心脑血管疾病已成为全球致病和致死率最高的疾病之一,血栓形成是心脑血管疾病的主要诱因。传统的抗凝药物以肝素和华法林为主,但存在出血、血小板减少的明显不良反应。Xa因子处于内源性凝血和外源性凝血通路的中心位置,并且每分子的Xa因子可活化产生约1 000分子的凝血酶,Xa因子抑制剂的出现为抗凝药物的发展提供了新的方向。贝曲沙班是一种口服的直接Xa因子抑制剂,也是目前唯一经肾脏排泄最少的药物,在一系列研究中显示出良好的治疗前景。主要从贝曲沙班的药物概况、相关背景、合成路线、作用机制、临床研究等方面进行介绍。

Cardiovascular and cerebrovascular diseases have become one of the leading causes of morbidity and mortality in the world. Thrombosis is a major cause. Conventional antithrombotic therapy comprises heparin, warfarin, and so on. All these agents have a potential bleeding risk and a significant adverse reaction of thrombocytopenia. Factor Xa, presented at the juncture of the intrinsic and the extrinsic pathways, plays a pivotal role in the blood coagulation cascade, and per molecule produces thrombin approximately 1000 molecules. Factor Xa inhibitors provide a new direction for the development of anticoagnlant drugs. Betrixaban is an oral direct factor Xa inhibitor, and has the lowest renal excretion. In a series of researches, betrixaban shows a good prospect. The drug situation, background, route of synthesis, pharmacological action and clinical trials researches of betrixaban are reviewed in this paper.

国家科技重大专项资助项目(2013ZX09102104)