Chang Patrick
Jefferson Medical College, Internal Medicine Department, 833 Chestnut Street, Suite 701, Philadelphia, PA 19107, USA.
IDrugs. 2004 Jan;7(1):50-7.
Venous thromboembolic disease, including deep vein thrombosis and pulmonary embolism, is a cause of significant mortality and morbidity. In the US, approximately 260000 cases are diagnosed annually. Current drugs for the prevention and treatment of venous thromboembolism (VTE) include heparin, low-molecular-weight heparins and warfarin. Since they possess several disadvantages, researchers are investigating improved anticoagulants. To understand how any promising anticoagulant would work, a review of the pathophysiology and regulation of the coagulation cascade is provided. The more prominent drugs reviewed include tissue factor pathway inhibitor protein, nematode anticoagulant protein, Factor IX inhibitors, anti-Factor Xa inhibitors (DX-9065a (Daiichi Seiyaku Co Ltd), YM-60828 (Yamanouchi Pharmaceutical Co Ltd), fondaparinux, idraparinux (Sanofi-Synthelabo/NV Organon)), selective thrombin inhibitors (oral heparin, ximelagatran (AstraZeneca plc)) and enhancers of natural anticoagulants (activated protein C, ART-123 (Asahi Kasei Pharma Corp)).
静脉血栓栓塞性疾病,包括深静脉血栓形成和肺栓塞,是导致严重死亡率和发病率的原因。在美国,每年约有26万例病例被诊断出来。目前用于预防和治疗静脉血栓栓塞(VTE)的药物包括肝素、低分子量肝素和华法林。由于它们存在几个缺点,研究人员正在研究改进的抗凝剂。为了了解任何有前景的抗凝剂的作用方式,本文提供了对凝血级联反应的病理生理学和调节的综述。所综述的更突出的药物包括组织因子途径抑制蛋白、线虫抗凝蛋白、因子IX抑制剂、抗因子Xa抑制剂(DX - 9065a(第一制药株式会社)、YM - 60828(山之内制药株式会社)、磺达肝癸钠、依达肝素(赛诺菲 - 安万特/欧加农公司))、选择性凝血酶抑制剂(口服肝素、希美加群(阿斯利康公司))以及天然抗凝剂增强剂(活化蛋白C、ART - 123(旭化成制药株式会社))。