KIN-3248: Overcoming FGFR Resistance with a Next-Generation Pan-FGFR Inhibitor

KIN-3248 (Kinnate Biopharma) is a next-generation, irreversible, pan-fibroblast growth factor receptor inhibitor (FGFRi) in a first-in-human (FIH) dose-escalation study (NCT05242822) in adults with advanced tumors harboring FGFR2 and FGFR3 gene alterations. FGFR mutations drive various cancers, and a number of pan-FGFR inhibitors have been approved, as discussed in our recent article on the first irreversible pan-FGFR inhibitor, futibatinib.

The program is an excellent case study for rational covalent drug design to address kinase mutations while maintaining sufficient PK properties for oral daily dosing in humans.