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

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 45 Target ID: CHEMBL3650 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28341788	Antagonist 2778	1.2 nM [IC50]
Fibroblast growth factor receptor 2 25 Target ID: CHEMBL4142 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28341788	Antagonist 2778	2.5 nM [IC50]
Fibroblast growth factor receptor 3 32 Target ID: CHEMBL2742 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28341788	Antagonist 2778	3.0 nM [IC50]
Fibroblast growth factor receptor 4 16 Target ID: CHEMBL3973 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28341788	Antagonist 2778	5.7 nM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Cholangiocarcinoma 17 Sources: https://clinicaltrials.gov/ct2/show/NCT02699606 http://adisinsight.springer.com/drugs/800036975	Primary	Phase II 1132	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 1132	Unknown Approved Use Unknown
Esophageal cancer 12 Sources: https://clinicaltrials.gov/ct2/show/NCT02699606 http://adisinsight.springer.com/drugs/800036975	Primary	Phase II 1132	Unknown Approved Use Unknown
Non-Hodgkin's lymphoma 79 Sources: https://clinicaltrials.gov/ct2/show/NCT03210714	Primary	Phase II 1132	Unknown Approved Use Unknown
Cancer 592 Sources: https://clinicaltrials.gov/ct2/show/NCT03210714 http://adisinsight.springer.com/drugs/800036975	Primary	Phase II 1132	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 n = 7 Health Status: unhealthy Condition: Cancer Age Group: 62.7 years Sex: M+F Population Size: 7 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 n = 3 Health Status: unhealthy Condition: Cancer Age Group: 65.7 years Sex: M+F Population Size: 3 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 n = 13 Health Status: unhealthy Condition: solid tumors Age Group: adult Sex: unknown Population Size: 13 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 Page: 84	unhealthy, adult n = 7 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 7 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf Page: 84	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf Page: 84
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 Page: 6.1	unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf Page: 6.1	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 Page: 6.1
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 Page: Table 3	unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf Page: Table 3	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 Page: Table 3
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 Page: Table 4	unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf Page: Table 4	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 Page: Table 4

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inducer 781	inhibitor 1767 substrate 1037	inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 1524 CYP2C19 1478 CYP3A 214 OCT2 647 P-gp 1461	CYP3A 191 P-gp 1537	CYP1A2 701 CYP2B6 547

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf#page=14 Page: (label) 14	likely
CYP1A2 1692	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=54 Page: 53.0	no
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=54 Page: 53.0	no
CYP2B6 1001	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=54 Page: 53.0	no
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=54 Page: 53.0	no
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=54 Page: 53.0	no
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=54 Page: 53.0	no
CYP3A4 1925	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=54 Page: 53.0	weak
OCT2 648	inhibitor 3277 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 298	inhibitor 3277 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 1037	substrate 3367 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 191	substrate 3367 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 1537	substrate 3367 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 1647	inhibitor 1626 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
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
BOC Sciences	1346242-81-6	https://www.bocsci.com/erdafitinib-cas-1346242-81-6-item-470835.html
BioChemPartner	BCP20346	http://www.biochempartner.com/1346242-81-6-BCP20346
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
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
abcr GmbH	AB478989	http://www.abcr.com/shop/en/AB478989
eNovation Chemicals	D640591	https://www.enovationchem.com/ProductDetails.asp?ProductID=D640591
eNovation Chemicals	Y1002414	https://www.enovationchem.com/ProductDetails.asp?ProductID=Y1002414

PubMed

Title	Date	PubMed
Oncogenic Characterization and Pharmacologic Sensitivity of Activating Fibroblast Growth Factor Receptor (FGFR) Genetic Alterations to the Selective FGFR Inhibitor Erdafitinib.	2017 Aug	28416604
RACK1 forms a complex with FGFR1 and PKM2, and stimulates the growth and migration of squamous lung cancer cells.	2017 Nov	28418088
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	28965185

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

Official 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 [INN]

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