General Information of Drug (ID: DMI782S)

Drug Name
Erdafitinib Drug Info
Synonyms
1346242-81-6; UNII-890E37NHMV; 890E37NHMV; Erdafitinib [USAN:INN]; Erdafitinib (USAN/INN); GTPL9039; SCHEMBL2583760; CHEMBL3545376; MolPort-044-560-398; JNJ-42756493 (Erdafitinib); s8401; compound 4 [WO2011135376]; ZINC168520308; AKOS030526429; CS-4988; DB12147; AC-30222; 1,2-Ethanediamine, N1-(3,5-dimethoxyphenyl)-N2-(1-methylethyl)-N1-(3-(1-methyl-1H-pyrazol-4-yl)-6-quinoxalinyl)-; HY-18708; AS-35040; KB-333716; D10927; N'-(3,5-dimethoxyphenyl)-N'-[3-(1-methylpyrazol-4-yl)quino
Indication
Disease Entry ICD 11 Status REF
Bladder cancer 2C94 Approved [1]
Solid tumour/cancer 2A00-2F9Z Phase 2 [2]
Urothelial carcinoma 2C92.0 Phase 2 [3]
Lymphoma 2A80-2A86 Phase 1/2 [4]
Cross-matching ID
PubChem CID
67462786
CAS Number
CAS 1346242-81-6
TTD Drug ID
DMI782S
INTEDE Drug ID
DR0595

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Investigative Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Futibatinib DMWM4D0 Intrahepatic cholangiocarcinoma 2C12.10 Approved [7]
Infigratinib DMNKBEC Cholangiocarcinoma 2C12.10 Approved [3]
HIF-1alpha DM4OQRD Lymphoma 2A80-2A86 Phase 4 [8]
ARQ-087 DM02BVQ Intrahepatic cholangiocarcinoma 2C12.10 Phase 3 [3]
AZD4547 DM3827C Solid tumour/cancer 2A00-2F9Z Phase 2/3 [3]
Debio 1347 DMZW50O Solid tumour/cancer 2A00-2F9Z Phase 2 [9]
BAY1163877 DMCSGJ2 Bladder cancer 2C94 Phase 2 [10]
ICP-192 DM524GR Bladder cancer 2C94 Phase 2 [11]
PRN1371 DMR7BAO Solid tumour/cancer 2A00-2F9Z Phase 1 [3]
PD173074 DMP0N4U Nasopharyngeal carcinoma 2B6B Investigative [8]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [12]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [13]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [14]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [15]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [16]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [17]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [18]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [19]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [13]
Verapamil DMA7PEW Angina pectoris BA40 Approved [20]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 2C9 (CYP2C9)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Progesterone DMUY35B Amenorrhea GA20.0 Approved [21]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [22]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [23]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [24]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [25]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [24]
Verapamil DMA7PEW Angina pectoris BA40 Approved [26]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [27]
Estrone DM5T6US Acne vulgaris ED80 Approved [28]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [29]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Cytochrome P450 3A5 (CYP3A5)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Eplerenone DMF0NQR Heart failure BD10-BD13 Approved [30]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [31]
Nelfinavir mesylate DMFX6G8 N. A. N. A. Approved [32]
Ritonavir DMU764S Human immunodeficiency virus infection 1C62 Approved [32]
Ifosfamide DMCT3I8 Adult central nervous system germ cell tumor Approved [33]
Omeprazole DM471KJ Cystic fibrosis CA25 Approved [34]
Thalidomide DM70BU5 Adult T-cell leukemia/lymphoma Approved [35]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [36]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [37]
Hydrocortisone DMGEMB7 Acne vulgaris ED80 Approved [38]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Fibroblast growth factor receptor (FGFR) TT0LF7H NOUNIPROTAC Inhibitor [1]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) Main DME DE4LYSA CP3A4_HUMAN Substrate [5]
Cytochrome P450 2C9 (CYP2C9) Main DME DE5IED8 CP2C9_HUMAN Substrate [5]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Cytochrome P450 3A5 (CYP3A5) OTSXFBXB CP3A5_HUMAN Regulation of Drug Effects [6]

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
2 ClinicalTrials.gov (NCT03210714) Erdafitinib in Treating Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphoma, or Histiocytic Disorders With FGFR Mutations (A Pediatric MATCH Treatment Trial). U.S. National Institutes of Health.
3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800036975)
5 FDA label of Erdafitinib. The 2020 official website of the U.S. Food and Drug Administration.
6 Mechanism-Based Inactivation of Cytochrome P450 3A4 and 3A5 by the Fibroblast Growth Factor Receptor Inhibitor Erdafitinib. Chem Res Toxicol. 2021 Jul 19;34(7):1800-1813. doi: 10.1021/acs.chemrestox.1c00178. Epub 2021 Jun 30.
7 TAS-120, a highly potent and selective irreversible FGFR inhibitor, is effective in tumors harboring various FGFR gene abnormalities. Molecular Cancer Therapeutics. 01/2014; 12(11_Supplement):A270-A270.
8 Tumor angiogenesis as a therapeutic target. Drug Discov Today. 2001 Oct 1;6(19):1005-1024.
9 The fibroblast growth factor receptor genetic status as a potential predictor of the sensitivity to CH5183284/Debio 1347, a novel selective FGFR inhibitor. Mol Cancer Ther. 2014 Nov;13(11):2547-58.
10 Preclinical profile of BAY 1163877 - a selective pan-FGFR inhibitor in phase 1 clinical trial. Cancer Research. 10/2014; 74(19 Supplement):1739-1739.
11 Clinical pipeline report, company report or official report of InnoCare Pharma.
12 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
13 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
14 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
15 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
16 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
17 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
18 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
19 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
20 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
21 Progesterone and testosterone hydroxylation by cytochromes P450 2C19, 2C9, and 3A4 in human liver microsomes. Arch Biochem Biophys. 1997 Oct 1;346(1):161-9.
22 Tamoxifen inhibits cytochrome P450 2C9 activity in breast cancer patients. J Chemother. 2006 Aug;18(4):421-4.
23 Characterization of the oxidative metabolites of 17beta-estradiol and estrone formed by 15 selectively expressed human cytochrome p450 isoforms. Endocrinology. 2003 Aug;144(8):3382-98.
24 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
25 Drug-drug interactions with imatinib: an observational study. Medicine (Baltimore). 2016 Oct;95(40):e5076.
26 Drug interactions with calcium channel blockers: possible involvement of metabolite-intermediate complexation with CYP3A. Drug Metab Dispos. 2000 Feb;28(2):125-30.
27 New insights into the structural features and functional relevance of human cytochrome P450 2C9. Part I. Curr Drug Metab. 2009 Dec;10(10):1075-126.
28 A potential role for the estrogen-metabolizing cytochrome P450 enzymes in human breast carcinogenesis. Breast Cancer Res Treat. 2003 Dec;82(3):191-7.
29 A mechanistic approach to antiepileptic drug interactions. Ann Pharmacother. 1998 May;32(5):554-63.
30 The relative role of CYP3A4 and CYP3A5 in eplerenone metabolism. Toxicol Lett. 2019 Oct 15;315:9-13.
31 Characterization of the structural determinants required for potent mechanism-based inhibition of human cytochrome P450 1A1 by cannabidiol. Chem Biol Interact. 2014 May 25;215:62-8.
32 Mechanism-based inactivation of CYP3A by HIV protease inhibitors. J Pharmacol Exp Ther. 2005 Feb;312(2):583-91.
33 Contribution of CYP3A5 to hepatic and renal ifosfamide N-dechloroethylation. Drug Metab Dispos. 2005 Jul;33(7):1074-81. doi: 10.1124/dmd.104.002279. Epub 2005 Apr 8.
34 Use of mRNA expression to detect the induction of drug metabolising enzymes in rat and human hepatocytes. Toxicol Appl Pharmacol. 2009 Feb 15;235(1):86-96.
35 Induction of human cytochrome P450 3A enzymes in cultured placental cells by thalidomide and relevance to bioactivation and toxicity. J Toxicol Sci. 2017;42(3):343-348.
36 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
37 Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
38 Induction of hepatic CYP3A enzymes by pregnancy-related hormones: studies in human hepatocytes and hepatic cell lines. Drug Metab Dispos. 2013 Feb;41(2):281-90.