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Details

Stereochemistry ACHIRAL
Molecular Formula C25H30N6O2
Molecular Weight 446.5447
Optical Activity UNSPECIFIED
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ERDAFITINIB

SMILES

COC1=CC(=CC(OC)=C1)N(CCNC(C)C)C2=CC=C3N=CC(=NC3=C2)C4=CN(C)N=C4

InChI

InChIKey=OLAHOMJCDNXHFI-UHFFFAOYSA-N
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

HIDE SMILES / InChI

Description

Erdafitinib (JNJ-42756493) is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. It was discovered in collaboration with Janssen Pharmaceutica, N.V. from a partnership which commenced in June 2008. Astex’s FGFr inhibitor program originated from a collaboration initiated in 2005 with the Cancer Research UK Drug Discovery Group at the Newcastle Cancer Centre (Newcastle University UK), and Cancer Research Technology Limited. JNJ42756493 is currently being evaluated by Janssen in Phase 2 clinical trials in patients with urothelial cancer, advanced hepatocellular carcinoma, advanced non-small lung cancer, esophageal cancer or cholangiocarcinoma. JNJ-42756493 is a potent, oral pan-FGFR tyrosine kinase inhibitor with half-maximal inhibitory concentration values in the low nanomolar range for all members of the FGFR family (FGFR1 to FGFR4), with minimal activity on vascular endothelial growth factor receptor (VEGFR) kinases compared with FGFR kinases (approximately 20-fold potency difference). In vitro, the proliferation of cells treated with JNJ-42756493 is decreased, associated with increased apoptotic death and decreased cell survival. It is also in phase I trials for the treatment of advanced refractory solid tumors or advanced refractory hematologic cancer.

Approval Year

PubMed

PubMed

TitleDatePubMed
Oncogenic Characterization and Pharmacologic Sensitivity of Activating Fibroblast Growth Factor Receptor (FGFR) Genetic Alterations to the Selective FGFR Inhibitor Erdafitinib.
2017 Aug
RACK1 forms a complex with FGFR1 and PKM2, and stimulates the growth and migration of squamous lung cancer cells.
2017 Nov
Safety, pharmacokinetic, and pharmacodynamics of erdafitinib, a pan-fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitor, in patients with advanced or refractory solid tumors.
2018 Jun
Patents

Patents

Sample Use Guides

In Vivo Use Guide
Cancer patients will receive a 8 milligram (mg) starting dose once daily with option to up-titrate to 9 mg on a 28-day cycle.
Route of Administration: Oral
In Vitro Use Guide
Erdafitinib (JNJ-42756493) effectively inhibited pFGFR1, pFGFR3 and pFGFR4 at 100nM in NCI-H1581, KMS-11 and MDA-MB-453 cells, respectively, and pFGFR2 at 30nM in SNU-16 cells. Inhibition of FGFR auto-phosphorylation was consistent with its antiproliferative IC50s in these cell lines (2.6, 0.40, 102.4, and 129.2 nM, for NCI-H1581, SNU-16, KMS-11 and MDA-MB-453, respectively)
Name Type Language
ERDAFITINIB
INN   USAN   WHO-DD  
USAN   INN  
Official Name English
ERDAFITINIB [INN]
Common Name English
ERDAFITINIB [USAN]
Common Name English
JNJ-42756493
Code English
ERDAFITINIB [WHO-DD]
Common Name English
1,2-ETHANEDIAMINE, N1-(3,5-DIMETHOXYPHENYL)-N2-(1-METHYLETHYL)-N1-(3-(1-METHYL-1H-PYRAZOL-4-YL)-6-QUINOXALINYL)-
Systematic Name English
Code System Code Type Description
NCI_THESAURUS
C103273
Created by admin on Tue Mar 06 11:01:58 UTC 2018 , Edited by admin on Tue Mar 06 11:01:58 UTC 2018
PRIMARY
CAS
1346242-81-6
Created by admin on Tue Mar 06 11:01:58 UTC 2018 , Edited by admin on Tue Mar 06 11:01:58 UTC 2018
PRIMARY
INN
10147
Created by admin on Tue Mar 06 11:01:58 UTC 2018 , Edited by admin on Tue Mar 06 11:01:58 UTC 2018
PRIMARY
ChEMBL
CHEMBL3545376
Created by admin on Tue Mar 06 11:01:58 UTC 2018 , Edited by admin on Tue Mar 06 11:01:58 UTC 2018
PRIMARY
CAS
1620332-47-9
Created by admin on Tue Mar 06 11:01:58 UTC 2018 , Edited by admin on Tue Mar 06 11:01:58 UTC 2018
NO STRUCTURE GIVEN
PUBCHEM
67462786
Created by admin on Tue Mar 06 11:01:58 UTC 2018 , Edited by admin on Tue Mar 06 11:01:58 UTC 2018
PRIMARY SWITZERF