Futibatinib is a kinase inhibitor used to treat intrahepatic cholangiocarcinoma in previously treated adults. Futibatinib is an inhibitor of Fibroblast Growth Factor receptor (FGFR), which comprises a group of receptor tyrosine kinases that play a key role in cell proliferation, differentiation, migration, and survival.
- Mechanism
- Curator reviewed · 9 references
Fibroblast Growth Factor receptor (FGFR) pathway play a key role in cell proliferation, differentiation, migration, and survival. Notably, FGFR genomic aberrations and aberrant FGFR signalling pathways are observed in some cancers, as constitutive FGFR signalling can support the proliferation and survival of malignant cells.
Futibatinib is a selective, irreversible inhibitor of FGFR 1, 2, 3, and 4 with IC50 values of less than 4 nM. It binds to the FGFR kinase domain by forming a covalent bond with cysteine in the ATP-binding pocket. Upon binding to FGFR, futibatinib blocks FGFR phosphorylation and downstream signalling pathways, such as the RAS-dependent mitogen-activated protein kinase (MAPK), phosphatidylinositol 3-kinase (PI3KCA)/Akt/mTOR, phospholipase Cγ (PLCγ), and JAK/STAT. Futibatinib ultimately decreases cell viability in cancer cell lines with FGFR alterations, including FGFR fusions or rearrangements, amplifications, and mutations.
- Primary indication
- Futibatinib is indicated to treat adults with previously treated, unresectable, locally advanced or metastatic intrahepatic cholangiocarcinoma harbouring fibroblast growth factor receptor 2 (FGFR2) gene fusions or other rearrangements.Curator reviewed · 5 structured indications
- Formula / weight
- C22H22N6O3 · 418.457 g/mol (avg)
- First approval
- United States, 2023 · European Union, 2023
- Code names
- TAS-120
- Brand names
Resolves to
KEIPNCCJPRMIAX-HNNXBMFYSA-NSMILESCOC1=CC(=CC(OC)=C1)C#CC1=NN([C@H]2CCN(C2)C(=O)C=C)C2=C1C(N)=NC=N2What you can answer from here — as of June 15, 2026
Which drugs share a target with Futibatinib, and which of those have an active Phase 3 trial?
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