口服异柠檬酸脱氢酶-2抑制剂——伊那尼布

A new oral isocitrate dehydrogenase-2 inhibitor——enasidenib

伊那尼布(enasidenib,商品名:IDHIFA)是由Agios公司开发的第1个获FDA批准上市的致癌代谢物合成抑制剂,用于治疗异柠檬酸脱氢酶-2(isocitrate dehydrogenase-2,IDH2)变异、复发难治型急性髓系白血病。伊那尼布的问世,解决了部分复发难治型急性髓系白血病患者的治疗难题。笔者就伊那尼布的研发历程、基本性质、作用机制、药动学、药效学、临床试验及应用作一概述,以期能为临床用药提供帮助。

Enasidenib （trade name： IDHIFA） developed by Agios is the first oncometabolite inhibitor approved by FDA to treat relapsed or refractory acute myeloid leukemia adult patients with an isoeitrate dehydrogenase-2 mutation. Enasidenib is a targeted therapy that fills an unmet need for relapsed or refractory acute myeloid leukemia patients within isocitrate dehydrogenase-2 mutation. The development process, properties, mechanism, pharmacokinetics, pharmaeodynamics, clinical trials and applications of enasidenib are summarized in this paper for the purpose of providing reference for clinical treatment.