Harenberg Job, Wehling Martin
Clinical Pharmacology Mannheim, Vascular Pharmacotherapy, Faculty of Medicine, University of Heidelberg, Mannheim, Germany.
Semin Thromb Hemost. 2008 Feb;34(1):39-57. doi: 10.1055/s-2008-1066023.
Indirect systemic and direct oral factor Xa and direct oral factor IIa inhibitors with improved pharmacologic profiles compared with heparins and vitamin K antagonists are currently in clinical development. This overview focuses on the indirect antithrombin dependent pentasaccharide derivatives of idraparinux and on the most advanced oral direct inhibitors to factor Xa (rivaroxaban and apixaban) and IIa (dabigatran). Specifically, the results of dose-finding studies for the prevention of venous thromboembolism after elective orthopedic surgery, the results of dose-finding studies for treatment of acute venous thromboembolism including prolonged prophylaxis of recurrent events, and the designs of ongoing clinical trials are reviewed.
与肝素和维生素K拮抗剂相比，具有改善药理学特征的间接全身性和直接口服Xa因子抑制剂以及直接口服IIa因子抑制剂目前正处于临床开发阶段。本综述重点关注依达肝素的间接抗凝血酶依赖性五糖衍生物以及最先进的口服Xa因子直接抑制剂（利伐沙班和阿哌沙班）和IIa因子直接抑制剂（达比加群）。具体而言，本文回顾了择期骨科手术后预防静脉血栓栓塞的剂量探索研究结果、治疗急性静脉血栓栓塞（包括延长预防复发性事件）的剂量探索研究结果以及正在进行的临床试验设计。
