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TACROLIMUS Drug Record

  • Summary
  • Interactions
  • Claims
  • TACROLIMUS chembl:CHEMBL269732 ApprovedAntineoplasticImmunotherapy

    Alternate Names:

    TACROLIMUS
    TACROLIMUS MONOHYDRATE
    FK-506
    PROTOPIC
    PROGRAF
    FK506
    FR-900506
    TACROLIMUS ANHYDROUS
    (-)-FK 506
    PROTOPIC®
    PROGRAF®
    TACROLIMUS, ANHYDROUS
    FUJIMYCIN
    ANHYDROUS TACROLIMUS
    rxcui:42316
    pubchem.compound:445643
    chemidplus:104987-11-3
    rxcui:235991
    drugbank:00864
    chembl:CHEMBL269732

    Drug Info:

    Drug Class immunosuppressive agents
    Year of Approval 1994
    Drug Class Small Molecule
    FDA Approval not approved
    Drug Class small molecule
    Drug Indications immunosuppressant
    (5 More Sources)

    Publications:

    Ren L et al., 2017, Donors FMO3 polymorphisms affect tacrolimus elimination in Chinese liver transplant patients., Pharmacogenomics
    Zhang X et al., 2011, Impact of interleukin-10 gene polymorphisms on tacrolimus dosing requirements in Chinese liver transplant patients during the early posttransplantation period., Eur J Clin Pharmacol
    Fan J et al., 2015, Donor IL-18 rs5744247 polymorphism as a new biomarker of tacrolimus elimination in Chinese liver transplant patients during the early post-transplantation period: results from two cohort studies., Pharmacogenomics
    Xing J et al., 2015, Association between interleukin-18 promoter variants and tacrolimus pharmacokinetics in Chinese renal transplant patients., Eur J Clin Pharmacol
    Kuinose et al., 2000, Calcineurin antagonists inhibit interferon-gamma production by downregulation of interleukin-18 in human mixed lymphocyte reactions., Acta Med. Okayama
    Kurzawski M et al., 2010, Association of calpain-10 gene polymorphism and posttransplant diabetes mellitus in kidney transplant patients medicated with tacrolimus., Pharmacogenomics J
    Oetting WS et al., 2018, Attempted validation of 44 reported SNPs associated with tacrolimus troughs in a cohort of kidney allograft recipients., Pharmacogenomics
    Ling Q et al., 2013, Association between donor and recipient TCF7L2 gene polymorphisms and the risk of new-onset diabetes mellitus after liver transplantation in a Han Chinese population., J Hepatol
    Kurzawski M et al., 2011, Association of transcription factor 7-like 2 (TCF7L2) gene polymorphism with posttransplant diabetes mellitus in kidney transplant patients medicated with tacrolimus., Pharmacol Rep
    Niwa et al., 2007, Effect of cyclosporine and tacrolimus on cytochrome p450 activities in human liver microsomes., Yakugaku Zasshi
    Masri et al., 2007, An assay for the determination of sirolimus levels in the lymphocyte of transplant patients., Transplant. Proc.
    Labrande et al., 2006, Neuroprotective effects of tacrolimus (FK506) in a model of ischemic cortical cell cultures: role of glutamate uptake and FK506 binding protein 12 kDa., Neuroscience
    Khanna, 2005, Tacrolimus and cyclosporinein vitro and in vivo induce osteopontin mRNA and protein expression in renal tissues., Nephron Exp. Nephrol.
    Stifft F et al., 2018, Increase in tacrolimus exposure after steroid tapering is influenced by CYP3A5 and pregnane X receptor genetic polymorphisms in renal transplant recipients., Nephrol Dial Transplant
    Kurzawski M et al., 2017, Analysis of common polymorphisms within NR1I2 and NR1I3 genes and tacrolimus dose-adjusted concentration in stable kidney transplant recipients., Pharmacogenet Genomics
    Choi Y et al., 2017, A pharmacogenomic study on the pharmacokinetics of tacrolimus in healthy subjects using the DMET<sup>TM</sup> Plus platform., Pharmacogenomics J
    Bruckmueller H et al., 2015, Which Genetic Determinants Should be Considered for Tacrolimus Dose Optimization in Kidney Transplantation? A Combined Analysis of Genes Affecting the CYP3A Locus., Ther Drug Monit
    Lancia P et al., 2018, Pharmacogenetics of post-transplant diabetes mellitus in children with renal transplantation treated with tacrolimus., Pediatr Nephrol
    Lunde I et al., 2014, The influence of CYP3A, PPARA, and POR genetic variants on the pharmacokinetics of tacrolimus and cyclosporine in renal transplant recipients., Eur J Clin Pharmacol
    Elens L et al., 2013, Single-nucleotide polymorphisms in P450 oxidoreductase and peroxisome proliferator-activated receptor-α are associated with the development of new-onset diabetes after transplantation in kidney transplant recipients treated with tacrolimus., Pharmacogenet Genomics
    Quteineh L et al., 2017, CRTC2 polymorphism as a risk factor for the incidence of metabolic syndrome in patients with solid organ transplantation., Pharmacogenomics J
    Genvigir FDV et al., 2017, Influence of ABCC2, CYP2C8, and CYP2J2 Polymorphisms on Tacrolimus and Mycophenolate Sodium-Based Treatment in Brazilian Kidney Transplant Recipients., Pharmacotherapy
    Gervasini G et al., 2013, CYP2C8*3 polymorphism and donor age are associated with allograft dysfunction in kidney transplant recipients treated with calcineurin inhibitors., J Clin Pharmacol
    Smith HE et al., 2008, Role of cytochrome P450 2C8 and 2J2 genotypes in calcineurin inhibitor-induced chronic kidney disease., Pharmacogenet Genomics
    Woillard JB et al., 2010, Risk of diarrhoea in a long-term cohort of renal transplant patients given mycophenolate mofetil: the significant role of the UGT1A8 2 variant allele., Br J Clin Pharmacol
    Knops N et al., 2017, Tacrolimus dose requirements in paediatric renal allograft recipients are characterized by a biphasic course determined by age and bone maturation., Br J Clin Pharmacol
    Zucker et al., 1999, Evidence that tacrolimus augments the bioavailability of mycophenolate mofetil through the inhibition of mycophenolic acid glucuronidation., Ther Drug Monit
    Furukawa et al., 2004, Enhanced TARC production by dust-mite allergens and its modulation by immunosuppressive drugs in PBMCs from patients with atopic dermatitis., J. Dermatol. Sci.
    Zhang T et al., 2018, Association of donor small ubiquitin-like modifier 4 rs237025 genetic variant with tacrolimus elimination in the early period after liver transplantation., Liver Int
    Pawarode et al., 2007, Differential effects of the immunosuppressive agents cyclosporin A, tacrolimus and sirolimus on drug transport by multidrug resistance proteins., Cancer Chemother. Pharmacol.
    Bosó V et al., 2013, Increased hospital stay and allograft dysfunction in renal transplant recipients with Cyp2c19 AA variant in SNP rs4244285., Drug Metab Dispos
    Liu X et al., 2015, Associations of HSD11B1 polymorphisms with tacrolimus concentrations in Chinese renal transplant recipients with prednisone combined therapy., Drug Metab Dispos
    Wu Z et al., 2017, FOXP3 rs3761548 polymorphism is associated with tacrolimus-induced acute nephrotoxicity in renal transplant patients., Eur J Clin Pharmacol
    Boillot et al., 1998, Reversal of early acute rejection with increased doses of tacrolimus in liver transplantation: a pilot study., Transplantation
    Liu J et al., 2018, Donor and recipient P450 gene polymorphisms influence individual pharmacological effects of tacrolimus in Chinese liver transplantation patients., Int Immunopharmacol
    Si S et al., 2019, Impact of single nucleotide polymorphisms on P450 oxidoreductase and peroxisome proliferator-activated receptor alpha on tacrolimus pharmacokinetics in renal transplant recipients., Pharmacogenomics J
    Phupradit A et al., 2018, Impact of POR and CYP3A5 Polymorphisms on Trough Concentration to Dose Ratio of Tacrolimus in the Early Post-operative Period Following Kidney Transplantation., Ther Drug Monit
    Almeida-Paulo GN et al., 2018, Weight of ABCB1 and POR genes on oral tacrolimus exposure in CYP3A5 nonexpressor pediatric patients with stable kidney transplant., Pharmacogenomics J
    Jannot AS et al., 2016, A Lack of Significant Effect of POR*28 Allelic Variant on Tacrolimus Exposure in Kidney Transplant Recipients., Ther Drug Monit
    Zhang JJ et al., 2015, The genetic polymorphisms of POR*28 and CYP3A5*3 significantly influence the pharmacokinetics of tacrolimus in Chinese renal transplant recipients., Int J Clin Pharmacol Ther
    Kuypers DR et al., 2014, Combined effects of CYP3A5*1, POR*28, and CYP3A4*22 single nucleotide polymorphisms on early concentration-controlled tacrolimus exposure in de-novo renal recipients., Pharmacogenet Genomics
    Kurzawski M et al., 2014, Impact of PPARA and POR polymorphisms on tacrolimus pharmacokinetics and new-onset diabetes in kidney transplant recipients., Pharmacogenet Genomics
    Lesche D et al., 2014, CYP3A5*3 and POR*28 genetic variants influence the required dose of tacrolimus in heart transplant recipients., Ther Drug Monit
    Elens L et al., 2014, Impact of POR*28 on the pharmacokinetics of tacrolimus and cyclosporine A in renal transplant patients., Ther Drug Monit
    Zhang JJ et al., 2013, Effect of the P450 oxidoreductase 28 polymorphism on the pharmacokinetics of tacrolimus in Chinese healthy male volunteers., Eur J Clin Pharmacol
    de Jonge H et al., 2011, The P450 oxidoreductase *28 SNP is associated with low initial tacrolimus exposure and increased dose requirements in CYP3A5-expressing renal recipients., Pharmacogenomics
    Tavira B et al., 2011, KCNQ1 gene variants and risk of new-onset diabetes in tacrolimus-treated renal-transplanted patients., Clin Transplant
    Tavira B et al., 2012, Association between a common KCNJ11 polymorphism (rs5219) and new-onset posttransplant diabetes in patients treated with Tacrolimus., Mol Genet Metab
    Wang Z et al., 2014, Influence of TLR4 rs1927907 locus polymorphisms on tacrolimus pharmacokinetics in the early stage after liver transplantation., Eur J Clin Pharmacol
  • TACROLIMUS   SUMO4

    Interaction Score: 3.64

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28941036


    Sources:
    PharmGKB

  • TACROLIMUS   POR

    Interaction Score: 3.41

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    30323313 29878980 29399716 28094348 26829596 26227094 25322286 25271728 24921414 24739669 24113216 24061445 23097010 21770725


    Sources:
    PharmGKB

  • TACROLIMUS   ZSCAN25

    Interaction Score: 1.82

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    29454235 29318894


    Sources:
    PharmGKB

  • TACROLIMUS   GPT

    Interaction Score: 1.82

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9825815


    Sources:
    NCI

  • TACROLIMUS   IL3

    Interaction Score: 1.82

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • TACROLIMUS   CAPN10

    Interaction Score: 1.82

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19752882


    Sources:
    PharmGKB

  • TACROLIMUS   IL18

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25712187 25487141 11061569


    Sources:
    NCI PharmGKB

  • TACROLIMUS   FOXP3

    Interaction Score: 1.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27747372


    Sources:
    PharmGKB

  • TACROLIMUS   TCF7L2

    Interaction Score: 1.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23041303 21857094


    Sources:
    PharmGKB

  • TACROLIMUS   CRTC2

    Interaction Score: 0.73

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26644205


    Sources:
    PharmGKB

  • TACROLIMUS   FKBP1A

    Interaction Score: 0.7

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name tacrolimus hydrate,Prograf, Advagraf, Graceptor
    Novel drug target Established target
    Trial Name tacrolimus,LCP-Tacro

    PMIDs:
    17524933 16289353


    Sources:
    TdgClinicalTrial ChemblInteractions TEND

  • TACROLIMUS   SPP1

    Interaction Score: 0.61

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16103732


    Sources:
    NCI

  • TACROLIMUS   HSD11B1

    Interaction Score: 0.52

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25587129


    Sources:
    PharmGKB

  • TACROLIMUS   CCL17

    Interaction Score: 0.45

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15194145


    Sources:
    NCI

  • TACROLIMUS   PPP3CA

    Interaction Score: 0.45

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • TACROLIMUS   FMO3

    Interaction Score: 0.45

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28084894


    Sources:
    PharmGKB

  • TACROLIMUS   CYP2J2

    Interaction Score: 0.36

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28316087


    Sources:
    PharmGKB

  • TACROLIMUS   CYP3A7

    Interaction Score: 0.36

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27966227


    Sources:
    PharmGKB

  • TACROLIMUS   TLR4

    Interaction Score: 0.33

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24820765


    Sources:
    PharmGKB

  • TACROLIMUS   UGT1A8

    Interaction Score: 0.33

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20565459


    Sources:
    PharmGKB

  • TACROLIMUS   NOD2

    Interaction Score: 0.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23175667


    Sources:
    PharmGKB

  • TACROLIMUS   CYP2C8

    Interaction Score: 0.29

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28316087 23426640 18769365


    Sources:
    PharmGKB

  • TACROLIMUS   KCNQ1

    Interaction Score: 0.28

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21355884


    Sources:
    PharmGKB

  • TACROLIMUS   UGT1A4

    Interaction Score: 0.26

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10051052


    Sources:
    NCI

  • TACROLIMUS   IL10

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21359536


    Sources:
    PharmGKB

  • TACROLIMUS   KCNJ11

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22264780


    Sources:
    PharmGKB

  • TACROLIMUS   PPARA

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    29399716 24658827 24113216


    Sources:
    PharmGKB

  • TACROLIMUS   ABCC2

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    29318894 28316087


    Sources:
    PharmGKB

  • TACROLIMUS   CTLA4

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • TACROLIMUS   NR1I2

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    29733390 28777242 26882121 25271728


    Sources:
    PharmGKB

  • TACROLIMUS   ABCG2

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17031644


    Sources:
    NCI

  • TACROLIMUS   CYP2D6

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17202802


    Sources:
    NCI

  • TACROLIMUS   CYP3A4

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    29318894


    Sources:
    PharmGKB

  • TACROLIMUS   AR

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TEND: TACROLIMUS

    • Version: 01-August-2011

    Alternate Names:
    TACROLIMUS Primary Drug Name

    Drug Info:
    Year of Approval 1994
    Drug Class immunosuppressive agents

    Publications:

  • TdgClinicalTrial: TACROLIMUS

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications immunosuppressant
    Drug Class small molecule
    FDA Approval not approved

    Publications:

  • NCI: TACROLIMUS

    • Version: 14-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Niwa et al., 2007, Effect of cyclosporine and tacrolimus on cytochrome p450 activities in human liver microsomes., Yakugaku Zasshi
    Khanna, 2005, Tacrolimus and cyclosporinein vitro and in vivo induce osteopontin mRNA and protein expression in renal tissues., Nephron Exp. Nephrol.
    Boillot et al., 1998, Reversal of early acute rejection with increased doses of tacrolimus in liver transplantation: a pilot study., Transplantation

  • PharmGKB: tacrolimus

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Ren L et al., 2017, Donors FMO3 polymorphisms affect tacrolimus elimination in Chinese liver transplant patients., Pharmacogenomics
    Kurzawski M et al., 2010, Association of calpain-10 gene polymorphism and posttransplant diabetes mellitus in kidney transplant patients medicated with tacrolimus., Pharmacogenomics J
    Lunde I et al., 2014, The influence of CYP3A, PPARA, and POR genetic variants on the pharmacokinetics of tacrolimus and cyclosporine in renal transplant recipients., Eur J Clin Pharmacol

  • TTD: Tacrolimus

    • Version: 2020.06.01

    Alternate Names:
    D06OMK TTD Drug ID

    Drug Info:

    Publications:

  • DTC: TACROLIMUS

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL269732 ChEMBL Drug ID

    Drug Info:

    Publications:

  • MyCancerGenomeClinicalTrial: TACROLIMUS

    • Version: 30-February-2014

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL269732

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL269732

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21