Article
RLY-4008, the First Highly Selective FGFR2 Inhibitor with Activity across FGFR2 Alterations and Resistance Mutations.
Cancer discovery - 6 Sept 2023
Subbiah Vivek, Sahai Vaibhav, Maglic Dejan, Bruderek Kamil, Touré B Barry, Zhao Songping, Valverde Roberto, O'Hearn Patrick J, Moustakas Demetri T, Schönherr Heike, Gerami-Moayed Nastaran, Taylor Alexander M, Hudson Brandi M, Houde Damian J, Pal Debjani, Foster Lindsey, Gunaydin Hakan, Ayaz Pelin, Sharon Dina A, Goyal Lipika, Schram Alison M, Kamath Suneel, Sherwin Cori Ann, Schmidt-Kittler Oleg, Jen Kai Yu, Ricard Fabien, Wolf Beni B, Shaw David E, Bergstrom Donald A, Watters James, Casaletto Jessica B
Abstract excerpt
Oncogenic activation of fibroblast growth factor receptor 2 (FGFR2) drives multiple cancers and represents a broad therapeutic opportunity, yet selective targeting of FGFR2 has not been achieved. Although the clinical efficacy of pan-FGFR inhibitors (pan-FGFRi) validates FGFR2 driver status in FGFR2 fusion-positive intrahepatic cholangiocarcinoma, their benefit is limited by incomplete target coverage due to...
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