futibatinib

Overview

Futibatinib is a covalent, irreversible pan-FGFR inhibitor targeting FGFR1, FGFR2, FGFR3, and FGFR4. Unlike reversible FGFR inhibitors (pemigatinib, infigratinib), its covalent mechanism of action retains activity against secondary kinase-domain resistance mutations that commonly emerge on reversible agents. Approved for FGFR2 fusion/rearrangement-positive intrahepatic cholangiocarcinoma (iCCA) based on the FOENIX-CCA2 phase II trial.

Evidence in the corpus

  • FGFR2 fusion/rearrangement-positive iCCA: FOENIX-CCA2 phase II ORR 42.0%, mPFS 9.0 mo, mOS 21.7 mo; as a covalent irreversible FGFR inhibitor it retains activity against on-target secondary FGFR2 kinase-domain resistance mutations (N550, V565) that emerge under reversible inhibitors PMID:25526346
  • Cited as an FGFR2-targeted agent that synergizes with cisplatin in FGFR2-rearranged iCCA, proposed as a backbone for combination strategies in cholangiocarcinoma treatment PMID:25608663

Resistance mechanisms

  • Secondary FGFR2 kinase-domain mutations (N550, V565) that confer resistance to reversible inhibitors (pemigatinib, infigratinib) may remain sensitive to futibatinib due to its covalent mechanism PMID:25526346

Cancer types (linked)

Sources

This page was processed by crosslinker on 2026-05-14. - PMID:25608663

This page was processed by crosslinker on 2026-05-14.