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Ref Type Journal Article
PMID (28341788)
Authors Perera TPS, Jovcheva E, Mevellec L, Vialard J, De Lange D, Verhulst T, Paulussen C, Van De Ven K, King P, Freyne E, Rees DC, Squires M, Saxty G, Page M, Murray CW, Gilissen R, Ward G, Thompson NT, Newell DR, Cheng N, Xie L, Yang J, Platero SJ, Karkera JD, Moy C, Angibaud P, Laquerre S, Lorenzi MV
Title Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor.
Journal Molecular cancer therapeutics
Vol 16
Issue 6
Date 2017 Jun
URL
Abstract Text Fibroblast growth factor (FGF) signaling plays critical roles in key biological processes ranging from embryogenesis to wound healing and has strong links to several hallmarks of cancer. Genetic alterations in FGF receptor (FGFR) family members are associated with increased tumor growth, metastasis, angiogenesis, and decreased survival. JNJ-42756493, erdafitinib, is an orally active small molecule with potent tyrosine kinase inhibitory activity against all four FGFR family members and selectivity versus other highly related kinases. JNJ-42756493 shows rapid uptake into the lysosomal compartment of cells in culture, which is associated with prolonged inhibition of FGFR signaling, possibly due to sustained release of the inhibitor. In xenografts from human tumor cell lines or patient-derived tumor tissue with activating FGFR alterations, JNJ-42756493 administration results in potent and dose-dependent antitumor activity accompanied by pharmacodynamic modulation of phospho-FGFR and phospho-ERK in tumors. The results of the current study provide a strong rationale for the clinical investigation of JNJ-42756493 in patients with tumors harboring FGFR pathway alterations. Mol Cancer Ther; 16(6); 1010-20. ©2017 AACR.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Erdafitinib Erdafitinib 59 8
Drug Name Trade Name Synonyms Drug Classes Drug Description
Erdafitinib Balversa JNJ-42756493 FGFR Inhibitor (Pan) 18 Balversa (erdafitinib) selectively inhibits FGFR1-4, resulting in decreased downstream signaling, and potentially leading to reduced growth of tumors with activated FGFR signaling (PMID: 28341788, PMID: 28965185). Balversa (erdafitinib) is FDA approved for use in patients with locally advanced or metastatic urothelial carcinoma with susceptible FGFR3 or FGFR2 genetic alterations (FDA.gov).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
FGFR1 amp lung cancer predicted - sensitive Erdafitinib Preclinical - Cell line xenograft Actionable In a preclinical study, Balversa (erdafitinib) inhibited FGFR downstream signaling and proliferation of several lung cancer cell lines with FGFR1 amplification in culture, and inhibited tumor growth in an FGFR1-amplified lung cancer cell line xenograft model (PMID: 28341788). 28341788
FGFR2 amp stomach cancer sensitive Erdafitinib Preclinical - Cell line xenograft Actionable In a preclinical study, Balversa (erdafitinib) inhibited proliferation of a gastric cancer cell line with FGFR2 amplification in culture, and inhibited tumor growth in xenograft models (PMID: 28341788). 28341788
FGFR2 amp colorectal cancer sensitive Erdafitinib Preclinical - Cell line xenograft Actionable In a preclinical study, Balversa (erdafitinib) inhibited tumor growth in an FGFR2-amplified colorectal cancer cell line xenograft model (PMID: 28341788). 28341788
FGFR3 - TACC3 lung non-small cell carcinoma sensitive Erdafitinib Preclinical - Pdx Actionable In a preclinical study, Balversa (erdafitinib) inhibited pERK signaling and tumor growth in a patient-derived xenograft (PDX) model of non-small cell lung cancer harboring FGFR3-TACC3 (PMID: 28341788). 28341788