Futibatinib: A Potent and Irreversible Inhibitor of Fibroblast Growth Factor Receptors for Treatment of the Bile Duct Cancer

被引:3
作者
De, Surya K. [1 ,2 ]
机构
[1] Conju Probe, Dept Chem, San Diego, CA 92121 USA
[2] Bharath Univ, Chennai 600126, Tamil Nadu, India
关键词
Cholangiocarcinoma; futibatinib; fibroblast growth factor receptor; pharmacodynamics; pharmacokinetics; drug interactions;
D O I
10.2174/0929867330666230416152913
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
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.
引用
收藏
页码:666 / 670
页数:5
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