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futibatinib
- Development stage
- Approved
- Lead developer
- Taiho Pharmaceutical
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Futibatinib is a small molecule, oral kinase inhibitor used to treat adults with previously treated, unresectable, locally advanced or metastatic intrahepatic cholangiocarcinoma (bile duct cancer within the liver) harboring fibroblast growth factor receptor 2 (FGFR2) gene fusions or other rearrangements. It acts as a selective and irreversible inhibitor of FGFR1, FGFR2, FGFR3, and FGFR4 by covalently binding to the kinase domain at cysteine residues in the ATP-binding pocket. This blocks phosphorylation of FGFRs and downstream signaling pathways such as MAPK, PI3K/Akt/mTOR, PLCγ, and JAK/STAT—ultimately inhibiting cell proliferation in tumors with FGFR alterations. Futibatinib is approved under accelerated approval based on response rate and duration of response; continued approval may depend on confirmatory trials demonstrating clinical benefit. The drug was developed by Taiho Pharmaceutical[1][5][7][8].
- Brand names
- Lytgobi
- Other names
- futibatinibTAS-120TAS120TAS 120Lytgobi
02
Targets
FGFR4 (Fibroblast growth factor receptor 4)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)FGFR1 (Fibroblast growth factor receptor 1)
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