Unknown Manufacturer • 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. In Europe, it is indicated in patients whose disease has progressed after at least one prior line of systemic therapy. Futibatinib is approved in the US under accelerated approval and in Europe under conditional marketing authorization. This currently approved indication is subject to change, as it may be contingent upon verification and description of clinical benefit in a confirmatory trial(s).
Futibatinib is a kinase inhibitor used to treat intrahepatic cholangiocarcinoma in previously treated adults.
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 IC 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.
