Title:Futibatinib: A Potent and Irreversible Inhibitor of Fibroblast Growth
Factor Receptors for Treatment of the Bile Duct Cancer
Volume: 31
Issue: 6
关键词:
胆管癌,福替替尼,成纤维细胞生长因子受体,药效学,药代动力学,药物相互作用。
摘要: Cholangiocarcinoma is a rare type of cancer. Futibatinib is an irreversible, potent,
selective inhibitor of fibroblast growth factor receptors (FGFR 1-4). On September
30, 2022, the US FDA first approved futibatinib to treat adult patients with bile duct cancer
whose disease is unresectable, locally advanced, or metastatic intrahepatic cholangiocarcinoma
harboring fibroblast growth factor receptor 2 (FGFR2) gene mutations or other
classes of rearrangements. The approval of this medicine was based on phase 3 clinical
trial results including an overall response rate (ORR) of 42% and a duration of response
(DoR) of 9.7 months. This short perspective summarizes Futibatinib’s synthesis, physicochemical
properties, dosage, route of administration, mechanism of action, binding mode,
pharmacodynamics, pharmacokinetics, drug interactions, adverse events, and possible
mechanism of resistance.