ERDAFITINIB

Details

Stereochemistry	ACHIRAL
Molecular Formula	C25H30N6O2
Molecular Weight	446.5447
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

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

Molecular Formula	C25H30N6O2
Molecular Weight	446.5447
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://astx.com/research-development/partnered-products-and-programs/jnj42756493-erdafitinib-fgfr-inhibitor-oncology/ | https://www.ncbi.nlm.nih.gov/pubmed/28965185 | https://www.ncbi.nlm.nih.gov/pubmed/28341788

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.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Fibroblast growth factor receptor 1 46 Target ID: CHEMBL3650 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28341788	Antagonist 2849	1.2 nM [IC50]
Fibroblast growth factor receptor 2 25 Target ID: CHEMBL4142 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28341788	Antagonist 2849	2.5 nM [IC50]
Fibroblast growth factor receptor 3 32 Target ID: CHEMBL2742 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28341788	Antagonist 2849	3.0 nM [IC50]
Fibroblast growth factor receptor 4 16 Target ID: CHEMBL3973 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28341788	Antagonist 2849	5.7 nM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Cholangiocarcinoma 18 Sources: https://clinicaltrials.gov/ct2/show/NCT02699606 http://adisinsight.springer.com/drugs/800036975	Primary	Phase II 1147	Unknown Approved Use Unknown
Advanced non-small cell lung cancer 4 Sources: https://clinicaltrials.gov/ct2/show/NCT02699606 http://adisinsight.springer.com/drugs/800036975	Primary	Phase II 1147	Unknown Approved Use Unknown
Esophageal cancer 12 Sources: https://clinicaltrials.gov/ct2/show/NCT02699606 http://adisinsight.springer.com/drugs/800036975	Primary	Phase II 1147	Unknown Approved Use Unknown
Non-Hodgkin's lymphoma 81 Sources: https://clinicaltrials.gov/ct2/show/NCT03210714	Primary	Phase II 1147	Unknown Approved Use Unknown
Cancer 609 Sources: https://clinicaltrials.gov/ct2/show/NCT03210714 http://adisinsight.springer.com/drugs/800036975	Primary	Phase II 1147	Unknown Approved Use Unknown

C_max

Value	Dose	Co-administered	Analyte	Population
1399 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf	8 mg 1 times / day steady-state, oral dose: 8 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		ERDAFITINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
29268 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf	8 mg 1 times / day steady-state, oral dose: 8 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		ERDAFITINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
59 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf	8 mg 1 times / day steady-state, oral dose: 8 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		ERDAFITINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
0.2% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf	8 mg 1 times / day steady-state, oral dose: 8 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		ERDAFITINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
12 mg 1 times / day multiple, oral Highest studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28965185/	unhealthy, 62.7 years Health Status: unhealthy Age Group: 62.7 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/28965185/	DLT: Retinal pigment epithelium atrophy... Dose limiting toxicities: Retinal pigment epithelium atrophy (grade 2, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/28965185/
10 mg 1 times / day multiple, oral RP2D Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28965185/	unhealthy, 65.7 years Health Status: unhealthy Age Group: 65.7 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/28965185/	Other AEs: Hyperphosphatemia... Other AEs: Hyperphosphatemia (3 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/28965185/
12 mg 1 times / day multiple, oral Highest studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/26324363/	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://pubmed.ncbi.nlm.nih.gov/26324363/	DLT: Alanine aminotransferase increase... Dose limiting toxicities: Alanine aminotransferase increase (grade 3, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/26324363/
12 mg 1 times / day steady, oral Highest studied dose Dose: 12 mg, 1 times / day Route: oral Route: steady Dose: 12 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf
8 mg 1 times / day steady, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: steady Dose: 8 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf	Other AEs: Stomatitis, Diarrhea... Other AEs: Stomatitis (all grades, 56%) Diarrhea (all grades, 47%) Dry mouth (all grades, 45%) Constipation (all grades, 28%) Abdominal pain (all grades, 23%) Nausea (all grades, 21%) Vomiting (all grades, 13%) Decreased appetite (all grades, 38%) Fatigue (all grades, 54%) Pyrexia (all grades, 14%) Onycholysis (all grades, 41%) Dry skin (all grades, 34%) Palmar-plantar erythrodysaesth. (all grades, 26%) Alopecia (all grades, 26%) Nail discoloration (all grades, 11%) Dry eye (all grades, 28%) Vision blurred (all grades, 17%) Lacrimation increased (all grades, 10%) Dysgeusia (all grades, 37%) Paronychia (all grades, 17%) Urinary tract infection (all grades, 17%) Conjunctivitis (all grades, 11%) Oropharyngeal pain (all grades, 11%) Dyspnea (all grades, 10%) Hematuria (all grades, 11%) Musculoskeletal pain (all grades, 20%) Arthralgia (all grades, 11%) Weight decreased (all grades, 16%) Stomatitis (grade 3-4, 9%) Diarrhea (grade 3-4, 2%) Constipation (grade 3-4, 1%) Abdominal pain (grade 3-4, 2%) Nausea (grade 3-4, 1%) Vomiting (grade 3-4, 2%) Fatigue (grade 3-4, 10%) Pyrexia (grade 3-4, 1%) Onycholysis (grade 3-4, 10%) Palmar-plantar erythrodysaesth. (grade 3-4, 6%) Dry eye (grade 3-4, 6%) Dysgeusia (grade 3-4, 1%) Paronychia (grade 3-4, 3%) Urinary tract infection (grade 3-4, 6%) Oropharyngeal pain (grade 3-4, 1%) Dyspnea (grade 3-4, 2%) Hematuria (grade 3-4, 2%) Gastrointestinal disorders (all grades, 94%) Metabolism and nutrition disorders (all grades, 90%) Skin and subcutaneous tissue disorders (all grades, 75%) Eye disorders (all grades, 62%) Nervous system disorders (all grades, 57%) Infections and infestations (all grades, 56%) Respiratory, thoracic and mediastinal disorders (all grades, 40%) Renal and urinary disorders (all grades, 38%) Musculoskeletal and connective tissue disorders (all grades, 31%) Gastrointestinal disorders (grade 3-4, 24%) Metabolism and nutrition disorders (grade 3-4, 16%) Skin and subcutaneous tissue disorders (grade 3-4, 16%) Eye disorders (grade 3-4, 11%) Nervous system disorders (grade 3-4, 5%) Infections and infestations (grade 3-4, 20%) Respiratory, thoracic and mediastinal disorders (grade 3-4, 7%) Renal and urinary disorders (grade 3-4, 10%) Hemoglobin decreased (all grades, 35%) Platelets decreased (all grades, 19%) Leukocyte count decreased (all grades, 17%) Neutrophil count decreased (all grades, 10%) Phosphate increased (all grades, 76%) Creatinine increased (all grades, 52%) Sodium decreased (all grades, 40%) Alanine aminotransferase increased (all grades, 41%) Alkaline phosphatase increased (all grades, 41%) Albumin decreased (all grades, 37%) Aspartate aminotransferase increased (all grades, 30%) Magnesium decreased (all grades, 30%) Phosphate decreased (all grades, 24%) Calcium increased (all grades, 22%) Potassium increased (all grades, 16%) Fasting blood glucose increased (all grades, 10%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf
8 mg 1 times / day steady, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: steady Dose: 8 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf	Other AEs: Hemoglobin decreased, Platelets decreased... Other AEs: Hemoglobin decreased (grade 3-4, 3%) Platelets decreased (grade 3-4, 1%) Neutrophil count decreased (grade 3-4, 2%) Phosphate increased (grade 3-4, 1%) Creatinine increased (grade 3-4, 5%) Sodium decreased (grade 3-4, 16%) Alanine aminotransferase increased (grade 3-4, 1%) Alkaline phosphatase increased (grade 3-4, 1%) Magnesium decreased (grade 3-4, 1%) Phosphate decreased (grade 3-4, 9%) Calcium increased (grade 3-4, 3%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf
8 mg 1 times / day steady, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: steady Dose: 8 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf	Disc. AE: Acute myocardial infarction, Eye disorders... Other AEs: Hyperphosphatemia, Stomatitis... AEs leading to discontinuation/dose reduction: Acute myocardial infarction (grade 5, 1%) Eye disorders (6%) Other AEs: Hyperphosphatemia (24%) Stomatitis (17%) Eye disorders (17%) Palmar-plantar erythrodysaesthesia syndrome (8%) Eye disorders (23%) Stomatitis (15%) Hyperphosphatemia (7%) Palmar-plantar erythrodysaesthesia syndrome (7%) Paronychia (7%) Nail dystrophy (6%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inducer 1087	inhibitor 2438 substrate 1193	inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 2153 CYP2C19 2057 CYP3A 227 OCT2 779 P-gp 1741	CYP3A 220 P-gp 2052	CYP1A2 832 CYP2B6 669

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf#page=14 Page: (label) 14	likely
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=54 Page: 53.0	no
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=54 Page: 53.0	no
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=54 Page: 53.0	no
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=54 Page: 53.0	no
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=54 Page: 53.0	no
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=54 Page: 53.0	no
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=54 Page: 53.0	weak
OCT2 782	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=87; https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf#page=9 Page: 86, 98, (label) 9	yes
CYP3A 317	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=98; https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf#page=14 Page: 97, (label) 14	yes	likely (co-administration study) Comment: Time-dependent inhibitor, Concomitant CYP3A substrates with narrow therapeutic index should be avoided.; Erdafitinib mean ratios (90% CI) for Cmax and AUCinf were 105% (86.7, 127) and 134% (109, 164), respectively, when co-administered with itraconazole (a strong CYP3A4 inhibitor and P-gp inhibitor) relative to erdafitinib alone. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=98; https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf#page=14 Page: 97, (label) 14

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP2C9 1193	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=96 Page: 82, 95, 96	major	yes (co-administration study) Comment: Concomitant fluconazole (moderate CYP2C9/moderate CYP3A inhibitor, 400 mg QD for 11 days) increased erdafitinib (4 mg single dose on Day 5) AUC by 48% and Cmax by 21% (fasted, healthy subjects with CYP2C91/1, 1/2 genotypes). The contribution of CYP2C9 in the total clearance of erdafitinib isestimated to be 39%. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=96 Page: 82, 95, 96
CYP3A 220	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=96 Page: 82, 95, 96	major	yes (co-administration study) Comment: Concomitant itraconazole (strong CYP3A/P-gp inhibitor, 200 mg QD for 11 days) increased erdafitinib (4 mg single dose on Day 5) AUC by 34% but did not significantly change Cmax (5%)(fasted, healthy subjects with CYP2C91/1, 1/2 genotypes). The contribution of CYP3A in the total clearance of erdafitinib is estimated to be 20%. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=96 Page: 82, 95, 96
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=96 Page: 95, 96	yes	yes (co-administration study) Comment: Concomitant itraconazole (strong CYP3A/P-gp inhibitor, 200 mg QD for 11 days) increased erdafitinib (4 mg single dose on Day 5) AUC by 34% but did not significantly change Cmax (5%)(fasted, healthy subjects with CYP2C91/1, 1/2 genotypes). The contribution of CYP3A in the total clearance of erdafitinib is estimated to be 20%. Erdafinitib dosse should be separated by >/= 6 h befor or after administration of P-gp substrates with narrow therapeutic index. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=96 Page: 95, 96

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=36 Page: 35.0

Sourcing

Vendor/Aggregator	ID	URL
AA Blocks	AA009CF1	https://www.aablocks.com/goods/Goods/detail?id=AA009CF1
Aaron Chemicals	AR009D6T	http://www.aaronchem.com/1346242-81-6
abcr GmbH	AB478989	http://www.abcr.com/shop/en/AB478989
AbMole Bioscience	M9715	http://www.abmole.com/products/erdafitinib.html
Adooq BioScience	A15957	https://www.adooq.com/erdafitinib.html
Ambinter	Amb24087498	http://www.ambinter.com/reference/24087498
Angel Pharmatech	AG-10606	http://www.angelpharmatech.com/1346242-81-6.html
Ark Pharm	AK547250	http://www.arkpharminc.com/products/1346242-81-6.html
Ark Pharma Scientific Limited	H-026579	http://www.arkpharmtech.com/product/31632.html
BioChemPartner	BCP20346	http://www.biochempartner.com/1346242-81-6-BCP20346
BOC Sciences	1346242-81-6	https://www.bocsci.com/erdafitinib-cas-1346242-81-6-item-470835.html
Chem Scene	CS-4988	http://www.chemscene.com/1346242-81-6.html
Chemspace	CSSB00025704501	https://chem-space.com/CSSB00025704501
DC Chemicals	DC11387	http://www.dcchemicals.com/product_show-Erdafitinib.html
eNovation Chemicals	D640591	https://www.enovationchem.com/ProductDetails.asp?ProductID=D640591
eNovation Chemicals	Y1002414	https://www.enovationchem.com/ProductDetails.asp?ProductID=Y1002414
Excenen	EX-A2564	https://www.excenen.com/searchresultlist.php?id=1346242-81-6
Lab Network	LN01343567	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01343567
MedChem Express	HY-18708	https://www.medchemexpress.com/Erdafitinib.html
Smolecule	S527360	http://www.smolecule.com/products/s527360
Synblock Inc	SB16854	http://www.synblock.com/product/1346242-81-6.html
THE BioTek	bt-267626	https://www.thebiotek.com/product/inhibitors/bt-267626

PubMed

Title	Date	PubMed
Safety, pharmacokinetic, and pharmacodynamics of erdafitinib, a pan-fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitor, in patients with advanced or refractory solid tumors.	2018-06	28965185
RACK1 forms a complex with FGFR1 and PKM2, and stimulates the growth and migration of squamous lung cancer cells.	2017-11	28418088
Oncogenic Characterization and Pharmacologic Sensitivity of Activating Fibroblast Growth Factor Receptor (FGFR) Genetic Alterations to the Selective FGFR Inhibitor Erdafitinib.	2017-08	28416604

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)

Substance Class	Chemical Created by `admin` on `Wed Apr 02 09:06:02 GMT 2025` Edited by `admin` on `Wed Apr 02 09:06:02 GMT 2025`
Record UNII	890E37NHMV
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ERDAFITINIB

Official Name

English

erdafitinib [INN]

Preferred Name

English

PAN-FGFR TYROSINE KINASE INHIBITOR JNJ-42756493

Common Name

English

BALVERSA

Brand Name

English

ERDAFITINIB [MI]

Common Name

English

ERDAFITINIB [ORANGE BOOK]

Common Name

English

ERDAFITINIB [JAN]

Common Name

English

ERDAFITINIB [USAN]

Common Name

English

Erdafitinib [WHO-DD]

Common Name

English

JNJ-42756493

Code

English

1,2-ETHANEDIAMINE, N1-(3,5-DIMETHOXYPHENYL)-N2-(1-METHYLETHYL)-N1-(3-(1-METHYL-1H-PYRAZOL-4-YL)-6-QUINOXALINYL)-

Systematic Name

English

Classification Tree Code System Code

NCI_THESAURUS

C1967