lirafugratinib

Lirafugratinib is an orally bioavailable, highly selective small molecule inhibitor of fibroblast growth factor receptor 2 (FGFR2), a receptor tyrosine kinase frequently altered in certain cancers. It was designed to selectively inhibit FGFR2 while sparing other closely related FGFR family members, thereby reducing off-target toxicities commonly seen with pan-FGFR inhibitors. Lirafugratinib binds covalently to FGFR2 and blocks its signal transduction pathways, inhibiting the proliferation of tumor cells that overexpress or harbor alterations in FGFR2. The drug has demonstrated robust antitumor activity and high objective response rates in early clinical studies for patients with intrahepatic cholangiocarcinoma harboring FGFR2 fusions, as well as promising efficacy across other solid tumors with various types of FGFR2 alterations (fusions/rearrangements, amplifications, mutations). Lirafugratinib is being developed by Relay Therapeutics and Elevar Therapeutics and is currently under investigation in global Phase 1/2 trials for advanced or metastatic solid tumors driven by FGFR2 alterations[1][3][4][5][6][7][8].

Other names

lirafugratinib