DGIdb - TACROLIMUS Drug Record

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 POR28 and CYP3A53 significantly influence the pharmacokinetics of tacrolimus in Chinese renal transplant recipients., Int J Clin Pharmacol Ther
Kuypers DR et al., 2014, Combined effects of CYP3A51, POR28, 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, CYP3A53 and POR28 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:

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

TACROLIMUS Drug Record

TACROLIMUS chembl:CHEMBL269732 ApprovedAntineoplasticImmunotherapy

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28941036

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

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

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 29454235 29318894

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 9825815

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19752882

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25712187 25487141 11061569

Sources: NCI PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27747372

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23041303 21857094

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26644205

Sources: PharmGKB

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

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16103732

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25587129

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15194145

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28084894

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28316087

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27966227

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24820765

Interaction Types & Directionality:

n/a

PMIDs:
28941036

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

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

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
29454235 29318894

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
9825815

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
19752882

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
25712187 25487141 11061569

Sources:
NCI PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
27747372

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
23041303 21857094

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
26644205

Sources:
PharmGKB

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

Interaction Types & Directionality:

n/a

PMIDs:
16103732

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
25587129

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
15194145

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
28084894

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
28316087

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
27966227

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
24820765

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
20565459

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
23175667

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
28316087 23426640 18769365

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
21355884

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
10051052

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
21359536

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
22264780

Sources:
PharmGKB

Interaction Types & Directionality:

n/a