心腦血管疾病已成為全球致病和致死率最高的疾病之一,血栓形成是心腦血管疾病的主要誘因。傳統(tǒng)的抗凝藥物以肝素和華法林為主,但存在出血、血小板減少的明顯不良反應(yīng)。Xa因子處于內(nèi)源性凝血和外源性凝血通路的中心位置,并且每分子的Xa因子可活化產(chǎn)生約1 000分子的凝血酶,Xa因子抑制劑的出現(xiàn)為抗凝藥物的發(fā)展提供了新的方向。貝曲沙班是一種口服的直接Xa因子抑制劑,也是目前唯一經(jīng)腎臟排泄最少的藥物,在一系列研究中顯示出良好的治療前景。主要從貝曲沙班的藥物概況、相關(guān)背景、合成路線、作用機(jī)制、臨床研究等方面進(jìn)行介紹。

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.

國(guó)家科技重大專項(xiàng)資助項(xiàng)目(2013ZX09102104)