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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-tacrolimuscapsule (immediate release)0.5 mgoralAccord Healthcare IncNot applicableNot applicableCanada
Ach-tacrolimuscapsule (immediate release)1 mgoralAccord Healthcare IncNot applicableNot applicableCanada
Ach-tacrolimuscapsule (immediate release)5 mgoralAccord Healthcare IncNot applicableNot applicableCanada
AdvagrafProlonged release hard capsules1 mgOral useAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafProlonged release hard capsules1 mgOral useAstellas Pharma Europe B.V.2007-04-23Not applicableEu
Advagrafcapsule (extended release)1 mgoralAstellas Pharma Canada Inc2008-04-09Not applicableCanada
AdvagrafProlonged release hard capsules5 mgOral useAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafProlonged release hard capsules3 mgOral useAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafProlonged release hard capsules5 mgOral useAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafProlonged release hard capsules3 mgOral useAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafProlonged release hard capsules0.5 mgOral useAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafProlonged release hard capsules1 mgOral useAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafProlonged release hard capsules1 mgOral useAstellas Pharma Europe B.V.2007-04-23Not applicableEu
Advagrafcapsule (extended release)5 mgoralAstellas Pharma Canada Inc2008-04-09Not applicableCanada
AdvagrafProlonged release hard capsules3 mgOral useAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafProlonged release hard capsules5 mgOral useAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafProlonged release hard capsules3 mgOral useAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafProlonged release hard capsules0.5 mgOral useAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafProlonged release hard capsules0.5 mgOral useAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafProlonged release hard capsules1 mgOral useAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafProlonged release hard capsules1 mgOral useAstellas Pharma Europe B.V.2007-04-23Not applicableEu
Advagrafcapsule (extended release)3 mgoralAstellas Pharma Canada Inc2010-04-05Not applicableCanada
AdvagrafProlonged release hard capsules3 mgOral useAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafProlonged release hard capsules0.5 mgOral useAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafProlonged release hard capsules5 mgOral useAstellas Pharma Europe B.V.2007-04-23Not applicableEu
Advagrafcapsule (extended release)0.5 mgoralAstellas Pharma Canada Inc2008-04-09Not applicableCanada
AdvagrafProlonged release hard capsules0.5 mgOral useAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafProlonged release hard capsules1 mgOral useAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafProlonged release hard capsules1 mgOral useAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafProlonged release hard capsules3 mgOral useAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafProlonged release hard capsules0.5 mgOral useAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafProlonged release hard capsules5 mgOral useAstellas Pharma Europe B.V.2007-04-23Not applicableEu
AdvagrafProlonged release hard capsules5 mgOral useAstellas 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
EnvarsusProlonged-release tablet4 mgOral useChiesi Farmaceutici S.P.A.2014-07-18Not applicableEu
EnvarsusProlonged-release tablet1 mgOral useChiesi Farmaceutici S.P.A.2014-07-18Not applicableEu
EnvarsusProlonged-release tablet4 mgOral useChiesi Farmaceutici S.P.A.2014-07-18Not applicableEu
EnvarsusProlonged-release tablet0.75 mgOral useChiesi Farmaceutici S.P.A.2014-07-18Not applicableEu
EnvarsusProlonged-release tablet1 mgOral useChiesi Farmaceutici S.P.A.2014-07-18Not applicableEu
EnvarsusProlonged-release tablet4 mgOral useChiesi Farmaceutici S.P.A.2014-07-18Not applicableEu
EnvarsusProlonged-release tablet0.75 mgOral useChiesi Farmaceutici S.P.A.2014-07-18Not applicableEu
EnvarsusProlonged-release tablet1 mgOral useChiesi Farmaceutici S.P.A.2014-07-18Not applicableEu
EnvarsusProlonged-release tablet0.75 mgOral useChiesi 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
ModigrafGranules for oral suspension1 mgOral useAstellas Pharma Europe B.V.2009-05-15Not applicableEu
ModigrafGranules for oral suspension0.2 mgOral useAstellas 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
Prografcapsule, gelatin coated5 mg/1oralAstellas Pharma US, Inc.1994-04-08Not applicableUs
Prografcapsule1 mgoralAstellas Pharma Canada Inc1996-08-14Not applicableCanada
Prografcapsule, gelatin coated1 mg/1oralRebel Distributors Corp1994-04-08Not applicableUs
Protopicointment.3 mg/gtopicalAstellas Pharma US Inc.2000-12-08Not applicableUs
Protopicointment0.03 %topicalLeo Pharma Inc2001-09-06Not applicableCanada
Protopicointment1 mg/gtopicalAstellas Pharma US Inc.2000-12-08Not applicableUs
Protopicointment1 mg/gtopicalPhysicians Total Care, Inc.2008-05-08Not applicableUs
Protopicointment0.1 %topicalLeo Pharma Inc2001-09-06Not applicableCanada
Ran-tacrolimuscapsule (immediate release)5 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada
Sandoz Tacrolimuscapsule (immediate release)1 mgoralSandoz Canada Incorporated2013-11-25Not applicableCanada
Sandoz Tacrolimuscapsule (immediate release)5 mgoralSandoz Canada Incorporated2013-11-25Not applicableCanada
Sandoz Tacrolimuscapsule (immediate release)0.5 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/1oralStrides Arcolab Limited2014-08-13Not applicableUs
Tacrolimuscapsule1 mg/1oralMylan Pharmaceuticals Inc.2012-07-23Not applicableUs
Tacrolimuscapsule5 mg/1oralIngenus Pharmaceuticals, LLC2012-09-28Not applicableUs
Tacrolimuscapsule.5 mg/1oralCardinal Health2011-06-15Not applicableUs
Tacrolimuscapsule5 mg/1oralGolden State Medical Supply, Inc.2015-11-18Not applicableUs
Tacrolimuscapsule5 mg/1oralSandoz Inc2012-01-15Not applicableUs
Tacrolimuscapsule.5 mg/1oralDr. Reddy's Laboratories Limited2010-05-14Not applicableUs
Tacrolimuscapsule1 mg/1oralAmerican Health Packaging2013-07-17Not applicableUs
Tacrolimuscapsule1 mg/1oralSandoz Inc2009-08-10Not applicableUs
Tacrolimusointment.3 mg/gtopicalE. Fougera & Co. a division of Fougera Pharmaceuticals Inc.2014-09-09Not applicableUs
Tacrolimuscapsule5 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
Tacrolimuscapsule1 mg/1oralStrides Arcolab Limited2014-08-13Not applicableUs
Tacrolimuscapsule5 mg/1oralMylan Pharmaceuticals Inc.2012-07-23Not applicableUs
Tacrolimuscapsule5 mg/1oralMylan Institutional Inc.2010-11-01Not applicableUs
Tacrolimuscapsule1 mg/1oralCardinal Health2013-07-17Not applicableUs
Tacrolimuscapsule, gelatin coated.5 mg/1oralBion Pharma Inc.,2016-02-26Not applicableUs
Tacrolimuscapsule1 mg/1oralMajor Pharmaceuticals2015-01-05Not applicableUs
Tacrolimuscapsule5 mg/1oralSandoz Inc2009-08-10Not applicableUs
Tacrolimuscapsule1 mg/1oralDr. Reddy's Laboratories Limited2010-05-14Not applicableUs
Tacrolimuscapsule5 mg/1oralAmerican Health Packaging2013-07-17Not applicableUs
Tacrolimuscapsule1 mg/1oralKAISER FOUNDATION HOSPITALS2010-12-10Not applicableUs
Tacrolimuscapsule.5 mg/1oralIngenus Pharmaceuticals, LLC2012-09-28Not applicableUs
Tacrolimuscapsule, gelatin coated5 mg/1oralKremers Urban Pharmaceuticals Inc.2015-07-30Not applicableUs
Tacrolimuscapsule5 mg/1oralStrides Arcolab Limited2014-08-13Not applicableUs
Tacrolimuscapsule5 mg/1oralWatson Laboratories, Inc.2010-07-06Not applicableUs
Tacrolimuscapsule.5 mg/1oralMylan Institutional Inc.2010-11-15Not applicableUs
Tacrolimuscapsule1 mg/1oralCardinal Health2009-08-10Not applicableUs
Tacrolimuscapsule, gelatin coated1 mg/1oralBion Pharma Inc.,2016-02-26Not applicableUs
Tacrolimuscapsule.5 mg/1oralAccord Healthcare Inc.2011-08-31Not applicableUs
Tacrolimuscapsule.5 mg/1oralSandoz Inc2012-01-15Not applicableUs
Tacrolimuscapsule5 mg/1oralDr. Reddy's Laboratories Limited2010-05-14Not applicableUs
Tacrolimuscapsule.5 mg/1oralGolden State Medical Supply, Inc.2015-11-18Not applicableUs
Tacrolimuscapsule.5 mg/1oralMylan Pharmaceuticals Inc.2012-07-23Not applicableUs
Tacrolimuscapsule1 mg/1oralIngenus Pharmaceuticals, LLC2012-09-28Not applicableUs
Tacrolimuscapsule, gelatin coated1 mg/1oralbryant ranch prepack2012-10-30Not applicableUs
Tacrolimuscapsule.5 mg/1oralAmerican Health Packaging2013-07-17Not applicableUs
Tacrolimuscapsule.5 mg/1oralSandoz Inc2009-08-10Not applicableUs
Tacrolimuscapsule1 mg/1oralMylan Institutional Inc.2010-11-01Not 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
Tacrolimusointment1 mg/gtopicalE. Fougera & Co. a division of Fougera Pharmaceuticals Inc.2014-09-09Not applicableUs
Tacrolimuscapsule1 mg/1oralAccord Healthcare Inc.2011-08-31Not applicableUs
Tacrolimuscapsule1 mg/1oralSandoz Inc2012-01-15Not applicableUs
Tacrolimuscapsule1 mg/1oralCardinal Health2011-06-15Not applicableUs
Tacrolimuscapsule1 mg/1oralGolden State Medical Supply, Inc.2015-11-18Not 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 KeyInChIKey=QJJXYPPXXYFBGM-LFZNUXCKSA-N
InChI
InChI=1S/C44H69NO12/c1-10-13-31-19-25(2)18-26(3)20-37(54-8)40-38(55-9)22-28(5)44(52,57-40)41(49)42(50)45-17-12-11-14-32(45)43(51)56-39(29(6)34(47)24-35(31)48)27(4)21-30-15-16-33(46)36(23-30)53-7/h10,19,21,26,28-34,36-40,46-47,52H,1,11-18,20,22-24H2,2-9H3/b25-19+,27-21+/t26-,28+,29+,30-,31+,32-,33+,34-,36+,37-,38-,39+,40+,44+/m0/s1
IUPAC Name
(1R,9S,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-1,14-dihydroxy-12-[(1E)-1-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-17-(prop-2-en-1-yl)-11,28-dioxa-4-azatricyclo[22.3.1.0⁴,⁹]octacos-18-ene-2,3,10,16-tetrone
SMILES
CO[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
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
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.
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.
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
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 release)oral0.5 mg
Capsule (extended release)oral1 mg
Capsule (extended release)oral3 mg
Capsule (extended release)oral5 mg
Prolonged release hard capsulesOral use0.5 mg
Prolonged release hard capsulesOral use1 mg
Prolonged release hard capsulesOral use3 mg
Prolonged release hard capsulesOral use5 mg
Capsule, coated, extended releaseoral.5 mg/1
Capsule, coated, extended releaseoral1 mg/1
Capsule, coated, extended releaseoral5 mg/1
Prolonged-release tabletOral use0.75 mg
Prolonged-release tabletOral use1 mg
Prolonged-release tabletOral use4 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
Granules for oral suspensionOral use0.2 mg
Granules for oral suspensionOral use1 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
Ointmenttopical0.03 %
Ointmenttopical0.1 %
Capsule (immediate release)oral0.5 mg
Capsule (immediate release)oral1 mg
Capsule (immediate release)oral5 mg
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
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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
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)
Interactions
Drug Interactions
Drug
1,10-PhenanthrolineThe metabolism of Tacrolimus can be decreased when combined with 1,10-Phenanthroline.
2-HYDROXY-1,4-NAPHTHOQUINONEThe metabolism of Tacrolimus can be decreased when combined with 2-HYDROXY-1,4-NAPHTHOQUINONE.
2-mercaptobenzothiazoleThe metabolism of Tacrolimus can be decreased when combined with 2-mercaptobenzothiazole.
2-MethoxyethanolThe risk or severity of adverse effects can be increased when Tacrolimus is combined with 2-Methoxyethanol.
3,4-DichloroisocoumarinThe metabolism of Tacrolimus can be decreased when combined with 3,4-Dichloroisocoumarin.
4-(2-AMINOETHYL)BENZENESULFONYL FLUORIDEThe metabolism of Tacrolimus can be decreased when combined with 4-(2-AMINOETHYL)BENZENESULFONYL FLUORIDE.
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.
AbataceptThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Abatacept.
abetimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with abetimus.
ABR-215757The risk or severity of adverse effects can be increased when Tacrolimus is combined with ABR-215757.
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Tacrolimus.
AcebutololThe serum concentration of Acebutolol can be decreased when it is combined with Tacrolimus.
AceclofenacAceclofenac may increase the nephrotoxic activities of Tacrolimus.
AcetaminophenThe serum concentration of Acetaminophen can be decreased when it is combined with Tacrolimus.
AcetaminophenThe serum concentration of Tacrolimus can be increased when it is combined with Acetaminophen.
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Tacrolimus.
Acetylsalicylic acidAcetylsalicylic acid may increase the nephrotoxic activities of Tacrolimus.
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be decreased when it is combined with Tacrolimus.
AdalimumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Adalimumab.
AdapaleneAdapalene may increase the nephrotoxic activities of Tacrolimus.
AfatinibThe serum concentration of Afatinib can be decreased when it is combined with Tacrolimus.
AfatinibThe serum concentration of Tacrolimus can be increased when it is combined with Afatinib.
AfelimomabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Afelimomab.
AicarThe therapeutic efficacy of Aicar can be decreased when used in combination with Tacrolimus.
AlbendazoleThe serum concentration of Tacrolimus can be increased when it is combined with Albendazole.
AldosteroneThe serum concentration of Tacrolimus can be decreased when it is combined with Aldosterone.
AlectinibThe serum concentration of Tacrolimus can be increased when it is combined with Alectinib.
AlefaceptThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Alefacept.
AlemtuzumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Alemtuzumab.
AlfentanilThe serum concentration of Tacrolimus can be increased when it is combined with Alfentanil.
alicaforsenThe risk or severity of adverse effects can be increased when Tacrolimus is combined with alicaforsen.
AlitretinoinThe serum concentration of Alitretinoin can be decreased when it is combined with Tacrolimus.
AlogliptinThe metabolism of Tacrolimus can be decreased when combined with Alogliptin.
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Tacrolimus.
Alpha-1-proteinase inhibitorThe metabolism of Tacrolimus can be decreased when combined with Alpha-1-proteinase inhibitor.
AltretamineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Altretamine.
AmantadineThe serum concentration of Tacrolimus can be increased when it is combined with Amantadine.
AmbrisentanThe serum concentration of Ambrisentan can be decreased when it is combined with Tacrolimus.
AmilorideAmiloride may increase the hyperkalemic activities of Tacrolimus.
Aminohippuric acidThe serum concentration of Tacrolimus can be increased when it is combined with Aminohippuric acid.
AmiodaroneThe serum concentration of Tacrolimus can be decreased when it is combined with Amiodarone.
AmitriptylineThe serum concentration of Amitriptyline can be decreased when it is combined with Tacrolimus.
AmitriptylineThe serum concentration of Tacrolimus can be increased when it is combined with Amitriptyline.
AmlodipineThe serum concentration of Tacrolimus can be increased when it is combined with Amlodipine.
AmorolfineThe metabolism of Tacrolimus can be decreased when combined with Amorolfine.
AmoxapineThe metabolism of Tacrolimus can be decreased when combined with Amoxapine.
Amphotericin BThe metabolism of Tacrolimus can be decreased when combined with Amphotericin B.
AmprenavirThe metabolism of Tacrolimus can be decreased when combined with Amprenavir.
AmsacrineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Amsacrine.
AmsacrineThe serum concentration of Tacrolimus can be increased when it is combined with Amsacrine.
AN2690The metabolism of Tacrolimus can be decreased when combined with AN2690.
AnakinraThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Anakinra.
AnidulafunginThe metabolism of Tacrolimus can be decreased when combined with Anidulafungin.
Anti-thymocyte Globulin (Rabbit)The risk or severity of adverse effects can be increased when Tacrolimus is combined with Anti-thymocyte Globulin (Rabbit).
AntipyrineAntipyrine may increase the nephrotoxic activities of Tacrolimus.
Antithrombin III humanThe metabolism of Tacrolimus can be decreased when combined with Antithrombin III human.
ApixabanThe metabolism of Tacrolimus can be decreased when combined with Apixaban.
ApixabanThe serum concentration of Apixaban can be decreased when it is combined with Tacrolimus.
ApremilastThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Apremilast.
ApremilastApremilast may increase the nephrotoxic activities of Tacrolimus.
AprepitantThe serum concentration of Tacrolimus can be increased when it is combined with Aprepitant.
AprotininThe metabolism of Tacrolimus can be decreased when combined with Aprotinin.
ArgatrobanThe metabolism of Tacrolimus can be decreased when combined with Argatroban.
Arsenic trioxideThe serum concentration of Arsenic trioxide can be decreased when it is combined with Tacrolimus.
ArtemetherThe metabolism of Tacrolimus can be decreased when combined with Artemether.
AstemizoleThe serum concentration of Tacrolimus can be increased when it is combined with Astemizole.
AsunaprevirThe metabolism of Tacrolimus can be decreased when combined with Asunaprevir.
AtazanavirThe metabolism of Tacrolimus can be decreased when combined with Atazanavir.
AtazanavirThe serum concentration of Atazanavir can be decreased when it is combined with Tacrolimus.
AtenololThe serum concentration of Atenolol can be decreased when it is combined with Tacrolimus.
AtenololThe serum concentration of Tacrolimus can be increased when it is combined with Atenolol.
AtomoxetineThe metabolism of Tacrolimus can be decreased when combined with Atomoxetine.
AtorvastatinThe serum concentration of Tacrolimus can be increased when it is combined with Atorvastatin.
AxitinibThe serum concentration of Axitinib can be decreased when it is combined with Tacrolimus.
AzacitidineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Azacitidine.
AzapropazoneAzapropazone may increase the nephrotoxic activities of Tacrolimus.
AzathioprineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Azathioprine.
AzelastineAzelastine may increase the nephrotoxic activities of Tacrolimus.
AzithromycinThe serum concentration of Tacrolimus can be increased when it is combined with Azithromycin.
Bafilomycin A1The metabolism of Tacrolimus can be decreased when combined with Bafilomycin A1.
BalsalazideBalsalazide may increase the nephrotoxic activities of Tacrolimus.
BasiliximabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Basiliximab.
BatimastatThe metabolism of Tacrolimus can be decreased when combined with Batimastat.
BelataceptThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Belatacept.
BelimumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Belimumab.
BenazeprilThe metabolism of Tacrolimus can be decreased when combined with Benazepril.
BenoxaprofenBenoxaprofen may increase the nephrotoxic activities of Tacrolimus.
BenzamidineThe metabolism of Tacrolimus can be decreased when combined with Benzamidine.
BenzocaineThe serum concentration of Tacrolimus can be increased when it is combined with Benzocaine.
Benzoic AcidThe metabolism of Tacrolimus can be decreased when combined with Benzoic Acid.
BepridilThe serum concentration of Tacrolimus can be increased when it is combined with Bepridil.
BetamethasoneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Betamethasone.
BexaroteneThe serum concentration of Tacrolimus can be decreased when it is combined with Bexarotene.
BifonazoleThe metabolism of Tacrolimus can be decreased when combined with Bifonazole.
BiperidenThe serum concentration of Tacrolimus can be increased when it is combined with Biperiden.
BivalirudinThe metabolism of Tacrolimus can be decreased when combined with Bivalirudin.
BleomycinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Bleomycin.
BlinatumomabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Blinatumomab.
BoceprevirThe metabolism of Tacrolimus can be decreased when combined with Boceprevir.
BoceprevirThe serum concentration of Boceprevir can be decreased when it is combined with Tacrolimus.
BortezomibThe metabolism of Tacrolimus can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Tacrolimus can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Tacrolimus.
Brentuximab vedotinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Brentuximab vedotin.
BriakinumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Briakinumab.
BromfenacBromfenac may increase the nephrotoxic activities of Tacrolimus.
BromocriptineThe serum concentration of Bromocriptine can be decreased when it is combined with Tacrolimus.
BromocriptineThe serum concentration of Tacrolimus can be increased when it is combined with Bromocriptine.
BudesonideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Budesonide.
BuforminThe therapeutic efficacy of Buformin can be decreased when used in combination with Tacrolimus.
BuprenorphineThe serum concentration of Tacrolimus can be increased when it is combined with Buprenorphine.
BuspironeThe serum concentration of Tacrolimus can be increased when it is combined with Buspirone.
BusulfanThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Busulfan.
ButenafineThe metabolism of Tacrolimus can be decreased when combined with Butenafine.
ButoconazoleThe metabolism of Tacrolimus can be decreased when combined with Butoconazole.
CabazitaxelThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Cabazitaxel.
CabazitaxelThe serum concentration of Tacrolimus can be increased when it is combined with Cabazitaxel.
CaffeineThe serum concentration of Caffeine can be decreased when it is combined with Tacrolimus.
CaffeineThe serum concentration of Tacrolimus can be increased when it is combined with Caffeine.
CamptothecinThe serum concentration of Camptothecin can be decreased when it is combined with Tacrolimus.
CanagliflozinThe therapeutic efficacy of Canagliflozin can be decreased when used in combination with Tacrolimus.
CanagliflozinThe serum concentration of Tacrolimus can be increased when it is combined with Canagliflozin.
CanakinumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Canakinumab.
CandesartanThe serum concentration of Tacrolimus can be increased when it is combined with Candesartan.
CandicidinThe metabolism of Tacrolimus can be decreased when combined with Candicidin.
CandoxatrilThe metabolism of Tacrolimus can be decreased when combined with Candoxatril.
CapecitabineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Capecitabine.
CaptoprilThe metabolism of Tacrolimus can be decreased when combined with Captopril.
CarbamazepineThe serum concentration of Tacrolimus can be decreased when it is combined with Carbamazepine.
CarboplatinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Carboplatin.
CarfilzomibThe serum concentration of Carfilzomib can be decreased when it is combined with Tacrolimus.
CarmustineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Carmustine.
CarprofenCarprofen may increase the nephrotoxic activities of Tacrolimus.
CarvedilolThe serum concentration of Tacrolimus can be increased when it is combined with Carvedilol.
CaspofunginThe serum concentration of Tacrolimus can be decreased when it is combined with Caspofungin.
CastanospermineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Castanospermine.
CastanospermineCastanospermine may increase the nephrotoxic activities of Tacrolimus.
CelecoxibCelecoxib may increase the nephrotoxic activities of Tacrolimus.
CeritinibThe serum concentration of Tacrolimus can be increased when it is combined with Ceritinib.
CeritinibThe serum concentration of Ceritinib can be decreased when it is combined with Tacrolimus.
CerivastatinThe serum concentration of Cerivastatin can be decreased when it is combined with Tacrolimus.
Certolizumab pegolThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Certolizumab pegol.
CeruleninThe metabolism of Tacrolimus can be decreased when combined with Cerulenin.
ChlorambucilThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Chlorambucil.
ChloramphenicolThe serum concentration of Tacrolimus can be increased when it is combined with Chloramphenicol.
ChloroquineChloroquine may increase the nephrotoxic activities of Tacrolimus.
ChloroxineThe metabolism of Tacrolimus can be decreased when combined with Chloroxine.
ChlorpromazineThe serum concentration of Chlorpromazine can be decreased when it is combined with Tacrolimus.
ChlorpromazineThe serum concentration of Tacrolimus can be increased when it is combined with Chlorpromazine.
ChlorpropamideThe therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Tacrolimus.
ChlorpropamideThe serum concentration of Tacrolimus can be increased when it is combined with Chlorpropamide.
ChlorprothixeneThe serum concentration of Tacrolimus can be increased when it is combined with Chlorprothixene.
CholesterolThe serum concentration of Tacrolimus can be increased when it is combined with Cholesterol.
Cholic AcidThe serum concentration of Tacrolimus can be decreased when it is combined with Cholic Acid.
ChymostatinThe metabolism of Tacrolimus can be decreased when combined with Chymostatin.
CiclopiroxThe metabolism of Tacrolimus can be decreased when combined with Ciclopirox.
CiglitazoneThe therapeutic efficacy of Ciglitazone can be decreased when used in combination with Tacrolimus.
CilastatinThe metabolism of Tacrolimus can be decreased when combined with Cilastatin.
CilazaprilThe metabolism of Tacrolimus can be decreased when combined with Cilazapril.
CimetidineThe serum concentration of Tacrolimus can be decreased when it is combined with Cimetidine.
CinacalcetThe serum concentration of Tacrolimus can be decreased when it is combined with Cinacalcet.
CiprofloxacinThe serum concentration of Ciprofloxacin can be decreased when it is combined with Tacrolimus.
CiprofloxacinThe serum concentration of Tacrolimus can be increased when it is combined with Ciprofloxacin.
CisplatinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Cisplatin.
CitalopramThe metabolism of Tacrolimus can be decreased when combined with Citalopram.
CitalopramThe serum concentration of Citalopram can be decreased when it is combined with Tacrolimus.
CladribineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Cladribine.
ClarithromycinThe serum concentration of Clarithromycin can be decreased when it is combined with Tacrolimus.
ClarithromycinThe serum concentration of Tacrolimus can be increased when it is combined with Clarithromycin.
ClemastineThe metabolism of Tacrolimus can be decreased when combined with Clemastine.
ClobazamThe serum concentration of Clobazam can be decreased when it is combined with Tacrolimus.
ClofarabineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Clofarabine.
ClofazimineThe serum concentration of Tacrolimus can be increased when it is combined with Clofazimine.
ClomifeneThe serum concentration of Clomifene can be decreased when it is combined with Tacrolimus.
ClomipramineThe metabolism of Tacrolimus can be decreased when combined with Clomipramine.
ClonidineThe serum concentration of Clonidine can be decreased when it is combined with Tacrolimus.
ClonixinClonixin may increase the nephrotoxic activities of Tacrolimus.
ClopidogrelThe serum concentration of Clopidogrel can be decreased when it is combined with Tacrolimus.
ClotrimazoleThe serum concentration of Tacrolimus can be increased when it is combined with Clotrimazole.
ClozapineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Clozapine.
CobicistatThe serum concentration of Tacrolimus can be increased when it is combined with Cobicistat.
CobimetinibThe serum concentration of Cobimetinib can be decreased when it is combined with Tacrolimus.
ColchicineThe serum concentration of Colchicine can be decreased when it is combined with Tacrolimus.
ColchicineThe serum concentration of Tacrolimus can be increased when it is combined with Colchicine.
ColforsinThe serum concentration of Tacrolimus can be increased when it is combined with Colforsin.
ConivaptanThe serum concentration of Tacrolimus can be increased when it is combined with Conivaptan.
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be decreased when it is combined with Tacrolimus.
CorticotropinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Corticotropin.
Cortisone acetateThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Cortisone acetate.
CrizotinibThe serum concentration of Tacrolimus can be increased when it is combined with Crizotinib.
CrizotinibThe serum concentration of Crizotinib can be decreased when it is combined with Tacrolimus.
CyclophosphamideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Cyclophosphamide.
CyclophosphamideThe serum concentration of Tacrolimus can be increased when it is combined with Cyclophosphamide.
CyclosporineTacrolimus may increase the nephrotoxic activities of Cyclosporine.
CyclosporineThe metabolism of Tacrolimus can be decreased when combined with Cyclosporine.
CytarabineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Cytarabine.
D-LimoneneD-Limonene may increase the nephrotoxic activities of Tacrolimus.
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be decreased when it is combined with Tacrolimus.
Dabigatran etexilateThe metabolism of Tacrolimus can be decreased when combined with Dabigatran etexilate.
DabrafenibThe serum concentration of Tacrolimus can be decreased when it is combined with Dabrafenib.
DacarbazineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Dacarbazine.
DaclatasvirThe serum concentration of Tacrolimus can be increased when it is combined with Daclatasvir.
DaclizumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Daclizumab.
DactinomycinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Dactinomycin.
DactinomycinThe serum concentration of Tacrolimus can be increased when it is combined with Dactinomycin.
DanazolThe serum concentration of Tacrolimus can be increased when it is combined with Danazol.
DapagliflozinThe serum concentration of Dapagliflozin can be decreased when it is combined with Tacrolimus.
DapoxetineThe metabolism of Tacrolimus can be decreased when combined with Dapoxetine.
DarunavirThe metabolism of Tacrolimus can be decreased when combined with Darunavir.
DasatinibThe serum concentration of Tacrolimus can be increased when it is combined with Dasatinib.
DasatinibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Dasatinib.
DaunorubicinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Daunorubicin.
DaunorubicinThe serum concentration of Tacrolimus can be decreased when it is combined with Daunorubicin.
DebrisoquinThe serum concentration of Debrisoquin can be decreased when it is combined with Tacrolimus.
Decanoic AcidThe metabolism of Tacrolimus can be decreased when combined with Decanoic Acid.
DeferasiroxThe serum concentration of Tacrolimus can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Tacrolimus can be decreased when combined with Delavirdine.
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Tacrolimus.
DesipramineThe serum concentration of Tacrolimus can be increased when it is combined with Desipramine.
DesloratadineThe serum concentration of Tacrolimus can be increased when it is combined with Desloratadine.
DexamethasoneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Dexamethasone.
DexamethasoneThe serum concentration of Tacrolimus can be decreased when it is combined with Dexamethasone.
DextromethorphanThe serum concentration of Tacrolimus can be increased when it is combined with Dextromethorphan.
DiazepamThe serum concentration of Diazepam can be decreased when it is combined with Tacrolimus.
DiclofenacDiclofenac may increase the nephrotoxic activities of Tacrolimus.
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be decreased when it is combined with Tacrolimus.
DiflunisalDiflunisal may increase the nephrotoxic activities of Tacrolimus.
DigitoxinThe serum concentration of Digitoxin can be decreased when it is combined with Tacrolimus.
DigoxinThe serum concentration of Tacrolimus can be decreased when it is combined with Digoxin.
DihydroergotamineThe metabolism of Tacrolimus can be decreased when combined with Dihydroergotamine.
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be decreased when it is combined with Tacrolimus.
DiltiazemThe metabolism of Tacrolimus can be decreased when combined with Diltiazem.
DiltiazemThe serum concentration of Diltiazem can be decreased when it is combined with Tacrolimus.
Dimethyl fumarateThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Dimethyl fumarate.
DinutuximabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Dinutuximab.
DipyridamoleThe serum concentration of Dipyridamole can be decreased when it is combined with Tacrolimus.
DipyridamoleThe serum concentration of Tacrolimus can be increased when it is combined with Dipyridamole.
DocetaxelThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Docetaxel.
DomperidoneThe serum concentration of Domperidone can be decreased when it is combined with Tacrolimus.
DoxazosinThe serum concentration of Tacrolimus can be increased when it is combined with Doxazosin.
DoxepinThe serum concentration of Tacrolimus can be increased when it is combined with Doxepin.
DoxorubicinThe serum concentration of Doxorubicin can be decreased when it is combined with Tacrolimus.
DoxycyclineThe metabolism of Tacrolimus can be decreased when combined with Doxycycline.
DronabinolThe serum concentration of Tacrolimus can be increased when it is combined with Dronabinol.
DronedaroneTacrolimus may increase the QTc-prolonging activities of Dronedarone.
DronedaroneThe metabolism of Tacrolimus can be decreased when combined with Dronedarone.
DroxicamDroxicam may increase the nephrotoxic activities of Tacrolimus.
DulaglutideThe therapeutic efficacy of Dulaglutide can be decreased when used in combination with Tacrolimus.
EcabetThe metabolism of Tacrolimus can be decreased when combined with Ecabet.
EconazoleThe metabolism of Tacrolimus can be decreased when combined with Econazole.
EculizumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Eculizumab.
EdoxabanThe metabolism of Tacrolimus can be decreased when combined with Edoxaban.
EdoxabanThe serum concentration of Edoxaban can be decreased when it is combined with Tacrolimus.
EfalizumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Efalizumab.
EfavirenzThe serum concentration of Tacrolimus can be decreased when it is combined with Efavirenz.
EfinaconazoleThe metabolism of Tacrolimus can be decreased when combined with Efinaconazole.
EfonidipineThe serum concentration of Tacrolimus can be increased when it is combined with Efonidipine.
ElafinThe metabolism of Tacrolimus can be decreased when combined with Elafin.
ElbasvirThe serum concentration of Tacrolimus can be increased when it is combined with Elbasvir.
EletriptanThe serum concentration of Eletriptan can be decreased when it is combined with Tacrolimus.
EmpagliflozinThe therapeutic efficacy of Empagliflozin can be decreased when used in combination with Tacrolimus.
EnalaprilThe metabolism of Tacrolimus can be decreased when combined with Enalapril.
EnalaprilatThe metabolism of Tacrolimus can be decreased when combined with Enalaprilat.
EnalkirenThe metabolism of Tacrolimus can be decreased when combined with Enalkiren.
EnzalutamideThe serum concentration of Tacrolimus can be decreased when it is combined with Enzalutamide.
EpinastineThe serum concentration of Epinastine can be decreased when it is combined with Tacrolimus.
EpirizoleEpirizole may increase the nephrotoxic activities of Tacrolimus.
EpirubicinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Epirubicin.
EplerenoneEplerenone may increase the hyperkalemic activities of Tacrolimus.
ErgonovineThe serum concentration of Tacrolimus can be increased when it is combined with Ergonovine.
ErgotamineThe serum concentration of Tacrolimus can be increased when it is combined with Ergotamine.
ErlotinibThe serum concentration of Erlotinib can be decreased when it is combined with Tacrolimus.
ErtapenemThe serum concentration of Tacrolimus can be increased when it is combined with Ertapenem.
ErythromycinThe metabolism of Tacrolimus can be decreased when combined with Erythromycin.
ErythromycinThe serum concentration of Erythromycin can be decreased when it is combined with Tacrolimus.
EscitalopramThe metabolism of Tacrolimus can be decreased when combined with Escitalopram.
Eslicarbazepine acetateThe serum concentration of Tacrolimus can be decreased when it is combined with Eslicarbazepine acetate.
EsomeprazoleThe serum concentration of Tacrolimus can be increased when it is combined with Esomeprazole.
EstradiolThe serum concentration of Estradiol can be decreased when it is combined with Tacrolimus.
EstramustineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Estramustine.
EstramustineThe serum concentration of Tacrolimus can be increased when it is combined with Estramustine.
EstriolThe serum concentration of Estriol can be decreased when it is combined with Tacrolimus.
EstroneThe serum concentration of Estrone can be decreased when it is combined with Tacrolimus.
EtanerceptThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Etanercept.
EtanerceptEtanercept may increase the nephrotoxic activities of Tacrolimus.
EthanolEthanol can cause an increase in the absorption of Tacrolimus resulting in an increased serum concentration and potentially a worsening of adverse effects.
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be decreased when it is combined with Tacrolimus.
EtodolacEtodolac may increase the nephrotoxic activities of Tacrolimus.
EtofenamateEtofenamate may increase the nephrotoxic activities of Tacrolimus.
EtoperidoneThe metabolism of Tacrolimus can be decreased when combined with Etoperidone.
EtoposideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Etoposide.
EtoposideThe serum concentration of Tacrolimus can be increased when it is combined with Etoposide.
EtoricoxibEtoricoxib may increase the nephrotoxic activities of Tacrolimus.
EtravirineThe serum concentration of Tacrolimus can be decreased when it is combined with Etravirine.
Evening primrose oilEvening primrose oil may increase the nephrotoxic activities of Tacrolimus.
EverolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Everolimus.
ExenatideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Tacrolimus.
exisulindexisulind may increase the nephrotoxic activities of Tacrolimus.
EzetimibeThe serum concentration of Ezetimibe can be decreased when it is combined with Tacrolimus.
FelodipineThe serum concentration of Tacrolimus can be increased when it is combined with Felodipine.
FenbufenFenbufen may increase the nephrotoxic activities of Tacrolimus.
FenfluramineThe metabolism of Tacrolimus can be decreased when combined with Fenfluramine.
FenofibrateTacrolimus may increase the nephrotoxic activities of Fenofibrate.
FenoprofenFenoprofen may increase the nephrotoxic activities of Tacrolimus.
FentanylThe serum concentration of Tacrolimus can be increased when it is combined with Fentanyl.
FesoterodineThe serum concentration of Fesoterodine can be decreased when it is combined with Tacrolimus.
FexofenadineThe serum concentration of Fexofenadine can be decreased when it is combined with Tacrolimus.
FexofenadineThe serum concentration of Tacrolimus can be increased when it is combined with Fexofenadine.
FidaxomicinThe serum concentration of Fidaxomicin can be decreased when it is combined with Tacrolimus.
FidaxomicinThe serum concentration of Tacrolimus can be increased when it is combined with Fidaxomicin.
FingolimodThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Fingolimod.
FloctafenineFloctafenine may increase the nephrotoxic activities of Tacrolimus.
FloxuridineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Floxuridine.
FluconazoleThe metabolism of Tacrolimus can be decreased when combined with Fluconazole.
FlucytosineThe metabolism of Tacrolimus can be decreased when combined with Flucytosine.
FludarabineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Fludarabine.
FludrocortisoneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Fludrocortisone.
FlunixinFlunixin may increase the nephrotoxic activities of Tacrolimus.
FluorouracilThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Fluorouracil.
FluoxetineThe metabolism of Tacrolimus can be decreased when combined with Fluoxetine.
FlupentixolThe serum concentration of Tacrolimus can be increased when it is combined with Flupentixol.
FluphenazineThe serum concentration of Tacrolimus can be increased when it is combined with Fluphenazine.
FlurazepamThe serum concentration of Tacrolimus can be increased when it is combined with Flurazepam.
FlurbiprofenFlurbiprofen may increase the nephrotoxic activities of Tacrolimus.
Fluticasone furoateThe serum concentration of Fluticasone furoate can be decreased when it is combined with Tacrolimus.
FluvoxamineThe metabolism of Tacrolimus can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Tacrolimus can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Tacrolimus can be increased when it is combined with Fosaprepitant.
FoscarnetFoscarnet may increase the nephrotoxic activities of Tacrolimus.
FosinoprilThe metabolism of Tacrolimus can be decreased when combined with Fosinopril.
FosphenytoinThe serum concentration of Tacrolimus can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Tacrolimus can be increased when it is combined with Fusidic Acid.
Gallium nitrateThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Gallium nitrate.
GefitinibThe serum concentration of Gefitinib can be decreased when it is combined with Tacrolimus.
GefitinibThe serum concentration of Tacrolimus can be increased when it is combined with Gefitinib.
GeldanamycinThe metabolism of Tacrolimus can be decreased when combined with Geldanamycin.
GemcitabineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Gemcitabine.
Gemtuzumab ozogamicinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Gemtuzumab ozogamicin.
GenisteinThe serum concentration of Tacrolimus can be increased when it is combined with Genistein.
Glatiramer AcetateThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Glatiramer Acetate.
GlibornurideThe therapeutic efficacy of Glibornuride can be decreased when used in combination with Tacrolimus.
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Tacrolimus.
GlimepirideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Glimepiride.
GlipizideThe therapeutic efficacy of Glipizide can be decreased when used in combination with Tacrolimus.
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Tacrolimus.
GlyburideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Tacrolimus.
GlyburideThe serum concentration of Tacrolimus can be increased when it is combined with Glyburide.
GlycerolThe serum concentration of Tacrolimus can be increased when it is combined with Glycerol.
GlyphosateThe metabolism of Tacrolimus can be decreased when combined with Glyphosate.
GM6001The metabolism of Tacrolimus can be decreased when combined with GM6001.
GolimumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Golimumab.
Gramicidin DThe serum concentration of Tacrolimus can be increased when it is combined with Gramicidin D.
GrazoprevirThe serum concentration of Grazoprevir can be decreased when it is combined with Tacrolimus.
GrepafloxacinThe serum concentration of Grepafloxacin can be decreased when it is combined with Tacrolimus.
GrepafloxacinThe serum concentration of Tacrolimus can be increased when it is combined with Grepafloxacin.
GriseofulvinThe metabolism of Tacrolimus can be decreased when combined with Griseofulvin.
HaloperidolThe serum concentration of Haloperidol can be decreased when it is combined with Tacrolimus.
HaloperidolThe serum concentration of Tacrolimus can be increased when it is combined with Haloperidol.
HaloproginThe metabolism of Tacrolimus can be decreased when combined with Haloprogin.
HexetidineThe metabolism of Tacrolimus can be decreased when combined with Hexetidine.
HirulogThe metabolism of Tacrolimus can be decreased when combined with Hirulog.
HMPL-004HMPL-004 may increase the nephrotoxic activities of Tacrolimus.
HydrocortisoneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Hydrocortisone.
HydrocortisoneThe serum concentration of Tacrolimus can be increased when it is combined with Hydrocortisone.
HydroxyureaThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Hydroxyurea.
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Ibritumomab tiuxetan.
IbrutinibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Ibrutinib.
IbuprofenIbuprofen may increase the nephrotoxic activities of Tacrolimus.
IbuprofenThe serum concentration of Ibuprofen can be decreased when it is combined with Tacrolimus.
IbuproxamIbuproxam may increase the nephrotoxic activities of Tacrolimus.
IcatibantThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Icatibant.
IcatibantIcatibant may increase the nephrotoxic activities of Tacrolimus.
IdarubicinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Idarubicin.
IdelalisibThe serum concentration of Tacrolimus can be increased when it is combined with Idelalisib.
IdelalisibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Idelalisib.
IfosfamideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Ifosfamide.
ImatinibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Imatinib.
ImatinibThe metabolism of Tacrolimus can be decreased when combined with Imatinib.
ImipramineThe serum concentration of Imipramine can be decreased when it is combined with Tacrolimus.
ImipramineThe serum concentration of Tacrolimus can be increased when it is combined with Imipramine.
ImiquimodThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Imiquimod.
IndacaterolThe serum concentration of Indacaterol can be decreased when it is combined with Tacrolimus.
IndalpineThe metabolism of Tacrolimus can be decreased when combined with Indalpine.
IndinavirThe metabolism of Tacrolimus can be decreased when combined with Indinavir.
IndinavirThe serum concentration of Indinavir can be decreased when it is combined with Tacrolimus.
IndomethacinIndomethacin may increase the nephrotoxic activities of Tacrolimus.
IndomethacinThe serum concentration of Indomethacin can be decreased when it is combined with Tacrolimus.
IndoprofenIndoprofen may increase the nephrotoxic activities of Tacrolimus.
InfliximabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Infliximab.
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Tacrolimus.
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Tacrolimus.
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Tacrolimus.
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Tacrolimus.
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Tacrolimus.
Insulin PorkThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Tacrolimus.
IrinotecanThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Irinotecan.
IsavuconazoniumThe metabolism of Tacrolimus can be decreased when combined with Isavuconazonium.
IsoconazoleThe metabolism of Tacrolimus can be decreased when combined with Isoconazole.
IsoflurophateThe metabolism of Tacrolimus can be decreased when combined with Isoflurophate.
IsoxicamIsoxicam may increase the nephrotoxic activities of Tacrolimus.
IsradipineThe metabolism of Tacrolimus can be decreased when combined with Isradipine.
ItraconazoleThe metabolism of Tacrolimus can be decreased when combined with Itraconazole.
IvacaftorThe serum concentration of Tacrolimus can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Ivermectin can be decreased when it is combined with Tacrolimus.
IvermectinThe serum concentration of Tacrolimus can be increased when it is combined with Ivermectin.
IxazomibThe metabolism of Tacrolimus can be decreased when combined with Ixazomib.
KebuzoneKebuzone may increase the nephrotoxic activities of Tacrolimus.
KetamineThe serum concentration of Tacrolimus can be increased when it is combined with Ketamine.
KetazolamThe serum concentration of Ketazolam can be decreased when it is combined with Tacrolimus.
KetoconazoleThe serum concentration of Ketoconazole can be decreased when it is combined with Tacrolimus.
KetoconazoleThe serum concentration of Tacrolimus can be increased when it is combined with Ketoconazole.
KetoprofenKetoprofen may increase the nephrotoxic activities of Tacrolimus.
KetorolacKetorolac may increase the nephrotoxic activities of Tacrolimus.
L-PhenylalanineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with L-Phenylalanine.
LamivudineThe serum concentration of Lamivudine can be decreased when it is combined with Tacrolimus.
LamotrigineThe serum concentration of Lamotrigine can be decreased when it is combined with Tacrolimus.
LansoprazoleThe serum concentration of Lansoprazole can be decreased when it is combined with Tacrolimus.
LansoprazoleThe serum concentration of Tacrolimus can be increased when it is combined with Lansoprazole.
LapatinibThe serum concentration of Tacrolimus can be increased when it is combined with Lapatinib.
LedipasvirThe serum concentration of Ledipasvir can be decreased when it is combined with Tacrolimus.
LeflunomideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Leflunomide.
LeflunomideLeflunomide may increase the nephrotoxic activities of Tacrolimus.
LenalidomideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Lenalidomide.
LenvatinibThe serum concentration of Lenvatinib can be decreased when it is combined with Tacrolimus.
LepirudinThe metabolism of Tacrolimus can be decreased when combined with Lepirudin.
LevetiracetamThe serum concentration of Levetiracetam can be decreased when it is combined with Tacrolimus.
LevofloxacinLevofloxacin may increase the QTc-prolonging activities of Tacrolimus.
LevofloxacinThe serum concentration of Levofloxacin can be decreased when it is combined with Tacrolimus.
LevomilnacipranThe metabolism of Tacrolimus can be decreased when combined with Levomilnacipran.
LevomilnacipranThe serum concentration of Levomilnacipran can be decreased when it is combined with Tacrolimus.
LevothyroxineThe serum concentration of Tacrolimus can be decreased when it is combined with Levothyroxine.
LidocaineThe serum concentration of Tacrolimus can be increased when it is combined with Lidocaine.
LinagliptinThe metabolism of Tacrolimus can be decreased when combined with Linagliptin.
LinagliptinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Tacrolimus.
LiothyronineThe serum concentration of Tacrolimus can be decreased when it is combined with Liothyronine.
LiotrixThe serum concentration of Tacrolimus can be decreased when it is combined with Liotrix.
LiraglutideThe therapeutic efficacy of Liraglutide can be decreased when used in combination with Tacrolimus.
LisinoprilThe metabolism of Tacrolimus can be decreased when combined with Lisinopril.
LomitapideThe serum concentration of Tacrolimus can be increased when it is combined with Lomitapide.
LomustineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Lomustine.
LoperamideThe serum concentration of Loperamide can be decreased when it is combined with Tacrolimus.
LoperamideThe serum concentration of Tacrolimus can be increased when it is combined with Loperamide.
LopinavirThe metabolism of Tacrolimus can be decreased when combined with Lopinavir.
LoratadineThe serum concentration of Tacrolimus can be increased when it is combined with Loratadine.
LornoxicamLornoxicam may increase the nephrotoxic activities of Tacrolimus.
LosartanThe serum concentration of Losartan can be decreased when it is combined with Tacrolimus.
LosartanThe serum concentration of Tacrolimus can be increased when it is combined with Losartan.
LovastatinThe metabolism of Tacrolimus can be decreased when combined with Lovastatin.
LoxoprofenLoxoprofen may increase the nephrotoxic activities of Tacrolimus.
Lu AA21004The metabolism of Tacrolimus can be decreased when combined with Lu AA21004.
LuliconazoleThe serum concentration of Tacrolimus can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Tacrolimus can be decreased when it is combined with Lumacaftor.
LumiracoxibLumiracoxib may increase the nephrotoxic activities of Tacrolimus.
Magnesium salicylateMagnesium salicylate may increase the nephrotoxic activities of Tacrolimus.
MannitolThe serum concentration of Mannitol can be decreased when it is combined with Tacrolimus.
MaprotilineThe serum concentration of Tacrolimus can be increased when it is combined with Maprotiline.
MasoprocolMasoprocol may increase the nephrotoxic activities of Tacrolimus.
MebendazoleThe serum concentration of Tacrolimus can be increased when it is combined with Mebendazole.
MechlorethamineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Mechlorethamine.
Meclofenamic acidMeclofenamic acid may increase the nephrotoxic activities of Tacrolimus.
Mefenamic acidMefenamic acid may increase the nephrotoxic activities of Tacrolimus.
MefloquineThe serum concentration of Tacrolimus can be increased when it is combined with Mefloquine.
Megestrol acetateThe serum concentration of Tacrolimus can be increased when it is combined with Megestrol acetate.
MeloxicamMeloxicam may increase the nephrotoxic activities of Tacrolimus.
MelphalanThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Melphalan.
MepolizumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Mepolizumab.
MeprobamateThe serum concentration of Tacrolimus can be increased when it is combined with Meprobamate.
MercaptopurineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Mercaptopurine.
MesalazineMesalazine may increase the nephrotoxic activities of Tacrolimus.
MetamizoleMetamizole may increase the nephrotoxic activities of Tacrolimus.
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Tacrolimus.
MethadoneThe serum concentration of Tacrolimus can be increased when it is combined with Methadone.
MethotrexateThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Methotrexate.
MethylprednisoloneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Methylprednisolone.
MetoprololThe serum concentration of Metoprolol can be decreased when it is combined with Tacrolimus.
MetoprololThe serum concentration of Tacrolimus can be increased when it is combined with Metoprolol.
MevastatinThe metabolism of Tacrolimus can be decreased when combined with Mevastatin.
MibefradilThe serum concentration of Tacrolimus can be increased when it is combined with Mibefradil.
MicafunginThe metabolism of Tacrolimus can be decreased when combined with Micafungin.
MiconazoleThe metabolism of Tacrolimus can be decreased when combined with Miconazole.
MidazolamThe serum concentration of Midazolam can be decreased when it is combined with Tacrolimus.
MifepristoneMifepristone may increase the QTc-prolonging activities of Tacrolimus.
MiglitolThe therapeutic efficacy of Miglitol can be decreased when used in combination with Tacrolimus.
MiglustatThe therapeutic efficacy of Miglustat can be decreased when used in combination with Tacrolimus.
MilnacipranThe metabolism of Tacrolimus can be decreased when combined with Milnacipran.
MiltefosineThe metabolism of Tacrolimus can be decreased when combined with Miltefosine.
MirabegronThe serum concentration of Mirabegron can be decreased when it is combined with Tacrolimus.
MitiglinideThe therapeutic efficacy of Mitiglinide can be decreased when used in combination with Tacrolimus.
MitomycinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Mitomycin.
MitomycinThe serum concentration of Tacrolimus can be increased when it is combined with Mitomycin.
MitotaneThe serum concentration of Tacrolimus can be decreased when it is combined with Mitotane.
MitoxantroneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Mitoxantrone.
MitoxantroneThe serum concentration of Tacrolimus can be decreased when it is combined with Mitoxantrone.
ModafinilThe serum concentration of Tacrolimus can be decreased when it is combined with Modafinil.
MoexiprilThe metabolism of Tacrolimus can be decreased when combined with Moexipril.
MonensinThe metabolism of Tacrolimus can be decreased when combined with Monensin.
MorphineThe serum concentration of Morphine can be decreased when it is combined with Tacrolimus.
MorphineThe serum concentration of Tacrolimus can be increased when it is combined with Morphine.
MuromonabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Muromonab.
Mycophenolate mofetilThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Mycophenolate mofetil.
Mycophenolate mofetilMycophenolate mofetil may increase the nephrotoxic activities of Tacrolimus.
Mycophenolic acidThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Mycophenolic acid.
Mycophenolic acidMycophenolic acid may increase the nephrotoxic activities of Tacrolimus.
MyxothiazolThe metabolism of Tacrolimus can be decreased when combined with Myxothiazol.
N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-ProlineThe metabolism of Tacrolimus can be decreased when combined with N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-Proline.
NabumetoneNabumetone may increase the nephrotoxic activities of Tacrolimus.
NadololThe serum concentration of Nadolol can be decreased when it is combined with Tacrolimus.
NafcillinThe serum concentration of Tacrolimus can be decreased when it is combined with Nafcillin.
NaftifineNaftifine may increase the nephrotoxic activities of Tacrolimus.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Tacrolimus.
NaloxoneThe serum concentration of Naloxone can be decreased when it is combined with Tacrolimus.
NaltrexoneThe serum concentration of Tacrolimus can be increased when it is combined with Naltrexone.
NaproxenNaproxen may increase the nephrotoxic activities of Tacrolimus.
NaringeninThe serum concentration of Tacrolimus can be increased when it is combined with Naringenin.
NatalizumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Natalizumab.
NatamycinThe metabolism of Tacrolimus can be decreased when combined with Natamycin.
NateglinideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Tacrolimus.
NCX 4016The metabolism of Tacrolimus can be decreased when combined with NCX 4016.
NefazodoneThe serum concentration of Tacrolimus can be decreased when it is combined with Nefazodone.
NelarabineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Nelarabine.
NelfinavirThe metabolism of Tacrolimus can be decreased when combined with Nelfinavir.
NelfinavirThe serum concentration of Nelfinavir can be decreased when it is combined with Tacrolimus.
NeostigmineThe serum concentration of Tacrolimus can be increased when it is combined with Neostigmine.
NepafenacNepafenac may increase the nephrotoxic activities of Tacrolimus.
NetupitantThe serum concentration of Tacrolimus can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Tacrolimus can be decreased when combined with Nevirapine.
NicardipineThe serum concentration of Nicardipine can be decreased when it is combined with Tacrolimus.
NicardipineThe serum concentration of Tacrolimus can be increased when it is combined with Nicardipine.
NifedipineThe serum concentration of Tacrolimus can be decreased when it is combined with Nifedipine.
Niflumic AcidNiflumic Acid may increase the nephrotoxic activities of Tacrolimus.
NilotinibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Nilotinib.
NilotinibThe metabolism of Tacrolimus can be decreased when combined with Nilotinib.
NimesulideNimesulide may increase the nephrotoxic activities of Tacrolimus.
NintedanibThe serum concentration of Nintedanib can be decreased when it is combined with Tacrolimus.
NisoldipineThe serum concentration of Tacrolimus can be increased when it is combined with Nisoldipine.
NitrazepamThe serum concentration of Tacrolimus can be increased when it is combined with Nitrazepam.
NitrendipineThe serum concentration of Tacrolimus can be increased when it is combined with Nitrendipine.
NitroxolineThe metabolism of Tacrolimus can be decreased when combined with Nitroxoline.
NizatidineThe serum concentration of Nizatidine can be decreased when it is combined with Tacrolimus.
NorethisteroneThe serum concentration of Tacrolimus can be decreased when it is combined with Norethisterone.
NystatinThe metabolism of Tacrolimus can be decreased when combined with Nystatin.
ObinutuzumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Obinutuzumab.
OlanzapineThe metabolism of Tacrolimus can be decreased when combined with Olanzapine.
OlanzapineThe serum concentration of Olanzapine can be decreased when it is combined with Tacrolimus.
OlaparibThe metabolism of Tacrolimus can be decreased when combined with Olaparib.
OlopatadineOlopatadine may increase the nephrotoxic activities of Tacrolimus.
OlsalazineOlsalazine may increase the nephrotoxic activities of Tacrolimus.
OmapatrilatThe metabolism of Tacrolimus can be decreased when combined with Omapatrilat.
OmbitasvirThe serum concentration of Ombitasvir can be decreased when it is combined with Tacrolimus.
OmeprazoleThe serum concentration of Tacrolimus can be increased when it is combined with Omeprazole.
OrgoteinOrgotein may increase the nephrotoxic activities of Tacrolimus.
OsimertinibThe serum concentration of Tacrolimus can be increased when it is combined with Osimertinib.
OsimertinibThe serum concentration of Osimertinib can be decreased when it is combined with Tacrolimus.
OtamixabanThe metabolism of Tacrolimus can be decreased when combined with Otamixaban.
OxaliplatinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Oxaliplatin.
OxaprozinOxaprozin may increase the nephrotoxic activities of Tacrolimus.
OxiconazoleThe metabolism of Tacrolimus can be decreased when combined with Oxiconazole.
OxyphenbutazoneOxyphenbutazone may increase the nephrotoxic activities of Tacrolimus.
P-NitrophenolThe serum concentration of Tacrolimus can be increased when it is combined with P-Nitrophenol.
PaclitaxelThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Paclitaxel.
PaclitaxelThe serum concentration of Tacrolimus can be increased when it is combined with Paclitaxel.
pafuramidineThe metabolism of Tacrolimus can be decreased when combined with pafuramidine.
PalbociclibThe serum concentration of Tacrolimus can be increased when it is combined with Palbociclib.
PalbociclibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Palbociclib.
Palmitic AcidThe serum concentration of Tacrolimus can be increased when it is combined with Palmitic Acid.
PanobinostatThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Panobinostat.
PantoprazoleThe serum concentration of Tacrolimus can be increased when it is combined with Pantoprazole.
ParecoxibParecoxib may increase the nephrotoxic activities of Tacrolimus.
ParoxetineThe metabolism of Tacrolimus can be decreased when combined with Paroxetine.
PazopanibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Pazopanib.
PegaspargaseThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Pegaspargase.
PemetrexedThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Pemetrexed.
PentamidineThe metabolism of Tacrolimus can be decreased when combined with Pentamidine.
PentobarbitalThe metabolism of Tacrolimus can be increased when combined with Pentobarbital.
PentostatinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Pentostatin.
PerindoprilThe metabolism of Tacrolimus can be decreased when combined with Perindopril.
PhenforminThe therapeutic efficacy of Phenformin can be decreased when used in combination with Tacrolimus.
PhenobarbitalThe serum concentration of Phenobarbital can be decreased when it is combined with Tacrolimus.
PhenylbutazonePhenylbutazone may increase the nephrotoxic activities of Tacrolimus.
PhenytoinThe serum concentration of Tacrolimus can be decreased when it is combined with Phenytoin.
PhosphoramidonThe metabolism of Tacrolimus can be decreased when combined with Phosphoramidon.
PimecrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Pimecrolimus.
PimecrolimusPimecrolimus may increase the nephrotoxic activities of Tacrolimus.
PimozideThe serum concentration of Tacrolimus can be increased when it is combined with Pimozide.
PioglitazoneThe therapeutic efficacy of Pioglitazone can be decreased when used in combination with Tacrolimus.
PirfenidoneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Pirfenidone.
PirfenidonePirfenidone may increase the nephrotoxic activities of Tacrolimus.
PiroxicamPiroxicam may increase the nephrotoxic activities of Tacrolimus.
PitavastatinThe serum concentration of Pitavastatin can be decreased when it is combined with Tacrolimus.
Platelet Activating FactorThe serum concentration of Tacrolimus can be decreased when it is combined with Platelet Activating Factor.
PomalidomideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Pomalidomide.
PonatinibThe serum concentration of Ponatinib can be decreased when it is combined with Tacrolimus.
PonatinibThe serum concentration of Tacrolimus can be increased when it is combined with Ponatinib.
PosaconazoleThe metabolism of Tacrolimus can be decreased when combined with Posaconazole.
PralatrexateThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Pralatrexate.
PramlintideThe therapeutic efficacy of Pramlintide can be decreased when used in combination with Tacrolimus.
PravastatinThe serum concentration of Pravastatin can be decreased when it is combined with Tacrolimus.
PravastatinThe serum concentration of Tacrolimus can be increased when it is combined with Pravastatin.
PrazosinThe serum concentration of Prazosin can be decreased when it is combined with Tacrolimus.
PrazosinThe serum concentration of Tacrolimus can be increased when it is combined with Prazosin.
PrednisoloneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Prednisolone.
PrednisoneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Prednisone.
PrednisoneThe serum concentration of Tacrolimus can be increased when it is combined with Prednisone.
PrimidoneThe metabolism of Tacrolimus can be increased when combined with Primidone.
PrinomastatThe metabolism of Tacrolimus can be decreased when combined with Prinomastat.
ProbenecidThe serum concentration of Tacrolimus can be increased when it is combined with Probenecid.
ProcarbazineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Procarbazine.
ProgesteroneThe serum concentration of Tacrolimus can be decreased when it is combined with Progesterone.
PromethazineThe serum concentration of Tacrolimus can be increased when it is combined with Promethazine.
PropacetamolPropacetamol may increase the nephrotoxic activities of Tacrolimus.
PropafenoneThe serum concentration of Tacrolimus can be increased when it is combined with Propafenone.
PropranololThe serum concentration of Propranolol can be decreased when it is combined with Tacrolimus.
PropranololThe serum concentration of Tacrolimus can be increased when it is combined with Propranolol.
ProtriptylineThe serum concentration of Tacrolimus can be increased when it is combined with Protriptyline.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Tacrolimus.
PTC299PTC299 may increase the nephrotoxic activities of Tacrolimus.
QuercetinThe serum concentration of Tacrolimus can be increased when it is combined with Quercetin.
QuetiapineThe serum concentration of Quetiapine can be decreased when it is combined with Tacrolimus.
QuinacrineThe serum concentration of Tacrolimus can be increased when it is combined with Quinacrine.
QuinaprilThe metabolism of Tacrolimus can be decreased when combined with Quinapril.
QuinidineThe serum concentration of Quinidine can be decreased when it is combined with Tacrolimus.
QuinidineThe serum concentration of Tacrolimus can be increased when it is combined with Quinidine.
QuinineThe serum concentration of Quinine can be decreased when it is combined with Tacrolimus.
QuinineThe serum concentration of Tacrolimus can be increased when it is combined with Quinine.
RabeprazoleThe serum concentration of Tacrolimus can be increased when it is combined with Rabeprazole.
Rabies vaccineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Rabies vaccine.
RadicicolThe metabolism of Tacrolimus can be decreased when combined with Radicicol.
RamiprilThe metabolism of Tacrolimus can be decreased when combined with Ramipril.
RanitidineThe serum concentration of Ranitidine can be decreased when it is combined with Tacrolimus.
RanitidineThe serum concentration of Tacrolimus can be increased when it is combined with Ranitidine.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Tacrolimus.
ReboxetineThe serum concentration of Tacrolimus can be increased when it is combined with Reboxetine.
RegorafenibThe serum concentration of Tacrolimus can be increased when it is combined with Regorafenib.
RemikirenThe metabolism of Tacrolimus can be decreased when combined with Remikiren.
RepaglinideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Tacrolimus.
ReserpineThe serum concentration of Tacrolimus can be decreased when it is combined with Reserpine.
ResveratrolResveratrol may increase the nephrotoxic activities of Tacrolimus.
RifabutinThe metabolism of Tacrolimus can be increased when combined with Rifabutin.
RifampicinThe serum concentration of Tacrolimus can be decreased when it is combined with Rifampicin.
RifapentineThe metabolism of Tacrolimus can be increased when combined with Rifapentine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Tacrolimus.
RilonaceptThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Rilonacept.
RilpivirineThe serum concentration of Tacrolimus can be increased when it is combined with Rilpivirine.
RisperidoneThe serum concentration of Risperidone can be decreased when it is combined with Tacrolimus.
RitonavirThe metabolism of Tacrolimus can be decreased when combined with Ritonavir.
RitonavirThe serum concentration of Ritonavir can be decreased when it is combined with Tacrolimus.
RituximabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Rituximab.
RivaroxabanThe metabolism of Tacrolimus can be decreased when combined with Rivaroxaban.
RivaroxabanThe serum concentration of Rivaroxaban can be decreased when it is combined with Tacrolimus.
RofecoxibRofecoxib may increase the nephrotoxic activities of Tacrolimus.
RoflumilastRoflumilast may increase the immunosuppressive activities of Tacrolimus.
RolapitantThe serum concentration of Tacrolimus can be increased when it is combined with Rolapitant.
RomidepsinThe serum concentration of Romidepsin can be decreased when it is combined with Tacrolimus.
RosiglitazoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Tacrolimus.
RuxolitinibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Ruxolitinib.
SalicylamideSalicylamide may increase the nephrotoxic activities of Tacrolimus.
Salicylhydroxamic AcidThe metabolism of Tacrolimus can be decreased when combined with Salicylhydroxamic Acid.
Salicylic acidSalicylic acid may increase the nephrotoxic activities of Tacrolimus.
Salicylic acidThe serum concentration of Salicylic acid can be decreased when it is combined with Tacrolimus.
SalsalateSalsalate may increase the nephrotoxic activities of Tacrolimus.
SaquinavirThe metabolism of Tacrolimus can be decreased when combined with Saquinavir.
SaquinavirThe serum concentration of Saquinavir can be decreased when it is combined with Tacrolimus.
SaxagliptinThe metabolism of Tacrolimus can be decreased when combined with Saxagliptin.
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Tacrolimus.
ScopolamineThe serum concentration of Tacrolimus can be increased when it is combined with Scopolamine.
SecukinumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Secukinumab.
SelegilineThe serum concentration of Tacrolimus can be increased when it is combined with Selegiline.
SelexipagThe serum concentration of Selexipag can be decreased when it is combined with Tacrolimus.
SeocalcitolThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Seocalcitol.
SeratrodastSeratrodast may increase the nephrotoxic activities of Tacrolimus.
SertaconazoleThe metabolism of Tacrolimus can be decreased when combined with Sertaconazole.
SertralineThe metabolism of Tacrolimus can be decreased when combined with Sertraline.
SevelamerThe serum concentration of Tacrolimus can be decreased when it is combined with Sevelamer.
SildenafilThe metabolism of Tacrolimus can be decreased when combined with Sildenafil.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Tacrolimus.
SiltuximabThe serum concentration of Tacrolimus can be decreased when it is combined with Siltuximab.
SiltuximabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Siltuximab.
SimeprevirThe metabolism of Tacrolimus can be decreased when combined with Simeprevir.
SimeprevirThe serum concentration of Simeprevir can be decreased when it is combined with Tacrolimus.
SimvastatinThe serum concentration of Tacrolimus can be increased when it is combined with Simvastatin.
SinefunginThe metabolism of Tacrolimus can be decreased when combined with Sinefungin.
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Tacrolimus.
SirolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Sirolimus.
SirolimusThe metabolism of Tacrolimus can be decreased when combined with Sirolimus.
SitagliptinThe metabolism of Tacrolimus can be decreased when combined with Sitagliptin.
SitagliptinThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Tacrolimus.
SofosbuvirThe serum concentration of Sofosbuvir can be decreased when it is combined with Tacrolimus.
SorafenibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Sorafenib.
SorafenibThe serum concentration of Tacrolimus can be increased when it is combined with Sorafenib.
SparfloxacinThe serum concentration of Sparfloxacin can be decreased when it is combined with Tacrolimus.
SphingosineThe serum concentration of Sphingosine can be decreased when it is combined with Tacrolimus.
SpiraprilThe metabolism of Tacrolimus can be decreased when combined with Spirapril.
SpironolactoneSpironolactone may increase the hyperkalemic activities of Tacrolimus.
SRT501SRT501 may increase the nephrotoxic activities of Tacrolimus.
St. John's WortThe serum concentration of Tacrolimus can be decreased when it is combined with St. John's Wort.
StaurosporineThe serum concentration of Tacrolimus can be increased when it is combined with Staurosporine.
SteproninThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Stepronin.
StiripentolThe serum concentration of Tacrolimus can be increased when it is combined with Stiripentol.
StreptozocinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Streptozocin.
StreptozocinThe serum concentration of Tacrolimus can be decreased when it is combined with Streptozocin.
SulconazoleThe metabolism of Tacrolimus can be decreased when combined with Sulconazole.
SulfasalazineSulfasalazine may increase the nephrotoxic activities of Tacrolimus.
SulfinpyrazoneThe serum concentration of Tacrolimus can be increased when it is combined with Sulfinpyrazone.
SulfisoxazoleThe metabolism of Tacrolimus can be decreased when combined with Sulfisoxazole.
SulindacSulindac may increase the nephrotoxic activities of Tacrolimus.
SulodexideThe therapeutic efficacy of Sulodexide can be decreased when used in combination with Tacrolimus.
SumatriptanThe serum concentration of Tacrolimus can be increased when it is combined with Sumatriptan.
SunitinibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Sunitinib.
SunitinibThe serum concentration of Tacrolimus can be increased when it is combined with Sunitinib.
SuprofenSuprofen may increase the nephrotoxic activities of Tacrolimus.
TacrineThe serum concentration of Tacrolimus can be increased when it is combined with Tacrine.
TAK-390MRThe serum concentration of Tacrolimus can be increased when it is combined with TAK-390MR.
TamoxifenThe serum concentration of Tamoxifen can be decreased when it is combined with Tacrolimus.
Taurocholic AcidThe serum concentration of Taurocholic Acid can be decreased when it is combined with Tacrolimus.
Taurocholic AcidThe serum concentration of Tacrolimus can be increased when it is combined with Taurocholic Acid.
TavaboroleThe metabolism of Tacrolimus can be decreased when combined with Tavaborole.
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be decreased when it is combined with Tacrolimus.
TelaprevirThe metabolism of Tacrolimus can be decreased when combined with Telaprevir.
TelaprevirThe serum concentration of Telaprevir can be decreased when it is combined with Tacrolimus.
TelithromycinThe metabolism of Tacrolimus can be decreased when combined with Telithromycin.
TelmisartanThe serum concentration of Tacrolimus can be increased when it is combined with Telmisartan.
TemocaprilThe metabolism of Tacrolimus can be decreased when combined with Temocapril.
TemozolomideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Temozolomide.
TemsirolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Temsirolimus.
TemsirolimusThe serum concentration of Tacrolimus can be increased when it is combined with Temsirolimus.
TeniposideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Teniposide.
TenoxicamTenoxicam may increase the nephrotoxic activities of Tacrolimus.
TepoxalinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Tepoxalin.
TepoxalinTepoxalin may increase the nephrotoxic activities of Tacrolimus.
TerazosinThe serum concentration of Tacrolimus can be increased when it is combined with Terazosin.
TerbinafineThe metabolism of Tacrolimus can be decreased when combined with Terbinafine.
TerconazoleThe metabolism of Tacrolimus can be decreased when combined with Terconazole.
TerfenadineThe serum concentration of Tacrolimus can be increased when it is combined with Terfenadine.
TeriflunomideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Teriflunomide.
TeriflunomideTeriflunomide may increase the nephrotoxic activities of Tacrolimus.
TesmilifeneThe serum concentration of Tacrolimus can be decreased when it is combined with Tesmilifene.
TestosteroneThe serum concentration of Tacrolimus can be increased when it is combined with Testosterone.
ThalidomideThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Thalidomide.
ThiorphanThe metabolism of Tacrolimus can be decreased when combined with Thiorphan.
ThiotepaThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Thiotepa.
ThymolThe metabolism of Tacrolimus can be decreased when combined with Thymol.
Tiaprofenic acidTiaprofenic acid may increase the nephrotoxic activities of Tacrolimus.
TicagrelorThe serum concentration of Ticagrelor can be decreased when it is combined with Tacrolimus.
TicagrelorThe serum concentration of Tacrolimus can be increased when it is combined with Ticagrelor.
TiclopidineThe metabolism of Tacrolimus can be decreased when combined with Ticlopidine.
TimololThe serum concentration of Timolol can be decreased when it is combined with Tacrolimus.
TioconazoleThe metabolism of Tacrolimus can be decreased when combined with Tioconazole.
TioguanineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Tioguanine.
TipranavirThe metabolism of Tacrolimus can be decreased when combined with Tipranavir.
TocilizumabThe serum concentration of Tacrolimus can be decreased when it is combined with Tocilizumab.
TocilizumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Tocilizumab.
TofacitinibThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Tofacitinib.
TolazamideThe therapeutic efficacy of Tolazamide can be decreased when used in combination with Tacrolimus.
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Tacrolimus.
Tolfenamic AcidTolfenamic Acid may increase the nephrotoxic activities of Tacrolimus.
TolmetinTolmetin may increase the nephrotoxic activities of Tacrolimus.
TolnaftateThe metabolism of Tacrolimus can be decreased when combined with Tolnaftate.
TolvaptanThe serum concentration of Tolvaptan can be decreased when it is combined with Tacrolimus.
TolvaptanThe serum concentration of Tacrolimus can be increased when it is combined with Tolvaptan.
TopotecanThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Topotecan.
ToremifeneThe serum concentration of Toremifene can be decreased when it is combined with Tacrolimus.
TositumomabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Tositumomab.
TrabectedinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Trabectedin.
TrandolaprilThe metabolism of Tacrolimus can be decreased when combined with Trandolapril.
TranilastTranilast may increase the nephrotoxic activities of Tacrolimus.
TrastuzumabTrastuzumab may increase the neutropenic activities of Tacrolimus.
Trastuzumab emtansineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Trastuzumab emtansine.
TrazodoneThe metabolism of Tacrolimus can be decreased when combined with Trazodone.
TretinoinThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Tretinoin.
TriamcinoloneThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Triamcinolone.
TriamtereneTriamterene may increase the hyperkalemic activities of Tacrolimus.
TrifluoperazineThe serum concentration of Tacrolimus can be increased when it is combined with Trifluoperazine.
TriflupromazineThe serum concentration of Tacrolimus can be increased when it is combined with Triflupromazine.
TrimethoprimThe serum concentration of Tacrolimus can be decreased when it is combined with Trimethoprim.
TrimetrexateThe metabolism of Tacrolimus can be decreased when combined with Trimetrexate.
TrimipramineThe serum concentration of Tacrolimus can be increased when it is combined with Trimipramine.
Trisalicylate-cholineTrisalicylate-choline may increase the nephrotoxic activities of Tacrolimus.
TroglitazoneThe therapeutic efficacy of Troglitazone can be decreased when used in combination with Tacrolimus.
TroleandomycinThe serum concentration of Tacrolimus can be increased when it is combined with Troleandomycin.
UbenimexThe metabolism of Tacrolimus can be decreased when combined with Ubenimex.
UlipristalThe serum concentration of Ulipristal can be decreased when it is combined with Tacrolimus.
UmeclidiniumThe serum concentration of Umeclidinium can be decreased when it is combined with Tacrolimus.
UstekinumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Ustekinumab.
ValdecoxibValdecoxib may increase the nephrotoxic activities of Tacrolimus.
VecuroniumThe serum concentration of Vecuronium can be decreased when it is combined with Tacrolimus.
VedolizumabThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Vedolizumab.
VenlafaxineThe metabolism of Tacrolimus can be decreased when combined with Venlafaxine.
VenlafaxineThe serum concentration of Venlafaxine can be decreased when it is combined with Tacrolimus.
VerapamilThe metabolism of Tacrolimus can be decreased when combined with Verapamil.
VerapamilThe serum concentration of Verapamil can be decreased when it is combined with Tacrolimus.
VilanterolThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Vilanterol.
VilazodoneThe metabolism of Tacrolimus can be decreased when combined with Vilazodone.
VildagliptinThe metabolism of Tacrolimus can be decreased when combined with Vildagliptin.
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Tacrolimus.
VinblastineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Vinblastine.
VinblastineThe serum concentration of Tacrolimus can be decreased when it is combined with Vinblastine.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Tacrolimus.
VincristineThe serum concentration of Tacrolimus can be decreased when it is combined with Vincristine.
VindesineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Vindesine.
VinorelbineThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Vinorelbine.
VinorelbineThe serum concentration of Tacrolimus can be increased when it is combined with Vinorelbine.
VismodegibThe serum concentration of Vismodegib can be decreased when it is combined with Tacrolimus.
VogliboseThe therapeutic efficacy of Voglibose can be decreased when used in combination with Tacrolimus.
VoriconazoleThe metabolism of Tacrolimus can be decreased when combined with Voriconazole.
VortioxetineThe metabolism of Tacrolimus can be decreased when combined with Vortioxetine.
XimelagatranThe metabolism of Tacrolimus can be decreased when combined with Ximelagatran.
ZaltoprofenZaltoprofen may increase the nephrotoxic activities of Tacrolimus.
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Tacrolimus.
ZileutonZileuton may increase the nephrotoxic activities of Tacrolimus.
ZimelidineThe metabolism of Tacrolimus can be decreased when combined with Zimelidine.
ZiprasidoneThe metabolism of Tacrolimus can be decreased when combined with Ziprasidone.
ZomepiracZomepirac may increase the nephrotoxic activities of Tacrolimus.
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.

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
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]
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
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]

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 ]
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Drug created on June 13, 2005 07:24 / Updated on September 27, 2016 02:28