canada Inc1996-08-14Not applicableCanada
PrografCapsule, gelatin coated5 mg/1OralAstellas Pharma US, Inc.1994-04-08Not applicableUs
PrografCapsule, gelatin coated1 mg/1OralRebel Distributors Corp1994-04-08Not applicableUs
ProtopicOintment.3 mg/gTopicalAstellas Pharma US Inc.2000-12-08Not applicableUs
ProtopicOintment0.03 %CutaneousLeo Pharma A/S2002-02-28Not applicableEu
ProtopicOintment0.03 %CutaneousLeo Pharma A/S2002-02-28Not applicableEu
ProtopicOintment1 mg/gTopicalAstellas Pharma US Inc.2000-12-08Not applicableUs
ProtopicOintment0.1 %CutaneousLeo Pharma A/S2002-02-28Not applicableEu
ProtopicOintment1 mg/gTopicalPhysicians Total Care, Inc.2008-05-08Not applicableUs
ProtopicOintment0.03 %CutaneousLeo Pharma A/S2002-02-28Not applicableEu
ProtopicOintment0.1 %TopicalLeo Pharma Inc2001-09-06Not applicableCanada
ProtopicOintment.3 mg/gTopicalLEO Pharma Inc.2000-12-08Not applicableUs
ProtopicOintment0.1 %CutaneousLeo Pharma A/S2002-02-28Not applicableEu
ProtopicOintment0.03 %TopicalLeo Pharma Inc2001-09-06Not applicableCanada
ProtopicOintment1 mg/gTopicalLEO Pharma Inc.2000-12-08Not applicableUs
ProtopicOintment0.1 %CutaneousLeo Pharma A/S2002-02-28Not applicableEu
Ran-tacrolimusCapsule5 mgOralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada
Sandoz TacrolimusCapsule1 mgOralSandoz Canada Incorporated2013-11-25Not applicableCanada
Sandoz TacrolimusCapsule5 mgOralSandoz Canada Incorporated2013-11-25Not applicableCanada
Sandoz TacrolimusCapsule0.5 mgOralSandoz Canada Incorporated2014-06-11Not applicableCanada
TacrolimusOintment1 mg/gTopicalPerrigo New York Inc2014-11-20Not applicableUs
TacrolimusOintment.3 mg/gTopicalPerrigo New York Inc2014-11-20Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
HecoriaCapsule.5 mg/1OralNovartis Pharmaceuticals Corporation2011-12-20Not applicableUs
HecoriaCapsule1 mg/1OralNovartis Pharmaceuticals Corporation2011-12-20Not applicableUs
HecoriaCapsule5 mg/1OralNovartis Pharmaceuticals Corporation2011-12-20Not applicableUs
TacrolimusCapsule.5 mg/1OralSandoz Inc2009-08-10Not applicableUs
TacrolimusCapsule.5 mg/1OralDr. Reddy's Laboratories Limited2010-05-14Not applicableUs
TacrolimusCapsule.5 mg/1OralGolden State Medical Supply, Inc.2015-11-18Not applicableUs
TacrolimusCapsule5 mg/1OralAccord Healthcare Inc.2011-08-31Not applicableUs
TacrolimusCapsule, gelatin coated1 mg/1Oralbryant ranch prepack2012-10-30Not applicableUs
TacrolimusCapsule1 mg/1OralMylan Pharmaceuticals Inc.2010-09-17Not applicableUs
TacrolimusCapsule1 mg/1OralSandoz Inc2012-01-15Not applicableUs
TacrolimusCapsule1 mg/1OralCardinal Health2009-08-10Not applicableUs
TacrolimusCapsule, gelatin coated1 mg/1OralBion Pharma Inc.,2016-02-26Not applicableUs
TacrolimusOintment.3 mg/gTopicalE. Fougera & Co. a division of Fougera Pharmaceuticals Inc.2014-09-09Not applicableUs
TacrolimusCapsule5 mg/1OralMylan Institutional Inc.2010-11-01Not applicableUs
TacrolimusCapsule.5 mg/1OralAmerican Health Packaging2013-07-17Not applicableUs
TacrolimusCapsule.5 mg/1OralCardinal Health2011-06-15Not applicableUs
TacrolimusCapsule1 mg/1OralSandoz Inc2009-08-10Not applicableUs
TacrolimusCapsule1 mg/1OralDr. Reddy's Laboratories Limited2010-05-14Not applicableUs
TacrolimusCapsule1 mg/1OralGolden State Medical Supply, Inc.2015-11-18Not applicableUs
TacrolimusCapsule.5 mg/1OralIngenus Pharmaceuticals, LLC2012-09-28Not applicableUs
TacrolimusCapsule.5 mg/1OralStrides Arcolab Limited2014-08-13Not applicableUs
TacrolimusCapsule5 mg/1OralMylan Pharmaceuticals Inc.2010-09-17Not applicableUs
TacrolimusCapsule5 mg/1OralSandoz Inc2012-01-15Not applicableUs
TacrolimusCapsule, gelatin coated.5 mg/1OralKremers Urban Pharmaceuticals Inc.2015-07-30Not applicableUs
TacrolimusCapsule, gelatin coated5 mg/1OralBion Pharma Inc.,2016-02-26Not applicableUs
TacrolimusCapsule1 mg/1OralKAISER FOUNDATION HOSPITALS2010-12-10Not applicableUs
TacrolimusCapsule.5 mg/1OralMylan Institutional Inc.2010-11-15Not applicableUs
TacrolimusCapsule1 mg/1OralAmerican Health Packaging2013-07-17Not applicableUs
TacrolimusCapsule1 mg/1OralA S Medication Solutions2011-09-30Not applicableUs
TacrolimusCapsule5 mg/1OralSandoz Inc2009-08-10Not applicableUs
TacrolimusCapsule5 mg/1OralDr. Reddy's Laboratories Limited2010-05-14Not applicableUs
TacrolimusCapsule5 mg/1OralGolden State Medical Supply, Inc.2015-11-18Not applicableUs
TacrolimusCapsule1 mg/1OralStrides Arcolab Limited2014-08-13Not applicableUs
TacrolimusCapsule1 mg/1OralMajor Pharmaceuticals2015-01-05Not applicableUs
TacrolimusCapsule1 mg/1OralIngenus Pharmaceuticals, LLC2012-09-28Not applicableUs
TacrolimusCapsule.5 mg/1OralAccord Healthcare Inc.2011-08-31Not applicableUs
TacrolimusCapsule, gelatin coated1 mg/1OralKremers Urban Pharmaceuticals Inc.2015-07-30Not applicableUs
TacrolimusCapsule1 mg/1OralCardinal Health2009-08-10Not applicableUs
TacrolimusCapsule5 mg/1OralWatson Laboratories, Inc.2010-07-06Not applicableUs
TacrolimusCapsule1 mg/1OralMylan Institutional Inc.2010-11-01Not applicableUs
TacrolimusCapsule5 mg/1OralAmerican Health Packaging2013-07-17Not applicableUs
TacrolimusCapsule1 mg/1OralCardinal Health2013-07-17Not applicableUs
TacrolimusCapsule, gelatin coated.5 mg/1OralBion Pharma Inc.,2016-02-26Not applicableUs
TacrolimusCapsule.5 mg/1OralSandoz Inc2012-01-15Not applicableUs
TacrolimusCapsule5 mg/1OralIngenus Pharmaceuticals, LLC2012-09-28Not applicableUs
TacrolimusCapsule5 mg/1OralStrides Arcolab Limited2014-08-13Not applicableUs
TacrolimusCapsule1 mg/1OralCardinal Health2011-06-15Not applicableUs
TacrolimusOintment1 mg/gTopicalE. Fougera & Co. a division of Fougera Pharmaceuticals Inc.2014-09-09Not applicableUs
TacrolimusCapsule1 mg/1OralAccord Healthcare Inc.2011-08-31Not applicableUs
TacrolimusCapsule, gelatin coated5 mg/1OralKremers Urban Pharmaceuticals Inc.2015-07-30Not applicableUs
TacrolimusCapsule.5 mg/1OralMylan Pharmaceuticals Inc.2010-09-17Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Tacrolimus hydrate
109581-93-3
Thumb
  • InChI Key: NWJQLQGQZSIBAF-MSLXHMNKSA-N
  • Monoisotopic Mass: 821.492541363
  • Average Mass: 822.0334
DBSALT000167
Categories
UNIIY5L2157C4J
CAS number104987-11-3
WeightAverage: 804.0182
Monoisotopic: 803.481976677
Chemical FormulaC44H69NO12
InChI KeyQJJXYPPXXYFBGM-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[C@@H]1C[C@@H](CC[[email protected]]1O)\C=C(/C)[[email protected]]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@]2(O)O[C@@H]([[email protected]](C[[email protected]]2C)OC)[[email protected]](C[C@@H](C)C\C(C)=C\[C@@H](CC=C)C(=O)C[[email protected]](O)[[email protected]]1C)OC
Pharmacology
IndicationFor 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
PharmacodynamicsTacrolimus 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 actionThe 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.
TargetKindPharmacological actionActionsOrganismUniProt ID
Peptidyl-prolyl cis-trans isomerase FKBP1AProteinyes
inhibitor
HumanP62942 details
Related Articles
AbsorptionAbsorption 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.

SubstrateEnzymesProduct
Tacrolimus
31-O-DemethyltacrolimusDetails
Tacrolimus
Not Available
13-demethyl tacrolimusDetails
Route of eliminationIn 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 lifeThe 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]
ToxicitySide 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
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug Reactions
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeAdverse ReactionReference(s)
Multidrug resistance protein 1
Gene symbol: ABCB1
UniProt: P08183
rs2032582 Not AvailableT Allele (G2677T)Increased risk of neurotoxicity12352921
Interactions
Drug Interactions
DrugInteractionDrug group
1,10-PhenanthrolineThe metabolism of Tacrolimus can be decreased when combined with 1,10-Phenanthroline.Experimental
2-HYDROXY-1,4-NAPHTHOQUINONEThe metabolism of Tacrolimus can be decreased when combined with 2-HYDROXY-1,4-NAPHTHOQUINONE.Experimental
2-mercaptobenzothiazoleThe metabolism of Tacrolimus can be decreased when combined with 2-mercaptobenzothiazole.Vet Approved
2-MethoxyethanolThe risk or severity of adverse effects can be increased when Tacrolimus is combined with 2-Methoxyethanol.Experimental
3,4-DichloroisocoumarinThe metabolism of Tacrolimus can be decreased when combined with 3,4-Dichloroisocoumarin.Experimental
4-(2-AMINOETHYL)BENZENESULFONYL FLUORIDEThe metabolism of Tacrolimus can be decreased when combined with 4-(2-AMINOETHYL)BENZENESULFONYL FLUORIDE.Experimental
9-(2-phosphonylmethoxyethyl)-2,6-diaminopurineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine.Investigational
AbataceptThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Abatacept.Approved
abetimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with abetimus.Investigational
ABR-215757The risk or severity of adverse effects can be increased when Tacrolimus is combined with ABR-215757.Investigational
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Tacrolimus.Approved, Investigational
AcebutololThe serum concentration of Acebutolol can be decreased when it is combined with Tacrolimus.Approved
AceclofenacAceclofenac may increase the nephrotoxic activities of Tacrolimus.Approved
AcetaminophenThe serum concentration of Acetaminophen can be decreased when it is combined with Tacrolimus.Approved
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Tacrolimus.Withdrawn
AcetovanilloneAcetovanillone may increase the nephrotoxic activities of Tacrolimus.Investigational
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be decreased when it is combined with Tacrolimus.Approved, Vet Approved
Acetylsalicylic acidAcetylsalicylic acid may increase the nephrotoxic activities of Tacrolimus.Approved, Vet Approved
ActeosideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Acteoside.Investigational
AdalimumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Adalimumab.Approved
AdapaleneAdapalene may increase the nephrotoxic activities of Tacrolimus.Approved
Adefovir DipivoxilThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Adefovir Dipivoxil.Approved, Investigational
AfatinibThe serum concentration of Afatinib can be decreased when it is combined with Tacrolimus.Approved
AfelimomabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Afelimomab.Investigational
AicarThe therapeutic efficacy of Aicar can be decreased when used in combination with Tacrolimus.Experimental
AlbendazoleThe serum concentration of Tacrolimus can be increased when it is combined with Albendazole.Approved, Vet Approved
AldosteroneThe serum concentration of Tacrolimus can be decreased when it is combined with Aldosterone.Experimental
AlectinibThe serum concentration of Tacrolimus can be increased when it is combined with Alectinib.Approved
AlefaceptThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Alefacept.Approved, Withdrawn
AlemtuzumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Alemtuzumab.Approved, Investigational
AlfentanilThe serum concentration of Tacrolimus can be increased when it is combined with Alfentanil.Approved, Illicit
alicaforsenThe risk or severity of adverse effects can be increased when Tacrolimus is combined with alicaforsen.Investigational
AlitretinoinThe serum concentration of Alitretinoin can be decreased when it is combined with Tacrolimus.Approved, Investigational
AlogliptinThe metabolism of Tacrolimus can be decreased when combined with Alogliptin.Approved
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Tacrolimus.Approved
Alpha-1-proteinase inhibitorThe metabolism of Tacrolimus can be decreased when combined with Alpha-1-proteinase inhibitor.Approved
ALT-110The risk or severity of adverse effects can be increased when Tacrolimus is combined with ALT-110.Investigational
AltretamineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Altretamine.Approved
AmantadineThe serum concentration of Tacrolimus can be increased when it is combined with Amantadine.Approved
AmbrisentanThe serum concentration of Ambrisentan can be decreased when it is combined with Tacrolimus.Approved, Investigational
Amg 827The risk or severity of adverse effects can be increased when Tacrolimus is combined with Amg 827.Investigational
AmilorideAmiloride may increase the hyperkalemic activities of Tacrolimus.Approved
Aminohippuric acidThe serum concentration of Tacrolimus can be increased when it is combined with Aminohippuric acid.Approved
AmiodaroneThe metabolism of Tacrolimus can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Amitriptyline can be decreased when it is combined with Tacrolimus.Approved
AmlodipineThe serum concentration of Tacrolimus can be increased when it is combined with Amlodipine.Approved
AmorolfineThe metabolism of Tacrolimus can be decreased when combined with Amorolfine.Approved
AmoxapineThe metabolism of Tacrolimus can be decreased when combined with Amoxapine.Approved
Amphotericin BThe metabolism of Tacrolimus can be decreased when combined with Amphotericin B.Approved, Investigational
AmprenavirThe metabolism of Tacrolimus can be decreased when combined with Amprenavir.Approved
AmprenavirThe serum concentration of Tacrolimus can be decreased when it is combined with Amprenavir.Approved
AmsacrineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Amsacrine.Approved
AmsacrineThe serum concentration of Tacrolimus can be increased when it is combined with Amsacrine.Approved
AN2690The metabolism of Tacrolimus can be decreased when combined with AN2690.Investigational
AnakinraThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Anakinra.Approved
AnidulafunginThe metabolism of Tacrolimus can be decreased when combined with Anidulafungin.Approved, Investigational
AnisodamineAnisodamine may increase the nephrotoxic activities of Tacrolimus.Investigational
Anti-thymocyte Globulin (Rabbit)The risk or severity of adverse effects can be increased when Tacrolimus is combined with Anti-thymocyte Globulin (Rabbit).Approved
AntipyrineAntipyrine may increase the nephrotoxic activities of Tacrolimus.Approved
Antithrombin III humanThe metabolism of Tacrolimus can be decreased when combined with Antithrombin III human.Approved
ApixabanThe metabolism of Tacrolimus can be decreased when combined with Apixaban.Approved
ApixabanThe serum concentration of Apixaban can be decreased when it is combined with Tacrolimus.Approved
ApremilastThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Apremilast.Approved, Investigational
ApremilastApremilast may increase the nephrotoxic activities of Tacrolimus.Approved, Investigational
AprepitantThe serum concentration of Tacrolimus can be increased when it is combined with Aprepitant.Approved, Investigational
AprotininThe metabolism of Tacrolimus can be decreased when combined with Aprotinin.Approved, Withdrawn
ArgatrobanThe metabolism of Tacrolimus can be decreased when combined with Argatroban.Approved, Investigational
Arsenic trioxideThe serum concentration of Arsenic trioxide can be decreased when it is combined with Tacrolimus.Approved, Investigational
ArtemetherThe metabolism of Tacrolimus can be decreased when combined with Artemether.Approved
AstemizoleThe serum concentration of Tacrolimus can be increased when it is combined with Astemizole.Approved, Withdrawn
AsunaprevirThe metabolism of Tacrolimus can be decreased when combined with Asunaprevir.Approved, Investigational
AtazanavirThe metabolism of Tacrolimus can be decreased when combined with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Atenolol can be decreased when it is combined with Tacrolimus.Approved
AtomoxetineThe metabolism of Tacrolimus can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe serum concentration of Tacrolimus can be increased when it is combined with Atorvastatin.Approved
AxitinibThe serum concentration of Axitinib can be decreased when it is combined with Tacrolimus.Approved, Investigational
AzacitidineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Azacitidine.Approved, Investigational
AzapropazoneAzapropazone may increase the nephrotoxic activities of Tacrolimus.Withdrawn
AzathioprineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Azathioprine.Approved
AzelastineThe serum concentration of Tacrolimus can be increased when it is combined with Azelastine.Approved
AzelastineAzelastine may increase the nephrotoxic activities of Tacrolimus.Approved
AzithromycinThe serum concentration of Tacrolimus can be increased when it is combined with Azithromycin.Approved
Bafilomycin A1The metabolism of Tacrolimus can be decreased when combined with Bafilomycin A1.Experimental
BalaglitazoneThe therapeutic efficacy of Balaglitazone can be decreased when used in combination with Tacrolimus.Investigational
BalsalazideBalsalazide may increase the nephrotoxic activities of Tacrolimus.Approved, Investigational
BasiliximabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Basiliximab.Approved, Investigational
BatimastatThe metabolism of Tacrolimus can be decreased when combined with Batimastat.Experimental
BcgThe therapeutic efficacy of Bcg can be decreased when used in combination with Tacrolimus.Investigational
BelataceptThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Belatacept.Approved
BelimumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Belimumab.Approved
BenazeprilThe metabolism of Tacrolimus can be decreased when combined with Benazepril.Approved, Investigational
BenoxaprofenBenoxaprofen may increase the nephrotoxic activities of Tacrolimus.Withdrawn
BenzamidineThe metabolism of Tacrolimus can be decreased when combined with Benzamidine.Experimental
BenznidazoleThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Benznidazole.Investigational
BenzocaineThe serum concentration of Tacrolimus can be increased when it is combined with Benzocaine.Approved
Benzoic AcidThe metabolism of Tacrolimus can be decreased when combined with Benzoic Acid.Approved
BepridilThe serum concentration of Tacrolimus can be increased when it is combined with Bepridil.Approved, Withdrawn
BetamethasoneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Betamethasone.Approved, Vet Approved
BetamethasoneThe serum concentration of Betamethasone can be decreased when it is combined with Tacrolimus.Approved, Vet Approved
Betulinic AcidBetulinic Acid may increase the nephrotoxic activities of Tacrolimus.Investigational
BexaroteneThe serum concentration of Tacrolimus can be decreased when it is combined with Bexarotene.Approved, Investigational
Bi201335The metabolism of Tacrolimus can be decreased when combined with Bi201335.Investigational
BifonazoleThe metabolism of Tacrolimus can be decreased when combined with Bifonazole.Approved
BiperidenThe serum concentration of Tacrolimus can be increased when it is combined with Biperiden.Approved
BivalirudinThe metabolism of Tacrolimus can be decreased when combined with Bivalirudin.Approved, Investigational
BleomycinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Bleomycin.Approved
BlinatumomabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Blinatumomab.Approved
BoceprevirThe metabolism of Tacrolimus can be decreased when combined with Boceprevir.Approved
BoceprevirThe serum concentration of Tacrolimus can be increased when it is combined with Boceprevir.Approved
BortezomibThe metabolism of Tacrolimus can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Tacrolimus can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Tacrolimus.Approved
Brentuximab vedotinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Brentuximab vedotin.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be decreased when it is combined with Tacrolimus.Approved
BriakinumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Briakinumab.Investigational
BromfenacBromfenac may increase the nephrotoxic activities of Tacrolimus.Approved
BromocriptineThe serum concentration of Bromocriptine can be decreased when it is combined with Tacrolimus.Approved, Investigational
BucillamineBucillamine may increase the nephrotoxic activities of Tacrolimus.Investigational
BudesonideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Budesonide.Approved
BuforminThe therapeutic efficacy of Buformin can be decreased when used in combination with Tacrolimus.Withdrawn
BuprenorphineThe serum concentration of Tacrolimus can be increased when it is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe serum concentration of Tacrolimus can be increased when it is combined with Buspirone.Approved, Investigational
BusulfanThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Busulfan.Approved, Investigational
ButenafineThe metabolism of Tacrolimus can be decreased when combined with Butenafine.Approved
ButoconazoleThe metabolism of Tacrolimus can be decreased when combined with Butoconazole.Approved
C1 Esterase Inhibitor (Human)The risk or severity of adverse effects can be increased when Tacrolimus is combined with C1 Esterase Inhibitor (Human).Approved
CabazitaxelThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Cabazitaxel.Approved
CabazitaxelThe serum concentration of Cabazitaxel can be decreased when it is combined with Tacrolimus.Approved
CaffeineThe serum concentration of Caffeine can be decreased when it is combined with Tacrolimus.Approved
CamptothecinThe serum concentration of Camptothecin can be decreased when it is combined with Tacrolimus.Experimental
CanagliflozinThe serum concentration of Canagliflozin can be decreased when it is combined with Tacrolimus.Approved
CanakinumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Canakinumab.Approved, Investigational
CandesartanThe serum concentration of Tacrolimus can be increased when it is combined with Candesartan.Approved
CandicidinThe metabolism of Tacrolimus can be decreased when combined with Candicidin.Withdrawn
CandoxatrilThe metabolism of Tacrolimus can be decreased when combined with Candoxatril.Experimental
CandoxatrilatThe metabolism of Tacrolimus can be decreased when combined with Candoxatrilat.Experimental
CapecitabineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Capecitabine.Approved, Investigational
CaptoprilThe metabolism of Tacrolimus can be decreased when combined with Captopril.Approved
CaptoprilThe serum concentration of Tacrolimus can be increased when it is combined with Captopril.Approved
CarbamazepineThe metabolism of Tacrolimus can be increased when combined with Carbamazepine.Approved, Investigational
CarbomycinThe serum concentration of Tacrolimus can be increased when it is combined with Carbomycin.Vet Approved
CarboplatinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Carboplatin.Approved
CarfilzomibThe serum concentration of Carfilzomib can be decreased when it is combined with Tacrolimus.Approved
CarmustineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Carmustine.Approved
CarprofenCarprofen may increase the nephrotoxic activities of Tacrolimus.Approved, Vet Approved, Withdrawn
CarvedilolThe serum concentration of Tacrolimus can be increased when it is combined with Carvedilol.Approved, Investigational
CaspofunginThe metabolism of Tacrolimus can be decreased when combined with Caspofungin.Approved
CaspofunginThe serum concentration of Tacrolimus can be increased when it is combined with Caspofungin.Approved
CaspofunginThe serum concentration of Tacrolimus can be decreased when it is combined with Caspofungin.Approved
CastanospermineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Castanospermine.Experimental
CastanospermineThe therapeutic efficacy of Castanospermine can be decreased when used in combination with Tacrolimus.Experimental
CastanospermineCastanospermine may increase the nephrotoxic activities of Tacrolimus.Experimental
CDX-110The risk or severity of adverse effects can be increased when Tacrolimus is combined with CDX-110.Investigational
CelecoxibCelecoxib may increase the nephrotoxic activities of Tacrolimus.Approved, Investigational
CeritinibThe serum concentration of Tacrolimus can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be decreased when it is combined with Tacrolimus.Withdrawn
Certolizumab pegolThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Certolizumab pegol.Approved
CeruleninThe metabolism of Tacrolimus can be decreased when combined with Cerulenin.Approved
ChlorambucilThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Chlorambucil.Approved
ChloramphenicolThe serum concentration of Tacrolimus can be increased when it is combined with Chloramphenicol.Approved, Vet Approved
ChloroquineThe serum concentration of Tacrolimus can be increased when it is combined with Chloroquine.Approved, Vet Approved
ChloroquineChloroquine may increase the nephrotoxic activities of Tacrolimus.Approved, Vet Approved
ChloroxineThe metabolism of Tacrolimus can be decreased when combined with Chloroxine.Approved
ChlorpromazineThe serum concentration of Chlorpromazine can be decreased when it is combined with Tacrolimus.Approved, Vet Approved
ChlorpropamideThe serum concentration of Tacrolimus can be increased when it is combined with Chlorpropamide.Approved
ChlorprothixeneThe serum concentration of Tacrolimus can be increased when it is combined with Chlorprothixene.Approved, Withdrawn
CholesterolThe serum concentration of Tacrolimus can be increased when it is combined with Cholesterol.Experimental
Cholic AcidThe serum concentration of Tacrolimus can be decreased when it is combined with Cholic Acid.Approved
ChymostatinThe metabolism of Tacrolimus can be decreased when combined with Chymostatin.Experimental
CiclopiroxThe metabolism of Tacrolimus can be decreased when combined with Ciclopirox.Approved, Investigational
CiglitazoneThe therapeutic efficacy of Ciglitazone can be decreased when used in combination with Tacrolimus.Experimental
CilastatinThe metabolism of Tacrolimus can be decreased when combined with Cilastatin.Approved
CilazaprilThe metabolism of Tacrolimus can be decreased when combined with Cilazapril.Approved
CilazaprilThe serum concentration of Tacrolimus can be increased when it is combined with Cilazapril.Approved
CimetidineThe serum concentration of Tacrolimus can be decreased when it is combined with Cimetidine.Approved
CinacalcetThe serum concentration of Tacrolimus can be decreased when it is combined with Cinacalcet.Approved
CiprofloxacinThe serum concentration of Ciprofloxacin can be decreased when it is combined with Tacrolimus.Approved, Investigational
CisplatinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Cisplatin.Approved
CisplatinThe serum concentration of Cisplatin can be decreased when it is combined with Tacrolimus.Approved
CitalopramThe metabolism of Tacrolimus can be decreased when combined with Citalopram.Approved
CitalopramThe serum concentration of Citalopram can be decreased when it is combined with Tacrolimus.Approved
CladribineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Cladribine.Approved, Investigational
ClarithromycinThe metabolism of Tacrolimus can be decreased when combined with Clarithromycin.Approved
ClarithromycinThe serum concentration of Tacrolimus can be increased when it is combined with Clarithromycin.Approved
ClemastineThe metabolism of Tacrolimus can be decreased when combined with Clemastine.Approved
ClevidipineThe serum concentration of Tacrolimus can be increased when it is combined with Clevidipine.Approved
ClobazamThe serum concentration of Clobazam can be decreased when it is combined with Tacrolimus.Approved, Illicit
ClofarabineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Clofarabine.Approved, Investigational
ClofazimineThe serum concentration of Tacrolimus can be increased when it is combined with Clofazimine.Approved, Investigational
ClomifeneThe serum concentration of Clomifene can be decreased when it is combined with Tacrolimus.Approved, Investigational
ClomipramineThe metabolism of Tacrolimus can be decreased when combined with Clomipramine.Approved, Vet Approved
ClomipramineThe serum concentration of Tacrolimus can be increased when it is combined with Clomipramine.Approved, Vet Approved
ClonidineThe serum concentration of Clonidine can be decreased when it is combined with Tacrolimus.Approved
ClonixinClonixin may increase the nephrotoxic activities of Tacrolimus.Approved
ClopidogrelThe serum concentration of Clopidogrel can be decreased when it is combined with Tacrolimus.Approved, Nutraceutical
ClotrimazoleThe metabolism of Tacrolimus can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClotrimazoleThe serum concentration of Tacrolimus can be increased when it is combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Clozapine.Approved
CobicistatThe metabolism of Tacrolimus can be decreased when combined with Cobicistat.Approved
CobimetinibThe serum concentration of Cobimetinib can be decreased when it is combined with Tacrolimus.Approved
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Tacrolimus.Approved
ColforsinThe serum concentration of Tacrolimus can be increased when it is combined with Colforsin.Experimental
ConivaptanThe serum concentration of Tacrolimus can be increased when it is combined with Conivaptan.Approved, Investigational
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be decreased when it is combined with Tacrolimus.Approved
CordycepinThe metabolism of Tacrolimus can be decreased when combined with Cordycepin.Investigational
CorticotropinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Corticotropin.Approved, Vet Approved
Cortisone acetateThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Cortisone acetate.Approved
CrizotinibThe serum concentration of Tacrolimus can be increased when it is combined with Crizotinib.Approved
CrizotinibThe metabolism of Tacrolimus can be decreased when combined with Crizotinib.Approved
CurcuminCurcumin may increase the nephrotoxic activities of Tacrolimus.Investigational
CyclophosphamideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Cyclophosphamide.Approved, Investigational
CyclophosphamideThe serum concentration of Tacrolimus can be increased when it is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Cyclosporine.Approved, Investigational, Vet Approved
CyclosporineTacrolimus may increase the nephrotoxic activities of Cyclosporine.Approved, Investigational, Vet Approved
CyclosporineThe metabolism of Tacrolimus can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
CytarabineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Cytarabine.Approved, Investigational
D-LimoneneD-Limonene may increase the nephrotoxic activities of Tacrolimus.Investigational
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be decreased when it is combined with Tacrolimus.Approved
Dabigatran etexilateThe metabolism of Tacrolimus can be decreased when combined with Dabigatran etexilate.Approved
DabrafenibThe serum concentration of Tacrolimus can be decreased when it is combined with Dabrafenib.Approved
DacarbazineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Dacarbazine.Approved, Investigational
DaclatasvirThe serum concentration of Tacrolimus can be increased when it is combined with Daclatasvir.Approved
DaclizumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Daclizumab.Approved, Investigational
DactinomycinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Dactinomycin.Approved
DactinomycinThe serum concentration of Dactinomycin can be decreased when it is combined with Tacrolimus.Approved
DanazolThe serum concentration of Tacrolimus can be increased when it is combined with Danazol.Approved
DapagliflozinThe serum concentration of Dapagliflozin can be decreased when it is combined with Tacrolimus.Approved
DapoxetineThe metabolism of Tacrolimus can be decreased when combined with Dapoxetine.Investigational
DarunavirThe metabolism of Tacrolimus can be decreased when combined with Darunavir.Approved
DasabuvirThe serum concentration of Tacrolimus can be increased when it is combined with Dasabuvir.Approved
DasatinibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Dasatinib.Approved, Investigational
DasatinibThe serum concentration of Tacrolimus can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Daunorubicin.Approved
DaunorubicinThe serum concentration of Daunorubicin can be decreased when it is combined with Tacrolimus.Approved
DebrisoquinThe serum concentration of Debrisoquin can be decreased when it is combined with Tacrolimus.Approved
Decanoic AcidThe metabolism of Tacrolimus can be decreased when combined with Decanoic Acid.Experimental
DeferasiroxThe serum concentration of Tacrolimus can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Tacrolimus can be decreased when combined with Delavirdine.Approved
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Tacrolimus.Approved
DeoxyspergualinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Deoxyspergualin.Investigational
DeoxyspergualinThe therapeutic efficacy of Deoxyspergualin can be decreased when used in combination with Tacrolimus.Investigational
DesipramineThe serum concentration of Tacrolimus can be increased when it is combined with Desipramine.Approved
DesloratadineThe serum concentration of Tacrolimus can be increased when it is combined with Desloratadine.Approved, Investigational
DexamethasoneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Dexamethasone.Approved, Investigational, Vet Approved
DexamethasoneThe serum concentration of Tacrolimus can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextromethorphanThe serum concentration of Tacrolimus can be increased when it is combined with Dextromethorphan.Approved
DiazepamThe serum concentration of Diazepam can be decreased when it is combined with Tacrolimus.Approved, Illicit, Vet Approved
DiclofenacThe serum concentration of Tacrolimus can be increased when it is combined with Diclofenac.Approved, Vet Approved
DiclofenacDiclofenac may increase the nephrotoxic activities of Tacrolimus.Approved, Vet Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be decreased when it is combined with Tacrolimus.Approved
DiflunisalDiflunisal may increase the nephrotoxic activities of Tacrolimus.Approved
DigitoxinThe serum concentration of Digitoxin can be decreased when it is combined with Tacrolimus.Approved
DigoxinThe serum concentration of Tacrolimus can be decreased when it is combined with Digoxin.Approved
DihydroergotamineThe metabolism of Tacrolimus can be decreased when combined with Dihydroergotamine.Approved
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be decreased when it is combined with Tacrolimus.Illicit
DiltiazemThe metabolism of Tacrolimus can be decreased when combined with Diltiazem.Approved
Dimethyl fumarateThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Dimethyl fumarate.Approved, Investigational
DinutuximabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Dinutuximab.Approved
DipyridamoleThe serum concentration of Dipyridamole can be decreased when it is combined with Tacrolimus.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Docetaxel.Approved, Investigational
DocetaxelThe serum concentration of Docetaxel can be decreased when it is combined with Tacrolimus.Approved, Investigational
DomperidoneThe serum concentration of Domperidone can be decreased when it is combined with Tacrolimus.Approved, Investigational, Vet Approved
DoxazosinThe serum concentration of Tacrolimus can be increased when it is combined with Doxazosin.Approved
DoxepinThe serum concentration of Tacrolimus can be increased when it is combined with Doxepin.Approved
DoxifluridineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Doxifluridine.Investigational
DoxorubicinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Doxorubicin.Approved, Investigational
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Tacrolimus.Approved, Investigational
DoxorubicinThe serum concentration of Doxorubicin can be decreased when it is combined with Tacrolimus.Approved, Investigational
DoxycyclineThe metabolism of Tacrolimus can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronabinolThe serum concentration of Tacrolimus can be increased when it is combined with Dronabinol.Approved, Illicit
DronedaroneTacrolimus may increase the QTc-prolonging activities of Dronedarone.Approved
DronedaroneThe metabolism of Tacrolimus can be decreased when combined with Dronedarone.Approved
DroxicamDroxicam may increase the nephrotoxic activities of Tacrolimus.Approved
DulaglutideThe therapeutic efficacy of Dulaglutide can be decreased when used in combination with Tacrolimus.Approved
DuvelisibDuvelisib may increase the nephrotoxic activities of Tacrolimus.Investigational
E6201E6201 may increase the nephrotoxic activities of Tacrolimus.Investigational
EbselenEbselen may increase the nephrotoxic activities of Tacrolimus.Investigational
EcabetThe metabolism of Tacrolimus can be decreased when combined with Ecabet.Approved, Investigational
EconazoleThe metabolism of Tacrolimus can be decreased when combined with Econazole.Approved
EculizumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Eculizumab.Approved, Investigational
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Tacrolimus.Approved
EdoxabanThe metabolism of Tacrolimus can be decreased when combined with Edoxaban.Approved
EfalizumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Efalizumab.Approved, Investigational
EfavirenzThe serum concentration of Tacrolimus can be decreased when it is combined with Efavirenz.Approved, Investigational
EfinaconazoleThe metabolism of Tacrolimus can be decreased when combined with Efinaconazole.Approved
EfonidipineThe serum concentration of Tacrolimus can be increased when it is combined with Efonidipine.Approved
ElafinThe metabolism of Tacrolimus can be decreased when combined with Elafin.Investigational
ElbasvirThe serum concentration of Tacrolimus can be increased when it is combined with Elbasvir.Approved
EletriptanThe serum concentration of Eletriptan can be decreased when it is combined with Tacrolimus.Approved, Investigational
EmpagliflozinThe therapeutic efficacy of Empagliflozin can be decreased when used in combination with Tacrolimus.Approved
EnalaprilThe metabolism of Tacrolimus can be decreased when combined with Enalapril.Approved, Vet Approved
EnalaprilThe serum concentration of Tacrolimus can be increased when it is combined with Enalapril.Approved, Vet Approved
EnalaprilatThe metabolism of Tacrolimus can be decreased when combined with Enalaprilat.Approved
EnalkirenThe metabolism of Tacrolimus can be decreased when combined with Enalkiren.Experimental
EnzalutamideThe serum concentration of Tacrolimus can be decreased when it is combined with Enzalutamide.Approved
EpinastineThe serum concentration of Epinastine can be decreased when it is combined with Tacrolimus.Approved, Investigational
EpirizoleEpirizole may increase the nephrotoxic activities of Tacrolimus.Approved
EpirubicinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Epirubicin.Approved
EplerenoneEplerenone may increase the hyperkalemic activities of Tacrolimus.Approved
ErgonovineThe serum concentration of Tacrolimus can be increased when it is combined with Ergonovine.Approved
ErgotamineThe serum concentration of Tacrolimus can be increased when it is combined with Ergotamine.Approved
ErlotinibThe serum concentration of Erlotinib can be decreased when it is combined with Tacrolimus.Approved, Investigational
ErtapenemThe serum concentration of Tacrolimus can be increased when it is combined with Ertapenem.Approved, Investigational
ErythromycinThe serum concentration of Tacrolimus can be increased when it is combined with Erythromycin.Approved, Vet Approved
ErythromycinThe metabolism of Tacrolimus can be decreased when combined with Erythromycin.Approved, Vet Approved
EscitalopramThe metabolism of Tacrolimus can be decreased when combined with Escitalopram.Approved, Investigational
Eslicarbazepine acetateThe serum concentration of Tacrolimus can be decreased when it is combined with Eslicarbazepine acetate.Approved
EsomeprazoleThe serum concentration of Tacrolimus can be increased when it is combined with Esomeprazole.Approved, Investigational
EstradiolThe serum concentration of Estradiol can be decreased when it is combined with Tacrolimus.Approved, Investigational, Vet Approved
EstramustineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Estramustine.Approved
EstramustineThe serum concentration of Tacrolimus can be increased when it is combined with Estramustine.Approved
EstriolThe serum concentration of Estriol can be decreased when it is combined with Tacrolimus.Approved, Vet Approved
EstroneThe serum concentration of Estrone can be decreased when it is combined with Tacrolimus.Approved
EtanerceptThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Etanercept.Approved, Investigational
EtanerceptEtanercept may increase the nephrotoxic activities of Tacrolimus.Approved, Investigational
EthanolEthanol can cause an increase in the absorption of Tacrolimus resulting in an increased serum concentration and potentially a worsening of adverse effects.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be decreased when it is combined with Tacrolimus.Approved
EtodolacEtodolac may increase the nephrotoxic activities of Tacrolimus.Approved, Investigational, Vet Approved
EtofenamateEtofenamate may increase the nephrotoxic activities of Tacrolimus.Approved
EtoperidoneThe metabolism of Tacrolimus can be decreased when combined with Etoperidone.Approved
EtoposideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Etoposide.Approved
EtoposideThe serum concentration of Etoposide can be decreased when it is combined with Tacrolimus.Approved
EtoricoxibEtoricoxib may increase the nephrotoxic activities of Tacrolimus.Approved, Investigational
EtravirineThe serum concentration of Tacrolimus can be decreased when it is combined with Etravirine.Approved
Evening primrose oilEvening primrose oil may increase the nephrotoxic activities of Tacrolimus.Approved
EverolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Everolimus.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Tacrolimus.Approved
ExenatideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Tacrolimus.Approved, Investigational
exisulindexisulind may increase the nephrotoxic activities of Tacrolimus.Investigational
EzetimibeThe serum concentration of Ezetimibe can be decreased when it is combined with Tacrolimus.Approved
FelodipineThe serum concentration of Tacrolimus can be increased when it is combined with Felodipine.Approved, Investigational
FenbufenFenbufen may increase the nephrotoxic activities of Tacrolimus.Approved
FenfluramineThe metabolism of Tacrolimus can be decreased when combined with Fenfluramine.Illicit, Withdrawn
FenofibrateTacrolimus may increase the nephrotoxic activities of Fenofibrate.Approved
FenoprofenFenoprofen may increase the nephrotoxic activities of Tacrolimus.Approved
FentanylThe serum concentration of Tacrolimus can be increased when it is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FesoterodineThe serum concentration of Fesoterodine can be decreased when it is combined with Tacrolimus.Approved
FexofenadineThe serum concentration of Fexofenadine can be decreased when it is combined with Tacrolimus.Approved
FidaxomicinThe serum concentration of Fidaxomicin can be decreased when it is combined with Tacrolimus.Approved
FingolimodThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Fingolimod.Approved, Investigational
FingolimodTacrolimus may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
FloctafenineFloctafenine may increase the nephrotoxic activities of Tacrolimus.Approved, Withdrawn
FloxuridineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Floxuridine.Approved
FluconazoleThe serum concentration of Tacrolimus can be increased when it is combined with Fluconazole.Approved
FluconazoleThe metabolism of Tacrolimus can be decreased when combined with Fluconazole.Approved
FlucytosineThe metabolism of Tacrolimus can be decreased when combined with Flucytosine.Approved
FludarabineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Fludarabine.Approved
FludrocortisoneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Fludrocortisone.Approved
FlunixinFlunixin may increase the nephrotoxic activities of Tacrolimus.Vet Approved
FluorouracilThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Fluorouracil.Approved
FluoxetineThe metabolism of Tacrolimus can be decreased when combined with Fluoxetine.Approved, Vet Approved
FluoxetineThe serum concentration of Tacrolimus can be increased when it is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe serum concentration of Tacrolimus can be increased when it is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe serum concentration of Tacrolimus can be increased when it is combined with Fluphenazine.Approved
FlurazepamThe serum concentration of Tacrolimus can be increased when it is combined with Flurazepam.Approved, Illicit
FlurbiprofenFlurbiprofen may increase the nephrotoxic activities of Tacrolimus.Approved, Investigational
Fluticasone furoateThe serum concentration of Fluticasone furoate can be decreased when it is combined with Tacrolimus.Approved
FluvoxamineThe metabolism of Tacrolimus can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Tacrolimus can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Tacrolimus can be increased when it is combined with Fosaprepitant.Approved
FoscarnetFoscarnet may increase the nephrotoxic activities of Tacrolimus.Approved
FosinoprilThe metabolism of Tacrolimus can be decreased when combined with Fosinopril.Approved
FosphenytoinThe metabolism of Tacrolimus can be increased when combined with Fosphenytoin.Approved
FosphenytoinThe serum concentration of Tacrolimus can be decreased when it is combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Tacrolimus can be increased when it is combined with Fusidic Acid.Approved
G17DTThe risk or severity of adverse effects can be increased when Tacrolimus is combined with G17DT.Investigational
GabexateThe metabolism of Tacrolimus can be decreased when combined with Gabexate.Investigational
Gallium nitrateThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Gallium nitrate.Approved, Investigational
GefitinibThe serum concentration of Gefitinib can be decreased when it is combined with Tacrolimus.Approved, Investigational
GeldanamycinThe metabolism of Tacrolimus can be decreased when combined with Geldanamycin.Experimental
GemcitabineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Gemcitabine.Approved
GemcitabineThe serum concentration of Gemcitabine can be decreased when it is combined with Tacrolimus.Approved
Gemtuzumab ozogamicinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Gemtuzumab ozogamicin.Approved, Investigational, Withdrawn
GenisteinThe serum concentration of Tacrolimus can be increased when it is combined with Genistein.Investigational
GI-5005The risk or severity of adverse effects can be increased when Tacrolimus is combined with GI-5005.Investigational
Glatiramer AcetateThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Glatiramer Acetate.Approved, Investigational
GlibornurideThe therapeutic efficacy of Glibornuride can be decreased when used in combination with Tacrolimus.Withdrawn
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Tacrolimus.Approved
GlimepirideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Glimepiride.Approved
GlimepirideThe therapeutic efficacy of Glimepiride can be decreased when used in combination with Tacrolimus.Approved
GlipizideThe therapeutic efficacy of Glipizide can be decreased when used in combination with Tacrolimus.Approved
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Tacrolimus.Approved
GlyburideThe serum concentration of Tacrolimus can be increased when it is combined with Glyburide.Approved
GlycerolThe serum concentration of Tacrolimus can be increased when it is combined with Glycerol.Experimental
GlyphosateThe metabolism of Tacrolimus can be decreased when combined with Glyphosate.Experimental
GM6001The metabolism of Tacrolimus can be decreased when combined with GM6001.Experimental
GolimumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Golimumab.Approved
Gramicidin DThe serum concentration of Tacrolimus can be increased when it is combined with Gramicidin D.Approved
GrazoprevirThe serum concentration of Grazoprevir can be decreased when it is combined with Tacrolimus.Approved
GrepafloxacinThe serum concentration of Grepafloxacin can be decreased when it is combined with Tacrolimus.Withdrawn
GriseofulvinThe metabolism of Tacrolimus can be decreased when combined with Griseofulvin.Approved, Vet Approved
GusperimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Gusperimus.Investigational
GusperimusThe therapeutic efficacy of Gusperimus can be decreased when used in combination with Tacrolimus.Investigational
HaloperidolThe serum concentration of Haloperidol can be decreased when it is combined with Tacrolimus.Approved
HaloproginThe metabolism of Tacrolimus can be decreased when combined with Haloprogin.Approved, Withdrawn
HexetidineThe metabolism of Tacrolimus can be decreased when combined with Hexetidine.Approved
HigenamineHigenamine may increase the nephrotoxic activities of Tacrolimus.Investigational
HirulogThe metabolism of Tacrolimus can be decreased when combined with Hirulog.Experimental
HMPL-004HMPL-004 may increase the nephrotoxic activities of Tacrolimus.Investigational
HydrocortisoneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Hydrocortisone.Approved, Vet Approved
HydrocortisoneThe serum concentration of Hydrocortisone can be decreased when it is combined with Tacrolimus.Approved, Vet Approved
HydroxyureaThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Hydroxyurea.Approved
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Ibritumomab tiuxetan.Approved
IbrutinibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Ibrutinib.Approved
IbuprofenThe serum concentration of Ibuprofen can be decreased when it is combined with Tacrolimus.Approved
IbuprofenIbuprofen may increase the nephrotoxic activities of Tacrolimus.Approved
IbuproxamIbuproxam may increase the nephrotoxic activities of Tacrolimus.Withdrawn
IcatibantThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Icatibant.Approved
IcatibantIcatibant may increase the nephrotoxic activities of Tacrolimus.Approved
IdarubicinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Idarubicin.Approved
IdelalisibThe serum concentration of Tacrolimus can be increased when it is combined with Idelalisib.Approved
IdelalisibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Idelalisib.Approved
idraparinuxThe metabolism of Tacrolimus can be decreased when combined with idraparinux.Investigational
IfosfamideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Ifosfamide.Approved
ImatinibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Imatinib.Approved
ImatinibThe metabolism of Tacrolimus can be decreased when combined with Imatinib.Approved
ImidaprilThe metabolism of Tacrolimus can be decreased when combined with Imidapril.Investigational
ImipramineThe serum concentration of Imipramine can be decreased when it is combined with Tacrolimus.Approved
ImiquimodThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Imiquimod.Approved, Investigational
IndacaterolThe serum concentration of Indacaterol can be decreased when it is combined with Tacrolimus.Approved
IndalpineThe metabolism of Tacrolimus can be decreased when combined with Indalpine.Investigational, Withdrawn
IndinavirThe metabolism of Tacrolimus can be decreased when combined with Indinavir.Approved
IndomethacinThe serum concentration of Indomethacin can be decreased when it is combined with Tacrolimus.Approved, Investigational
IndomethacinIndomethacin may increase the nephrotoxic activities of Tacrolimus.Approved, Investigational
IndoprofenIndoprofen may increase the nephrotoxic activities of Tacrolimus.Withdrawn
InfliximabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Infliximab.Approved
INGN 201The risk or severity of adverse effects can be increased when Tacrolimus is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Tacrolimus is combined with INGN 225.Investigational
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Tacrolimus.Approved
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Tacrolimus.Approved
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Tacrolimus.Approved
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Tacrolimus.Approved
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Tacrolimus.Approved
Insulin PorkThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Tacrolimus.Approved
IrinotecanThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Irinotecan.Approved, Investigational
IrinotecanThe serum concentration of Irinotecan can be decreased when it is combined with Tacrolimus.Approved, Investigational
IsavuconazoniumThe metabolism of Tacrolimus can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoconazoleThe metabolism of Tacrolimus can be decreased when combined with Isoconazole.Approved
IsoflurophateThe metabolism of Tacrolimus can be decreased when combined with Isoflurophate.Approved, Withdrawn
IsoxicamIsoxicam may increase the nephrotoxic activities of Tacrolimus.Withdrawn
IsradipineThe metabolism of Tacrolimus can be decreased when combined with Isradipine.Approved
IsradipineThe serum concentration of Tacrolimus can be increased when it is combined with Isradipine.Approved
ItraconazoleThe metabolism of Tacrolimus can be decreased when combined with Itraconazole.Approved, Investigational
ItraconazoleThe serum concentration of Tacrolimus can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Tacrolimus can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Ivermectin can be decreased when it is combined with Tacrolimus.Approved, Vet Approved
IxazomibThe metabolism of Tacrolimus can be decreased when combined with Ixazomib.Approved
JosamycinThe serum concentration of Tacrolimus can be increased when it is combined with Josamycin.Approved
KebuzoneKebuzone may increase the nephrotoxic activities of Tacrolimus.Experimental
KetamineThe serum concentration of Tacrolimus can be increased when it is combined with Ketamine.Approved, Vet Approved
KetazolamThe serum concentration of Ketazolam can be decreased when it is combined with Tacrolimus.Approved
KetoconazoleThe metabolism of Tacrolimus can be decreased when combined with Ketoconazole.Approved, Investigational
KetoconazoleThe serum concentration of Tacrolimus can be increased when it is combined with Ketoconazole.Approved, Investigational
KetoprofenKetoprofen may increase the nephrotoxic activities of Tacrolimus.Approved, Vet Approved
KetorolacKetorolac may increase the nephrotoxic activities of Tacrolimus.Approved
KitasamycinThe serum concentration of Tacrolimus can be increased when it is combined with Kitasamycin.Experimental
L-PhenylalanineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with L-Phenylalanine.Approved, Nutraceutical
LamivudineThe serum concentration of Lamivudine can be decreased when it is combined with Tacrolimus.Approved, Investigational
LamotrigineThe serum concentration of Lamotrigine can be decreased when it is combined with Tacrolimus.Approved, Investigational
LansoprazoleThe serum concentration of Tacrolimus can be increased when it is combined with Lansoprazole.Approved, Investigational
LansoprazoleThe serum concentration of Lansoprazole can be decreased when it is combined with Tacrolimus.Approved, Investigational
LapatinibThe serum concentration of Tacrolimus can be increased when it is combined with Lapatinib.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be decreased when it is combined with Tacrolimus.Approved
LeflunomideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Leflunomide.Approved, Investigational
LeflunomideLeflunomide may increase the nephrotoxic activities of Tacrolimus.Approved, Investigational
LenalidomideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Lenalidomide.Approved
LenalidomideThe serum concentration of Lenalidomide can be decreased when it is combined with Tacrolimus.Approved
LenvatinibThe serum concentration of Lenvatinib can be decreased when it is combined with Tacrolimus.Approved
LepirudinThe metabolism of Tacrolimus can be decreased when combined with Lepirudin.Approved
LevetiracetamThe serum concentration of Levetiracetam can be decreased when it is combined with Tacrolimus.Approved, Investigational
LevofloxacinThe serum concentration of Levofloxacin can be decreased when it is combined with Tacrolimus.Approved, Investigational
LevofloxacinLevofloxacin may increase the QTc-prolonging activities of Tacrolimus.Approved, Investigational
LevomilnacipranThe metabolism of Tacrolimus can be decreased when combined with Levomilnacipran.Approved
LevomilnacipranThe serum concentration of Levomilnacipran can be decreased when it is combined with Tacrolimus.Approved
LevothyroxineThe serum concentration of Tacrolimus can be decreased when it is combined with Levothyroxine.Approved
LidocaineThe serum concentration of Tacrolimus can be increased when it is combined with Lidocaine.Approved, Vet Approved
LinagliptinThe metabolism of Tacrolimus can be decreased when combined with Linagliptin.Approved
LinagliptinThe serum concentration of Linagliptin can be decreased when it is combined with Tacrolimus.Approved
LiothyronineThe serum concentration of Tacrolimus can be decreased when it is combined with Liothyronine.Approved, Vet Approved
LiotrixThe serum concentration of Tacrolimus can be decreased when it is combined with Liotrix.Approved
LiraglutideThe therapeutic efficacy of Liraglutide can be decreased when used in combination with Tacrolimus.Approved
LisinoprilThe metabolism of Tacrolimus can be decreased when combined with Lisinopril.Approved, Investigational
LisinoprilThe serum concentration of Tacrolimus can be increased when it is combined with Lisinopril.Approved, Investigational
LisofyllineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Lisofylline.Investigational
LisofyllineLisofylline may increase the nephrotoxic activities of Tacrolimus.Investigational
LomitapideThe serum concentration of Tacrolimus can be increased when it is combined with Lomitapide.Approved
LomustineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Lomustine.Approved
LoperamideThe serum concentration of Loperamide can be decreased when it is combined with Tacrolimus.Approved
LopinavirThe metabolism of Tacrolimus can be decreased when combined with Lopinavir.Approved
LoratadineThe serum concentration of Tacrolimus can be increased when it is combined with Loratadine.Approved
LornoxicamLornoxicam may increase the nephrotoxic activities of Tacrolimus.Approved
LosartanThe serum concentration of Losartan can be decreased when it is combined with Tacrolimus.Approved
LovastatinThe metabolism of Tacrolimus can be decreased when combined with Lovastatin.Approved, Investigational
LoxoprofenLoxoprofen may increase the nephrotoxic activities of Tacrolimus.Approved
Lu AA21004The metabolism of Tacrolimus can be decreased when combined with Lu AA21004.Investigational
LuliconazoleThe serum concentration of Tacrolimus can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Tacrolimus can be decreased when it is combined with Lumacaftor.Approved
LumiracoxibLumiracoxib may increase the nephrotoxic activities of Tacrolimus.Approved, Investigational
Lx211The risk or severity of adverse effects can be increased when Tacrolimus is combined with Lx211.Investigational
Magnesium salicylateMagnesium salicylate may increase the nephrotoxic activities of Tacrolimus.Approved
MannitolThe serum concentration of Mannitol can be decreased when it is combined with Tacrolimus.Approved, Investigational
MaprotilineThe serum concentration of Tacrolimus can be increased when it is combined with Maprotiline.Approved
MasoprocolMasoprocol may increase the nephrotoxic activities of Tacrolimus.Approved
MebendazoleThe serum concentration of Tacrolimus can be increased when it is combined with Mebendazole.Approved, Vet Approved
MechlorethamineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Mechlorethamine.Approved
Meclofenamic acidMeclofenamic acid may increase the nephrotoxic activities of Tacrolimus.Approved, Vet Approved
Mefenamic acidMefenamic acid may increase the nephrotoxic activities of Tacrolimus.Approved
MefloquineThe serum concentration of Tacrolimus can be increased when it is combined with Mefloquine.Approved
Megestrol acetateThe serum concentration of Tacrolimus can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
MeloxicamMeloxicam may increase the nephrotoxic activities of Tacrolimus.Approved, Vet Approved
MelphalanThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Melphalan.Approved
MepolizumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Mepolizumab.Approved, Investigational
MeprobamateThe serum concentration of Tacrolimus can be increased when it is combined with Meprobamate.Approved, Illicit
MercaptopurineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Mercaptopurine.Approved
MesalazineMesalazine may increase the nephrotoxic activities of Tacrolimus.Approved
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Tacrolimus.Withdrawn
MetamizoleMetamizole may increase the nephrotoxic activities of Tacrolimus.Withdrawn
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Tacrolimus.Approved
MethadoneThe serum concentration of Tacrolimus can be increased when it is combined with Methadone.Approved
MethotrexateThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Methotrexate.Approved
MethotrexateThe serum concentration of Methotrexate can be decreased when it is combined with Tacrolimus.Approved
MethylprednisoloneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Methylprednisolone.Approved, Vet Approved
MethylprednisoloneThe serum concentration of Methylprednisolone can be decreased when it is combined with Tacrolimus.Approved, Vet Approved
MetoprololThe serum concentration of Metoprolol can be decreased when it is combined with Tacrolimus.Approved, Investigational
MevastatinThe metabolism of Tacrolimus can be decreased when combined with Mevastatin.Experimental
MibefradilThe serum concentration of Tacrolimus can be increased when it is combined with Mibefradil.Withdrawn
MicafunginThe metabolism of Tacrolimus can be decreased when combined with Micafungin.Approved, Investigational
MiconazoleThe metabolism of Tacrolimus can be decreased when combined with Miconazole.Approved, Investigational, Vet Approved
MiconazoleThe serum concentration of Tacrolimus can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Midazolam can be decreased when it is combined with Tacrolimus.Approved, Illicit
MifepristoneMifepristone may increase the QTc-prolonging activities of Tacrolimus.Approved, Investigational
MifepristoneThe serum concentration of Tacrolimus can be increased when it is combined with Mifepristone.Approved, Investigational
MiglitolThe therapeutic efficacy of Miglitol can be decreased when used in combination with Tacrolimus.Approved
MiglustatThe therapeutic efficacy of Miglustat can be decreased when used in combination with Tacrolimus.Approved
MilnacipranThe metabolism of Tacrolimus can be decreased when combined with Milnacipran.Approved
MiltefosineThe metabolism of Tacrolimus can be decreased when combined with Miltefosine.Approved
MirabegronThe serum concentration of Mirabegron can be decreased when it is combined with Tacrolimus.Approved
MitiglinideThe therapeutic efficacy of Mitiglinide can be decreased when used in combination with Tacrolimus.Approved, Investigational
MitomycinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Mitomycin.Approved
MitomycinThe serum concentration of Tacrolimus can be increased when it is combined with Mitomycin.Approved
MitotaneThe serum concentration of Tacrolimus can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Mitoxantrone.Approved, Investigational
MitoxantroneThe serum concentration of Mitoxantrone can be decreased when it is combined with Tacrolimus.Approved, Investigational
MizoribineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Mizoribine.Investigational
MizoribineMizoribine may increase the nephrotoxic activities of Tacrolimus.Investigational
ModafinilThe serum concentration of Tacrolimus can be decreased when it is combined with Modafinil.Approved, Investigational
MoexiprilThe metabolism of Tacrolimus can be decreased when combined with Moexipril.Approved
MonensinThe metabolism of Tacrolimus can be decreased when combined with Monensin.Vet Approved
MorphineThe serum concentration of Morphine can be decreased when it is combined with Tacrolimus.Approved, Investigational
MuromonabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Muromonab.Approved, Investigational
Mycophenolate mofetilThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Mycophenolate mofetil.Approved, Investigational
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be decreased when it is combined with Tacrolimus.Approved, Investigational
Mycophenolate mofetilMycophenolate mofetil may increase the nephrotoxic activities of Tacrolimus.Approved, Investigational
Mycophenolic acidThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Mycophenolic acid.Approved
Mycophenolic acidMycophenolic acid may increase the nephrotoxic activities of Tacrolimus.Approved
MyxothiazolThe metabolism of Tacrolimus can be decreased when combined with Myxothiazol.Experimental
N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-ProlineThe metabolism of Tacrolimus can be decreased when combined with N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-Proline.Experimental
NabumetoneNabumetone may increase the nephrotoxic activities of Tacrolimus.Approved
NadololThe serum concentration of Nadolol can be decreased when it is combined with Tacrolimus.Approved
NafamostatThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Nafamostat.Investigational
NafamostatThe metabolism of Tacrolimus can be decreased when combined with Nafamostat.Investigational
NafcillinThe serum concentration of Tacrolimus can be decreased when it is combined with Nafcillin.Approved
NaftifineThe metabolism of Tacrolimus can be decreased when combined with Naftifine.Approved
NaftifineNaftifine may increase the nephrotoxic activities of Tacrolimus.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Tacrolimus.Approved
NaloxoneThe serum concentration of Naloxone can be decreased when it is combined with Tacrolimus.Approved, Vet Approved
NaltrexoneThe serum concentration of Tacrolimus can be increased when it is combined with Naltrexone.Approved, Investigational, Vet Approved
NaproxenNaproxen may increase the nephrotoxic activities of Tacrolimus.Approved, Vet Approved
NaringeninThe serum concentration of Tacrolimus can be increased when it is combined with Naringenin.Experimental
NatalizumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Natalizumab.Approved, Investigational
NatamycinThe metabolism of Tacrolimus can be decreased when combined with Natamycin.Approved
NateglinideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Tacrolimus.Approved, Investigational
NCX 4016The metabolism of Tacrolimus can be decreased when combined with NCX 4016.Investigational
NefazodoneThe metabolism of Tacrolimus can be decreased when combined with Nefazodone.Approved, Withdrawn
NelarabineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Nelarabine.Approved, Investigational
NelfinavirThe metabolism of Tacrolimus can be decreased when combined with Nelfinavir.Approved
NeostigmineThe serum concentration of Tacrolimus can be increased when it is combined with Neostigmine.Approved, Vet Approved
NepafenacNepafenac may increase the nephrotoxic activities of Tacrolimus.Approved
NetupitantThe serum concentration of Tacrolimus can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Tacrolimus can be increased when combined with Nevirapine.Approved
NicardipineThe serum concentration of Nicardipine can be decreased when it is combined with Tacrolimus.Approved
NicardipineThe serum concentration of Tacrolimus can be increased when it is combined with Nicardipine.Approved
NifedipineThe serum concentration of Tacrolimus can be decreased when it is combined with Nifedipine.Approved
NifedipineThe serum concentration of Tacrolimus can be increased when it is combined with Nifedipine.Approved
Niflumic AcidNiflumic Acid may increase the nephrotoxic activities of Tacrolimus.Approved
NilotinibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Nilotinib.Approved, Investigational
NilotinibThe metabolism of Tacrolimus can be decreased when combined with Nilotinib.Approved, Investigational
NimesulideNimesulide may increase the nephrotoxic activities of Tacrolimus.Approved, Withdrawn
NimodipineThe serum concentration of Tacrolimus can be increased when it is combined with Nimodipine.Approved
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Tacrolimus.Approved
NisoldipineThe serum concentration of Tacrolimus can be increased when it is combined with Nisoldipine.Approved
NitrazepamThe serum concentration of Tacrolimus can be increased when it is combined with Nitrazepam.Approved
NitrendipineThe serum concentration of Tacrolimus can be increased when it is combined with Nitrendipine.Approved
NitroaspirinThe metabolism of Tacrolimus can be decreased when combined with Nitroaspirin.Investigational
NitroxolineThe metabolism of Tacrolimus can be decreased when combined with Nitroxoline.Approved
NizatidineThe serum concentration of Nizatidine can be decreased when it is combined with Tacrolimus.Approved
NorethisteroneThe serum concentration of Tacrolimus can be decreased when it is combined with Norethisterone.Approved
NystatinThe metabolism of Tacrolimus can be decreased when combined with Nystatin.Approved, Vet Approved
ObinutuzumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Obinutuzumab.Approved
OlanzapineThe metabolism of Tacrolimus can be decreased when combined with Olanzapine.Approved, Investigational
OlanzapineThe serum concentration of Olanzapine can be decreased when it is combined with Tacrolimus.Approved, Investigational
OlaparibThe metabolism of Tacrolimus can be decreased when combined with Olaparib.Approved
OleandomycinThe serum concentration of Tacrolimus can be increased when it is combined with Oleandomycin.Vet Approved
OlopatadineOlopatadine may increase the nephrotoxic activities of Tacrolimus.Approved
OlsalazineOlsalazine may increase the nephrotoxic activities of Tacrolimus.Approved
OmapatrilatThe metabolism of Tacrolimus can be decreased when combined with Omapatrilat.Investigational
OmbitasvirThe serum concentration of Tacrolimus can be increased when it is combined with Ombitasvir.Approved
OmbitasvirThe serum concentration of Ombitasvir can be decreased when it is combined with Tacrolimus.Approved
OmeprazoleThe serum concentration of Tacrolimus can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OrgoteinOrgotein may increase the nephrotoxic activities of Tacrolimus.Vet Approved
OsimertinibThe serum concentration of Tacrolimus can be increased when it is combined with Osimertinib.Approved
OtamixabanThe metabolism of Tacrolimus can be decreased when combined with Otamixaban.Investigational
OxaliplatinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Oxaliplatin.Approved, Investigational
OxaprozinOxaprozin may increase the nephrotoxic activities of Tacrolimus.Approved
OxiconazoleThe metabolism of Tacrolimus can be decreased when combined with Oxiconazole.Approved
OxyphenbutazoneOxyphenbutazone may increase the nephrotoxic activities of Tacrolimus.Withdrawn
P-NitrophenolThe serum concentration of Tacrolimus can be increased when it is combined with P-Nitrophenol.Experimental
PaclitaxelThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Paclitaxel.Approved, Vet Approved
PaclitaxelThe serum concentration of Paclitaxel can be decreased when it is combined with Tacrolimus.Approved, Vet Approved
pafuramidineThe metabolism of Tacrolimus can be decreased when combined with pafuramidine.Investigational
PalbociclibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Palbociclib.Approved
PalbociclibThe serum concentration of Tacrolimus can be increased when it is combined with Palbociclib.Approved
Palmitic AcidThe serum concentration of Tacrolimus can be increased when it is combined with Palmitic Acid.Experimental
PanobinostatThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Panobinostat.Approved, Investigational
PanobinostatThe serum concentration of Panobinostat can be decreased when it is combined with Tacrolimus.Approved, Investigational
PantoprazoleThe serum concentration of Tacrolimus can be increased when it is combined with Pantoprazole.Approved
ParecoxibParecoxib may increase the nephrotoxic activities of Tacrolimus.Approved
ParitaprevirThe serum concentration of Tacrolimus can be increased when it is combined with Paritaprevir.Approved
ParoxetineThe metabolism of Tacrolimus can be decreased when combined with Paroxetine.Approved, Investigational
ParoxetineThe serum concentration of Tacrolimus can be increased when it is combined with Paroxetine.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Tacrolimus.Approved
PazopanibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Pazopanib.Approved
PegaspargaseThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Pegaspargase.Approved, Investigational
PemetrexedThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Pemetrexed.Approved, Investigational
PentamidineThe metabolism of Tacrolimus can be decreased when combined with Pentamidine.Approved
PentobarbitalThe metabolism of Tacrolimus can be increased when combined with Pentobarbital.Approved, Vet Approved
PentostatinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Pentostatin.Approved, Investigational
PerindoprilThe metabolism of Tacrolimus can be decreased when combined with Perindopril.Approved
PerindoprilThe serum concentration of Tacrolimus can be increased when it is combined with Perindopril.Approved
PhenforminThe therapeutic efficacy of Phenformin can be decreased when used in combination with Tacrolimus.Approved, Withdrawn
PhenobarbitalThe metabolism of Tacrolimus can be increased when combined with Phenobarbital.Approved
PhenylbutazonePhenylbutazone may increase the nephrotoxic activities of Tacrolimus.Approved, Vet Approved
PhenytoinThe metabolism of Tacrolimus can be increased when combined with Phenytoin.Approved, Vet Approved
PhenytoinThe serum concentration of Tacrolimus can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PhosphoramidonThe metabolism of Tacrolimus can be decreased when combined with Phosphoramidon.Experimental
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Tacrolimus.Approved, Investigational
PimecrolimusPimecrolimus may increase the nephrotoxic activities of Tacrolimus.Approved, Investigational
PimozideThe serum concentration of Tacrolimus can be increased when it is combined with Pimozide.Approved
PioglitazoneThe therapeutic efficacy of Pioglitazone can be decreased when used in combination with Tacrolimus.Approved, Investigational
PirarubicinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Pirarubicin.Investigational
PirfenidoneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Pirfenidone.Investigational
PirfenidonePirfenidone may increase the nephrotoxic activities of Tacrolimus.Investigational
PiroxicamPiroxicam may increase the nephrotoxic activities of Tacrolimus.Approved, Investigational
PitavastatinThe serum concentration of Pitavastatin can be decreased when it is combined with Tacrolimus.Approved
Platelet Activating FactorThe serum concentration of Tacrolimus can be decreased when it is combined with Platelet Activating Factor.Experimental
PomalidomideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Pomalidomide.Approved
PomalidomideThe serum concentration of Pomalidomide can be decreased when it is combined with Tacrolimus.Approved
PonatinibThe serum concentration of Ponatinib can be decreased when it is combined with Tacrolimus.Approved
PosaconazoleThe metabolism of Tacrolimus can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PosaconazoleThe serum concentration of Tacrolimus can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PralatrexateThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Pralatrexate.Approved
PramlintideThe therapeutic efficacy of Pramlintide can be decreased when used in combination with Tacrolimus.Approved, Investigational
PravastatinThe serum concentration of Pravastatin can be decreased when it is combined with Tacrolimus.Approved
PrazosinThe serum concentration of Prazosin can be decreased when it is combined with Tacrolimus.Approved
PrednisoloneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Prednisolone.Approved, Vet Approved
PrednisoloneThe serum concentration of Prednisolone can be decreased when it is combined with Tacrolimus.Approved, Vet Approved
PrednisoneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Prednisone.Approved, Vet Approved
PrednisoneThe serum concentration of Prednisone can be decreased when it is combined with Tacrolimus.Approved, Vet Approved
PrimidoneThe metabolism of Tacrolimus can be increased when combined with Primidone.Approved, Vet Approved
PrinomastatThe metabolism of Tacrolimus can be decreased when combined with Prinomastat.Investigational
ProbenecidThe serum concentration of Tacrolimus can be increased when it is combined with Probenecid.Approved
ProcarbazineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Procarbazine.Approved
ProgesteroneThe serum concentration of Tacrolimus can be decreased when it is combined with Progesterone.Approved, Vet Approved
PromethazineThe serum concentration of Tacrolimus can be increased when it is combined with Promethazine.Approved
PropacetamolPropacetamol may increase the nephrotoxic activities of Tacrolimus.Approved
PropafenoneThe serum concentration of Tacrolimus can be increased when it is combined with Propafenone.Approved
PropranololThe serum concentration of Propranolol can be decreased when it is combined with Tacrolimus.Approved, Investigational
ProtriptylineThe serum concentration of Tacrolimus can be increased when it is combined with Protriptyline.Approved
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Tacrolimus.Approved
PTC299PTC299 may increase the nephrotoxic activities of Tacrolimus.Investigational
QuercetinThe serum concentration of Tacrolimus can be increased when it is combined with Quercetin.Experimental
QuetiapineThe serum concentration of Quetiapine can be decreased when it is combined with Tacrolimus.Approved
QuinacrineThe serum concentration of Tacrolimus can be increased when it is combined with Quinacrine.Approved
QuinaprilThe metabolism of Tacrolimus can be decreased when combined with Quinapril.Approved, Investigational
QuinidineThe serum concentration of Quinidine can be decreased when it is combined with Tacrolimus.Approved
QuinineThe serum concentration of Quinine can be decreased when it is combined with Tacrolimus.Approved
RabeprazoleThe serum concentration of Tacrolimus can be increased when it is combined with Rabeprazole.Approved, Investigational
Rabies vaccineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Rabies vaccine.Approved
Rabies vaccineThe therapeutic efficacy of Rabies vaccine can be decreased when used in combination with Tacrolimus.Approved
RacecadotrilThe metabolism of Tacrolimus can be decreased when combined with Racecadotril.Investigational
RadicicolThe metabolism of Tacrolimus can be decreased when combined with Radicicol.Experimental
RamiprilThe metabolism of Tacrolimus can be decreased when combined with Ramipril.Approved
RanitidineThe serum concentration of Ranitidine can be decreased when it is combined with Tacrolimus.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Tacrolimus.Approved, Investigational
ReboxetineThe serum concentration of Tacrolimus can be increased when it is combined with Reboxetine.Approved, Investigational
RegorafenibThe serum concentration of Tacrolimus can be increased when it is combined with Regorafenib.Approved
RemikirenThe metabolism of Tacrolimus can be decreased when combined with Remikiren.Approved
RepaglinideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Tacrolimus.Approved, Investigational
ReserpineThe serum concentration of Tacrolimus can be decreased when it is combined with Reserpine.Approved
ResveratrolResveratrol may increase the nephrotoxic activities of Tacrolimus.Experimental, Investigational
RifabutinThe metabolism of Tacrolimus can be increased when combined with Rifabutin.Approved
RifabutinThe serum concentration of Tacrolimus can be decreased when it is combined with Rifabutin.Approved
RifampicinThe metabolism of Tacrolimus can be increased when combined with Rifampicin.Approved
RifampicinThe serum concentration of Tacrolimus can be decreased when it is combined with Rifampicin.Approved
RifapentineThe metabolism of Tacrolimus can be increased when combined with Rifapentine.Approved
RifapentineThe serum concentration of Tacrolimus can be decreased when it is combined with Rifapentine.Approved
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Tacrolimus.Approved, Investigational
RilonaceptThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Rilonacept.Approved
RilpivirineThe serum concentration of Tacrolimus can be increased when it is combined with Rilpivirine.Approved
RisperidoneThe serum concentration of Risperidone can be decreased when it is combined with Tacrolimus.Approved, Investigational
RitonavirThe metabolism of Tacrolimus can be decreased when combined with Ritonavir.Approved, Investigational
RitonavirThe serum concentration of Tacrolimus can be increased when it is combined with Ritonavir.Approved, Investigational
RituximabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Rituximab.Approved
RivaroxabanThe metabolism of Tacrolimus can be decreased when combined with Rivaroxaban.Approved
RivaroxabanThe serum concentration of Rivaroxaban can be decreased when it is combined with Tacrolimus.Approved
RofecoxibRofecoxib may increase the nephrotoxic activities of Tacrolimus.Investigational, Withdrawn
RoflumilastRoflumilast may increase the immunosuppressive activities of Tacrolimus.Approved
RolapitantThe serum concentration of Tacrolimus can be increased when it is combined with Rolapitant.Approved
RomidepsinThe serum concentration of Romidepsin can be decreased when it is combined with Tacrolimus.Approved, Investigational
RosiglitazoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Tacrolimus.Approved, Investigational
RuxolitinibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Ruxolitinib.Approved
SalicylamideSalicylamide may increase the nephrotoxic activities of Tacrolimus.Approved
Salicylhydroxamic AcidThe metabolism of Tacrolimus can be decreased when combined with Salicylhydroxamic Acid.Experimental
Salicylic acidThe metabolism of Tacrolimus can be decreased when combined with Salicylic acid.Approved, Vet Approved
Salicylic acidThe serum concentration of Salicylic acid can be decreased when it is combined with Tacrolimus.Approved, Vet Approved
Salicylic acidSalicylic acid may increase the nephrotoxic activities of Tacrolimus.Approved, Vet Approved
SalsalateSalsalate may increase the nephrotoxic activities of Tacrolimus.Approved
SaquinavirThe metabolism of Tacrolimus can be decreased when combined with Saquinavir.Approved, Investigational
SaxagliptinThe metabolism of Tacrolimus can be decreased when combined with Saxagliptin.Approved
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Tacrolimus.Approved
ScopolamineThe serum concentration of Tacrolimus can be increased when it is combined with Scopolamine.Approved
SecukinumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Secukinumab.Approved
SelegilineThe serum concentration of Tacrolimus can be increased when it is combined with Selegiline.Approved, Investigational, Vet Approved
SelexipagThe serum concentration of Selexipag can be decreased when it is combined with Tacrolimus.Approved
SeocalcitolThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Seocalcitol.Experimental
SeratrodastSeratrodast may increase the nephrotoxic activities of Tacrolimus.Approved, Investigational
SertaconazoleThe metabolism of Tacrolimus can be decreased when combined with Sertaconazole.Approved
SertralineThe metabolism of Tacrolimus can be decreased when combined with Sertraline.Approved
SertralineThe serum concentration of Tacrolimus can be increased when it is combined with Sertraline.Approved
SevelamerThe serum concentration of Tacrolimus can be decreased when it is combined with Sevelamer.Approved
SildenafilThe metabolism of Tacrolimus can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Tacrolimus.Approved
SiltuximabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Siltuximab.Approved
SiltuximabThe serum concentration of Tacrolimus can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe metabolism of Tacrolimus can be decreased when combined with Simeprevir.Approved
SimeprevirThe serum concentration of Tacrolimus can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Tacrolimus can be increased when it is combined with Simvastatin.Approved
SinefunginThe metabolism of Tacrolimus can be decreased when combined with Sinefungin.Experimental
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Tacrolimus.Approved
SirolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Sirolimus.Approved, Investigational
SirolimusThe serum concentration of Tacrolimus can be decreased when it is combined with Sirolimus.Approved, Investigational
SitagliptinThe metabolism of Tacrolimus can be decreased when combined with Sitagliptin.Approved, Investigational
SitagliptinThe serum concentration of Sitagliptin can be decreased when it is combined with Tacrolimus.Approved, Investigational
SofosbuvirThe serum concentration of Sofosbuvir can be decreased when it is combined with Tacrolimus.Approved
SolithromycinThe serum concentration of Tacrolimus can be increased when it is combined with Solithromycin.Investigational
SorafenibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Sorafenib.Approved, Investigational
SorafenibThe serum concentration of Sorafenib can be decreased when it is combined with Tacrolimus.Approved, Investigational
SparfloxacinThe serum concentration of Sparfloxacin can be decreased when it is combined with Tacrolimus.Approved
SphingosineThe serum concentration of Sphingosine can be decreased when it is combined with Tacrolimus.Experimental
SpiraprilThe metabolism of Tacrolimus can be decreased when combined with Spirapril.Approved
SpironolactoneSpironolactone may increase the hyperkalemic activities of Tacrolimus.Approved
SpironolactoneThe serum concentration of Tacrolimus can be increased when it is combined with Spironolactone.Approved
SRP 299The risk or severity of adverse effects can be increased when Tacrolimus is combined with SRP 299.Investigational
SRT501SRT501 may increase the nephrotoxic activities of Tacrolimus.Investigational
St. John's WortThe serum concentration of Tacrolimus can be decreased when it is combined with St. John's Wort.Nutraceutical
StaurosporineThe serum concentration of Tacrolimus can be increased when it is combined with Staurosporine.Experimental
SteproninThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Stepronin.Approved
StiripentolThe serum concentration of Tacrolimus can be increased when it is combined with Stiripentol.Approved
StreptozocinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Streptozocin.Approved
StreptozocinThe serum concentration of Tacrolimus can be decreased when it is combined with Streptozocin.Approved
SulconazoleThe metabolism of Tacrolimus can be decreased when combined with Sulconazole.Approved
SulfasalazineSulfasalazine may increase the nephrotoxic activities of Tacrolimus.Approved
SulfinpyrazoneThe serum concentration of Tacrolimus can be increased when it is combined with Sulfinpyrazone.Approved
SulfisoxazoleThe metabolism of Tacrolimus can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulindacSulindac may increase the nephrotoxic activities of Tacrolimus.Approved
SulodexideThe therapeutic efficacy of Sulodexide can be decreased when used in combination with Tacrolimus.Approved, Investigational
SumatriptanThe serum concentration of Tacrolimus can be increased when it is combined with Sumatriptan.Approved, Investigational
SunitinibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Sunitinib.Approved, Investigational
SunitinibThe serum concentration of Tacrolimus can be increased when it is combined with Sunitinib.Approved, Investigational
SuprofenSuprofen may increase the nephrotoxic activities of Tacrolimus.Approved, Withdrawn
TacrineThe serum concentration of Tacrolimus can be increased when it is combined with Tacrine.Withdrawn
TAK-390MRThe serum concentration of Tacrolimus can be increased when it is combined with TAK-390MR.Investigational
TamoxifenThe serum concentration of Tamoxifen can be decreased when it is combined with Tacrolimus.Approved
Taurocholic AcidThe serum concentration of Taurocholic Acid can be decreased when it is combined with Tacrolimus.Experimental
TavaboroleThe metabolism of Tacrolimus can be decreased when combined with Tavaborole.Approved
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be decreased when it is combined with Tacrolimus.Approved
TelaprevirThe metabolism of Tacrolimus can be decreased when combined with Telaprevir.Approved
TelaprevirThe serum concentration of Tacrolimus can be increased when it is combined with Telaprevir.Approved
TelithromycinThe metabolism of Tacrolimus can be decreased when combined with Telithromycin.Approved
TelithromycinThe serum concentration of Tacrolimus can be increased when it is combined with Telithromycin.Approved
TelmisartanThe serum concentration of Tacrolimus can be increased when it is combined with Telmisartan.Approved, Investigational
TemocaprilThe metabolism of Tacrolimus can be decreased when combined with Temocapril.Experimental, Investigational
TemozolomideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Temozolomide.Approved, Investigational
TemsirolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Temsirolimus.Approved
TemsirolimusThe serum concentration of Temsirolimus can be decreased when it is combined with Tacrolimus.Approved
TeniposideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Teniposide.Approved
TenoxicamTenoxicam may increase the nephrotoxic activities of Tacrolimus.Approved
TepoxalinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Tepoxalin.Vet Approved
TepoxalinTepoxalin may increase the nephrotoxic activities of Tacrolimus.Vet Approved
TerazosinThe serum concentration of Tacrolimus can be increased when it is combined with Terazosin.Approved
TerbinafineThe metabolism of Tacrolimus can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TerconazoleThe metabolism of Tacrolimus can be decreased when combined with Terconazole.Approved
TerfenadineThe serum concentration of Tacrolimus can be increased when it is combined with Terfenadine.Withdrawn
TeriflunomideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Teriflunomide.Approved
TeriflunomideTeriflunomide may increase the nephrotoxic activities of Tacrolimus.Approved
TesmilifeneThe serum concentration of Tacrolimus can be decreased when it is combined with Tesmilifene.Investigational
TestosteroneThe serum concentration of Tacrolimus can be increased when it is combined with Testosterone.Approved, Investigational
TG4010The risk or severity of adverse effects can be increased when Tacrolimus is combined with TG4010.Investigational
ThalidomideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Thalidomide.Approved, Investigational, Withdrawn
ThiazolidinedioneThe therapeutic efficacy of Thiazolidinedione can be decreased when used in combination with Tacrolimus.Investigational
ThiorphanThe metabolism of Tacrolimus can be decreased when combined with Thiorphan.Experimental
ThiotepaThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Thiotepa.Approved
ThymolThe metabolism of Tacrolimus can be decreased when combined with Thymol.Approved
Tiaprofenic acidTiaprofenic acid may increase the nephrotoxic activities of Tacrolimus.Approved
TicagrelorThe serum concentration of Ticagrelor can be decreased when it is combined with Tacrolimus.Approved
TiclopidineThe metabolism of Tacrolimus can be decreased when combined with Ticlopidine.Approved
TimololThe serum concentration of Timolol can be decreased when it is combined with Tacrolimus.Approved
TinoridineTinoridine may increase the nephrotoxic activities of Tacrolimus.Investigational
TioconazoleThe metabolism of Tacrolimus can be decreased when combined with Tioconazole.Approved
TioguanineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Tioguanine.Approved
TipranavirThe metabolism of Tacrolimus can be decreased when combined with Tipranavir.Approved, Investigational
TocilizumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Tocilizumab.Approved
TocilizumabThe serum concentration of Tacrolimus can be decreased when it is combined with Tocilizumab.Approved
TofacitinibTacrolimus may increase the immunosuppressive activities of Tofacitinib.Approved, Investigational
TofacitinibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Tofacitinib.Approved, Investigational
TolazamideThe therapeutic efficacy of Tolazamide can be decreased when used in combination with Tacrolimus.Approved
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Tacrolimus.Approved
Tolfenamic AcidTolfenamic Acid may increase the nephrotoxic activities of Tacrolimus.Approved
TolmetinTolmetin may increase the nephrotoxic activities of Tacrolimus.Approved
TolnaftateThe metabolism of Tacrolimus can be decreased when combined with Tolnaftate.Approved, Vet Approved
TolvaptanThe serum concentration of Tolvaptan can be decreased when it is combined with Tacrolimus.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Tacrolimus.Approved, Investigational
TopotecanThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Topotecan.Approved, Investigational
ToremifeneThe serum concentration of Toremifene can be decreased when it is combined with Tacrolimus.Approved, Investigational
TositumomabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Tositumomab.Approved
TrabectedinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Trabectedin.Approved, Investigational
TrandolaprilThe metabolism of Tacrolimus can be decreased when combined with Trandolapril.Approved
TranilastTranilast may increase the nephrotoxic activities of Tacrolimus.Approved, Investigational
TrastuzumabTrastuzumab may increase the neutropenic activities of Tacrolimus.Approved, Investigational
Trastuzumab emtansineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Trastuzumab emtansine.Approved
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Tacrolimus.Approved
TrazodoneThe metabolism of Tacrolimus can be decreased when combined with Trazodone.Approved, Investigational
TrazodoneThe serum concentration of Tacrolimus can be decreased when it is combined with Trazodone.Approved, Investigational
TretinoinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Tretinoin.Approved, Investigational, Nutraceutical
TriamcinoloneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Triamcinolone.Approved, Vet Approved
TriamtereneTriamterene may increase the hyperkalemic activities of Tacrolimus.Approved
TrifluoperazineThe serum concentration of Tacrolimus can be increased when it is combined with Trifluoperazine.Approved
TriflupromazineThe serum concentration of Tacrolimus can be increased when it is combined with Triflupromazine.Approved, Vet Approved
TrimethoprimThe serum concentration of Tacrolimus can be decreased when it is combined with Trimethoprim.Approved, Vet Approved
TrimetrexateThe metabolism of Tacrolimus can be decreased when combined with Trimetrexate.Approved, Investigational
TrimipramineThe serum concentration of Tacrolimus can be increased when it is combined with Trimipramine.Approved
Trisalicylate-cholineTrisalicylate-choline may increase the nephrotoxic activities of Tacrolimus.Approved
TrofosfamideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Trofosfamide.Investigational
TroglitazoneThe therapeutic efficacy of Troglitazone can be decreased when used in combination with Tacrolimus.Withdrawn
TroleandomycinThe serum concentration of Tacrolimus can be increased when it is combined with Troleandomycin.Approved
TylosinThe serum concentration of Tacrolimus can be increased when it is combined with Tylosin.Vet Approved
UbenimexThe metabolism of Tacrolimus can be decreased when combined with Ubenimex.Experimental
UlinastatinThe metabolism of Tacrolimus can be decreased when combined with Ulinastatin.Investigational
UlipristalThe serum concentration of Ulipristal can be decreased when it is combined with Tacrolimus.Approved
UmeclidiniumThe serum concentration of Umeclidinium can be decreased when it is combined with Tacrolimus.Approved
UstekinumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Ustekinumab.Approved, Investigational
ValdecoxibValdecoxib may increase the nephrotoxic activities of Tacrolimus.Investigational, Withdrawn
VecuroniumThe serum concentration of Vecuronium can be decreased when it is combined with Tacrolimus.Approved
VedolizumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Vedolizumab.Approved
VenetoclaxThe serum concentration of Venetoclax can be decreased when it is combined with Tacrolimus.Approved
VenlafaxineThe metabolism of Tacrolimus can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Tacrolimus can be decreased when combined with Verapamil.Approved
VilanterolThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Vilanterol.Approved
VilazodoneThe metabolism of Tacrolimus can be decreased when combined with Vilazodone.Approved
VildagliptinThe metabolism of Tacrolimus can be decreased when combined with Vildagliptin.Approved, Investigational
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Tacrolimus.Approved, Investigational
VinblastineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Vinblastine.Approved
VinblastineThe serum concentration of Vinblastine can be decreased when it is combined with Tacrolimus.Approved
VincristineThe serum concentration of Vincristine can be decreased when it is combined with Tacrolimus.Approved, Investigational
VincristineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Vincristine.Approved, Investigational
VindesineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Vindesine.Approved
VinorelbineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Vinorelbine.Approved, Investigational
VinorelbineThe serum concentration of Tacrolimus can be increased when it is combined with Vinorelbine.Approved, Investigational
VismodegibThe serum concentration of Vismodegib can be decreased when it is combined with Tacrolimus.Approved
VogliboseThe therapeutic efficacy of Voglibose can be decreased when used in combination with Tacrolimus.Approved, Investigational
VoriconazoleThe metabolism of Tacrolimus can be decreased when combined with Voriconazole.Approved, Investigational
VoriconazoleThe serum concentration of Tacrolimus can be increased when it is combined with Voriconazole.Approved, Investigational
VortioxetineThe metabolism of Tacrolimus can be decreased when combined with Vortioxetine.Approved
XimelagatranThe metabolism of Tacrolimus can be decreased when combined with Ximelagatran.Approved, Investigational, Withdrawn
Ym150The metabolism of Tacrolimus can be decreased when combined with Ym150.Investigational
ZaltoprofenZaltoprofen may increase the nephrotoxic activities of Tacrolimus.Approved
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Tacrolimus.Approved
ZileutonZileuton may increase the nephrotoxic activities of Tacrolimus.Approved, Investigational, Withdrawn
ZimelidineThe metabolism of Tacrolimus can be decreased when combined with Zimelidine.Withdrawn
ZimelidineThe serum concentration of Tacrolimus can be increased when it is combined with Zimelidine.Withdrawn
ZiprasidoneThe metabolism of Tacrolimus can be decreased when combined with Ziprasidone.Approved
ZomepiracZomepirac 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
  1. 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 ]
  2. 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 ]
  3. 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 ]
  4. 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 ]
  5. 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
ATC CodesD11AH01L04AD02
AHFS Codes
  • 84:92.00
  • 92:00.00
PDB Entries
FDA labelDownload (144 KB)
MSDSDownload (54.9 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption-0.8264
Blood Brain Barrier-0.9659
Caco-2 permeable-0.5977
P-glycoprotein substrateSubstrate0.7862
P-glycoprotein inhibitor IInhibitor0.8687
P-glycoprotein inhibitor IIInhibitor0.7974
Renal organic cation transporterNon-inhibitor0.8135
CYP450 2C9 substrateNon-substrate0.9116
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.7435
CYP450 1A2 substrateNon-inhibitor0.8874
CYP450 2C9 inhibitorNon-inhibitor0.9053
CYP450 2D6 inhibitorNon-inhibitor0.9402
CYP450 2C19 inhibitorNon-inhibitor0.8969
CYP450 3A4 inhibitorNon-inhibitor0.869
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9807
Ames testNon AMES toxic0.6355
CarcinogenicityNon-carcinogens0.9422
BiodegradationNot ready biodegradable0.9698
Rat acute toxicity2.7541 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9817
hERG inhibition (predictor II)Non-inhibitor0.8733
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Astellas pharma us inc
  • Dr reddys laboratories ltd
  • Sandoz inc
  • Watson laboratories inc
  • Astellas Pharma US
Packagers
Dosage forms
FormRouteStrength
Capsule, extended releaseOral0.5 mg
Capsule, extended releaseOral1 mg
Capsule, extended releaseOral3 mg
Capsule, extended releaseOral5 mg
Capsule, coated, extended releaseOral.5 mg/1
Capsule, coated, extended releaseOral1 mg/1
Capsule, coated, extended releaseOral5 mg/1
Tablet, extended releaseOral0.75 mg
Tablet, extended releaseOral1 mg
Tablet, extended releaseOral4 mg
Tablet, extended releaseOral.75 mg/1
Tablet, extended releaseOral1 mg/1
Tablet, extended releaseOral4 mg/1
CapsuleOral.5 mg/1
CapsuleOral1 mg/1
CapsuleOral5 mg/1
GranuleOral0.2 mg
GranuleOral1 mg
CapsuleOral0.5 mg
CapsuleOral1 mg
CapsuleOral5 mg
Capsule, gelatin coatedOral.5 mg/1
Capsule, gelatin coatedOral1 mg/1
Capsule, gelatin coatedOral5 mg/1
Injection, solutionIntravenous5 mg/mL
SolutionIntravenous5 mg
OintmentCutaneous0.03 %
OintmentCutaneous0.1 %
OintmentTopical0.03 %
OintmentTopical0.1 %
OintmentTopical.3 mg/g
OintmentTopical1 mg/g
Prices
Unit descriptionCostUnit
Tacrolimus micronized powder2800.0USD g
Protopic 0.1% Ointment 60 gm Tube255.34USD tube
Protopic 0.03% Ointment 60 gm Tube251.17USD tube
Prograf 5 mg/ml ampule163.94USD ml
Protopic 0.03% Ointment 30 gm Tube132.99USD tube
Protopic 0.1% Ointment 30 gm Tube124.42USD tube
Prograf 5 mg capsule24.26USD capsule
Tacrolimus anhydrous 5 mg cap22.3USD each
Prograf 1 mg capsule4.85USD capsule
Tacrolimus 1 mg capsule4.64USD capsule
Tacrolimus anhydrous 1 mg cap4.46USD each
Protopic 0.1% ointment4.17USD g
Protopic 0.03% ointment4.09USD g
Prograf 0.5 mg capsule2.43USD capsule
Tacrolimus anhydrous 0.5 mg cap2.23USD each
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1338491 No1996-07-302013-07-30Canada
CA2037408 No2002-12-172011-03-01Canada
US5260301 No1994-02-282011-02-28Us
US5665727 No1994-09-092014-09-09Us
US6440458 No1999-03-252019-03-25Us
US6576259 No1999-03-252019-03-25Us
US6884433 No1999-03-252019-03-25Us
US7994214 No2004-08-302024-08-30Us
US8486993 No2004-08-302024-08-30Us
US8551522 No1999-03-252019-03-25Us
US8586084 No2004-08-302024-08-30Us
US8591946 No2004-08-302024-08-30Us
US8617599 No2004-08-302024-08-30Us
US8623410 No2004-08-302024-08-30Us
US8623411 No2004-08-302024-08-30Us
US8664239 No2008-05-302028-05-30Us
US8685998 No2008-05-302028-05-30Us
US8889185 No2004-08-302024-08-30Us
US8889186 No2004-08-302024-08-30Us
US9161907 No2004-08-302024-08-30Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point126 °CNot Available
water solubilityInsolubleFDA label
logP3.3Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00402 mg/mLALOGPS
logP3.19ALOGPS
logP5.59ChemAxon
logS-5.3ALOGPS
pKa (Strongest Acidic)9.96ChemAxon
pKa (Strongest Basic)-2.9ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count11ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area178.36 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity215.62 m3·mol-1ChemAxon
Polarizability87.41 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassPhenylpropanoids and polyketides
ClassMacrolide lactams
Sub ClassNot Available
Direct ParentMacrolide lactams
Alternative Parents
Substituents
  • Macrolide lactam
  • Macrolide
  • Alpha-amino acid ester
  • Cyclohexanol
  • Piperidine
  • Oxane
  • Tertiary carboxylic acid amide
  • Cyclic alcohol
  • Cyclic ketone
  • Tertiary amine
  • Secondary alcohol
  • Lactone
  • Lactam
  • Ketone
  • Hemiacetal
  • Carboxylic acid ester
  • Carboxamide group
  • Oxacycle
  • Azacycle
  • Organoheterocyclic compound
  • Monocarboxylic acid or derivatives
  • Ether
  • Dialkyl ether
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Alcohol
  • Aliphatic heteropolycyclic compound
Molecular FrameworkAliphatic heteropolycyclic compounds
External Descriptors

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 prevents the association of SMAD2 and SMAD3 with the activin receptor complex, thereby blocking the activin signal. May modulate the RYR1 calcium channel activity. PPIases accelerate the folding of proteins....
Gene Name:
FKBP1A
Uniprot ID:
P62942
Molecular Weight:
11950.665 Da
References
  1. 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 ]
  2. 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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. 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 ]
  2. 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 ]
  3. 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 unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. 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 ]
  2. 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 unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. 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 colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
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 the body. Appears to function in modulating the activity of the immune system during the acute-phase reaction.
Gene Name:
ORM1
Uniprot ID:
P02763
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
Molecular Weight:
141477.255 Da
References
  1. 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 ]
  2. 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 ]
  3. 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 ]
  4. 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 ]
  5. 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 ]
  6. 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
Molecular Weight:
186505.825 Da
References
  1. 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 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on December 09, 2016 02:41