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Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor

Perera, Timothy P.S., Jovcheva, Eleonora, Mevellec, Laurence, Vialard, Jorge, De Lange, Desiree, Verhulst, Tinne, Paulussen, Caroline, Van De Ven, Kelly, King, Peter, Freyne, Eddy, Rees, David C., Squires, Matthew, Saxty, Gordon, Page, Martin, Murray, Christopher W., Gilissen, Ron, Ward, George, Thompson, Neil T., Newell, Herbie, Cheng, Na, Xie, Liang, Yang, Jennifer, Platero, Suso J., Karkera, Jayaprakash D., Moy, Christopher, Angibaud, Patrick, Laquerre, Sylvie and Lorenzi, Matthew V. (2017) Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor. Molecular Cancer Therapeutics, 16 (6). pp. 1010-1020. ISSN 1535-7163

Item Type: Article


©2017 American Association for Cancer Research. 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.

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Depositing User: Michelle Marshall


Item ID: 11053
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ISSN: 1535-7163
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Date Deposited: 21 Aug 2019 15:23
Last Modified: 20 Jan 2023 10:09


Author: Timothy P.S. Perera
Author: Eleonora Jovcheva
Author: Laurence Mevellec
Author: Jorge Vialard
Author: Desiree De Lange
Author: Tinne Verhulst
Author: Caroline Paulussen
Author: Kelly Van De Ven
Author: Peter King
Author: Eddy Freyne
Author: David C. Rees
Author: Matthew Squires
Author: Gordon Saxty
Author: Martin Page
Author: Christopher W. Murray
Author: Ron Gilissen
Author: George Ward
Author: Neil T. Thompson
Author: Herbie Newell
Author: Na Cheng
Author: Liang Xie
Author: Jennifer Yang
Author: Suso J. Platero
Author: Jayaprakash D. Karkera
Author: Christopher Moy
Author: Patrick Angibaud
Author: Sylvie Laquerre
Author: Matthew V. Lorenzi

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Faculty of Health Sciences and Wellbeing



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