摘要
血管内血栓的形成是心肌梗塞、不稳定心绞痛及肺栓塞等疾病发生的关键性因素,抗凝药则是阻止血液凝固的一类药物。Xa因子抑制剂作为新型的抗凝血药,近年来受到了广泛的关注。Rivaroxaban的上市及处于临床研究中的Apixaban、Eribaxaban、Betrixaban、LY517717、DU-176b、YM150及TAK442等诸多口服Xa因子抑制剂的出现,为血栓栓塞疾病患者带来了新的福音。本文从Xa因子抑制剂与凝血因子Xa结合的晶体结构以及各Xa因子抑制剂的临床特点入手,来综述近年来开发的或正在开发中的Xa因子抑制剂。
Intravascular clot formation plays a key role in the development of many cardiovascular diseases such as myocardial infarction,unstable angina,and pulmonary embolism.Anticoagulants are a kind of drugs used for the prevention of blood clotting.As one of the novel oral anticoagulants,factor Xa（FXa） inhibitors have received much attention recently.Rivaroxaban is now approved for venous thromboprophylaxis,and other oral FXa inhititors such as Apixaban,Eribaxaban,Betrixaban,LY 517717,DU-176b,YM 150 and TAK442 are all in clinic development and show considerable promise for thromboembolic diseases.This article reviews the oral FXa inhibitors in development,with the focus on their mechanism and clinical studies.
出处
《药学与临床研究》
2010年第3期294-298,共5页
Pharmaceutical and Clinical Research
