首个获批FXa抑制剂特异性拮抗剂andexanet alfa  

Andexanet alfa,the first approved specific antagonist of FXa inhibitors

作　　者：肖胜伟 李伟炜 杜雪亭 XIAO Sheng-wei;LI Wei-wei;DU Xue-ting(Shenzhen Hospital of Southern Medical University,Shenzhen 518000,China;Harrison International Peace Hospital,Hengshui 053000,China)

机构地区：[1]南方医科大学深圳医院,深圳518000 [2]哈励逊国际和平医院,衡水053000

出　　处：《中国新药杂志》2019年第10期1164-1168,共5页Chinese Journal of New Drugs

摘　　要：andexanet alfa是一种重组的凝血因子Xa(FXa)诱导蛋白,是FXa抑制剂的竞争性拮抗剂。2018年5月3日获FDA批准andexanet alfa用于治疗与利伐沙班及阿哌沙班相关的危及生命或无控制出血后的抗凝逆转。andexanet alfa在FXa结构基础上修饰而获得,与FXa抑制剂具有相同的亲和力而无任何抗凝血活性和促凝血活性。作为首个且唯一FXa抑制剂的特异性拮抗剂,andexanet alfa获得FDA加速批准同时获得突破性疗法及孤儿药资格认定。本文对andexanet alfa的生化特性、临床药理学、临床评价和安全性等进行综述。Andexanet alfa is a recombinant modified human Factor Xa(FXa) protein,which is a competitive antagonist of FXa inhibitors. On May 3,2018,andexanet alfa was approved by FDA for the patients treated with rivaroxaban and apixaban,when reversal of anticoagulation is needed due to life-threatening or uncontrolled bleeding. Andexanet alfa is a recombinant modified FXa decoy protein that is catalytically inactive but that retains the ability to bind FXa at the active site with high affinity. As the first and only specific inhibitor of FXa,andexanet alfa was approved under accelerated approval and obtained breakthrough therapy and orphan drug qualification by FDA. This review presents the biochemical characteristics,clinical pharmacology,clinical evaluation and safety of andexanet alfa.

关 键 词：andexanet ALFA 竞争性拮抗剂 抗凝逆转 临床药理学 临床评价 

分 类 号：R951[医药卫生—药学]