A Newly Approved Alkyne: Covalent FGFR1-4 Kinase Inhibitor, Futibatinib

Futibatinib (Lytgobi) is a rare alkyne-containing, irreversible FGFR1-4 inhibitor that received accelerated approval from the FDA in September 2022. Structurally distinct from other approved FGFR2/3 inhibitors, futibatinib treats a range of FGFR-aberrant tumors, including those with fusions or TKI-resistant mutants like the V565I/L gatekeeper mutation.

This Premium report reviews:

  • the role of FGFR mutations in oncogenesis and drug resistance
  • differences between approved and emerging FGFR inhibitors
  • human data on futibatinib, including PK and efficacy

See our overview of all 36 of the novel small molecule and large molecule FDA approvals for 2022 here.

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