Details of the Drug

General Information of Drug (ID: DMI782S)

Drug Name
Erdafitinib
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]
Affected Organisms
Humans and other mammals
ATC Code
L01EN01: Erdafitinib
L01EN: Fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitors
L01E: PROTEIN KINASE INHIBITORS
L01: ANTINEOPLASTIC AGENTS
L: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 446.5
Logarithm of the Partition Coefficient (xlogp) 3.2
Rotatable Bond Count (rotbonds) 9
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 7
ADMET Property
Absorption AUC
The area under the plot of plasma concentration (AUC) of drug is 29,268 mcgh/L []
Absorption Cmax
The maximum plasma concentration (Cmax) of drug is 1,399 mcg/L []
Clearance
The apparent oral clearance of drug is 0.362 L/h [5]
Elimination
About 69% of the dose was recovered in feces (19% as unchanged) and 19% in urine (13% as unchanged) []
Half-life
The concentration or amount of drug in body reduced by one-half in 59 hours [5]
Metabolism
The drug is metabolized via the cytochrome P450 enzym CYP2C9 and CYP3A4 isoenzymes []
Vd
The volume of distribution (Vd) of drug is 26-29 L [5]
Chemical Identifiers
Formula
C25H30N6O2
IUPAC Name
N'-(3,5-dimethoxyphenyl)-N'-[3-(1-methylpyrazol-4-yl)quinoxalin-6-yl]-N-propan-2-ylethane-1,2-diamine
Canonical SMILES
CC(C)NCCN(C1=CC2=NC(=CN=C2C=C1)C3=CN(N=C3)C)C4=CC(=CC(=C4)OC)OC
InChI
InChI=1S/C25H30N6O2/c1-17(2)26-8-9-31(20-10-21(32-4)13-22(11-20)33-5)19-6-7-23-24(12-19)29-25(15-27-23)18-14-28-30(3)16-18/h6-7,10-17,26H,8-9H2,1-5H3
InChIKey
OLAHOMJCDNXHFI-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
67462786
ChEBI ID
CHEMBL3545376
CAS Number
1346242-81-6
UNII
890E37NHMV
DrugBank ID
DB12147
TTD ID
D0NW0T
INTEDE ID
DR0595
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Molecular Interaction Atlas of This Drug


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 [6]
Cytochrome P450 2C9 (CYP2C9)
Main DME 		DE5IED8 CP2C9_HUMAN Substrate [6]
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Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Erdafitinib (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Ivosidenib DM8S6T7 Moderate Increased metabolism of Erdafitinib caused by Ivosidenib mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [7]
Oliceridine DM6MDCF Moderate Increased metabolism of Erdafitinib caused by Oliceridine mediated induction of CYP450 enzyme. Acute pain [MG31] [7]
Troleandomycin DMUZNIG Major Decreased metabolism of Erdafitinib caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [7]
Eslicarbazepine DMZREFQ Major Increased plasma concentrations of Erdafitinib and Eslicarbazepine due to competitive inhibition of the same metabolic pathway. Epilepsy/seizure [8A61-8A6Z] [7]
Bay 80-6946 DMLOS5R Moderate Increased metabolism of Erdafitinib caused by Bay 80-6946 mediated induction of CYP450 enzyme. Follicular lymphoma [2A80] [7]
Rucaparib DM9PVX8 Moderate Decreased clearance of Erdafitinib due to the transporter inhibition by Rucaparib. Ovarian cancer [2C73] [7]
Betrixaban DM2C4RF Moderate Decreased clearance of Erdafitinib due to the transporter inhibition by Betrixaban. Venous thromboembolism [BD72] [7]
⏷ Show the Full List of 7 DDI Information of This Drug

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 Phase I Dose-Escalation Study of JNJ-42756493, an Oral Pan-Fibroblast Growth Factor Receptor Inhibitor, in Patients With Advanced Solid Tumors. J Clin Oncol. 2015 Oct 20;33(30):3401-8. doi: 10.1200/JCO.2014.60.7341. Epub 2015 Aug 31.
6 FDA label of Erdafitinib. The 2020 official website of the U.S. Food and Drug Administration.
7 Product Information. Balversa (erdafitinib). Janssen Products, LP, Horsham, PA.