Resigratinib

Resigratinib (KIN-3248) is a next-generation, selective, irreversible small molecule inhibitor of fibroblast growth factor receptors (FGFRs), specifically designed to target oncogenic alterations in FGFR2 and FGFR3. These genetic alterations are key drivers in a significant subset of cholangiocarcinoma and urothelial cancers. Resigratinib exhibits potent inhibitory activity against both primary driver mutations and secondary kinase domain mutations that confer resistance to currently approved FGFR inhibitors. The drug is orally bioavailable and has demonstrated efficacy in preclinical models with acquired resistance to other FGFR inhibitors. It is being developed by Kinnate Biopharma for the treatment of advanced solid tumors harboring FGFR2 and/or FGFR3 gene alterations, including unresectable or metastatic cholangiocarcinoma (CCA) and urothelial carcinoma (UC). In February 2023, it received FDA Fast Track designation for CCA with FGFR2 gene fusions or other alterations[1][2][5][6][7].

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