Cardiovascular Pharmacology, Pharma R&D Discovery Research, Bayer Schering Pharma AG, Aprather Weg 18a, 42096 Wuppertal, Germany.
Hamostaseologie. 2009 Aug;29(3):260-7.
Oral factor Xa (FXa) inhibitors are a promising alternative to current anticoagulants. This paper reviews the latest developments of oral direct FXa inhibitors and focuses on those which have been approved for the prevention of venous thromboembolism (VTE) after total hip or knee replacement or are in advanced development and have passed phase II (proof of principle) testing. The most advanced drugs are apixaban, betrixaban, edoxaban, eribaxaban, rivaroxaban, LY517717, TAK-442, and YM150. Rivaroxaban (Xareltoâ) is the first direct FXa inhibitor which has recently been approved for the prevention of VTE in adult patients after elective hip or knee replacement in several countries, including the European Union and Canada. Rivaroxaban has a flat dose-dependent anticoagulant response with a wide therapeutic window and low potential for drug-drug and drug-food interactions. Rivaroxaban can be given in fixed doses without coagulation monitoring. This review describes the pharmacodynamic and pharmacokinetic profiles and the results of clinical trials with FXa inhibitors in the prevention and treatment of thromboembolic disorders.
口服因子 Xa（FXa）抑制剂是目前抗凝剂的一种有前途的替代品。本文综述了口服直接 FXa 抑制剂的最新进展，重点介绍了那些已被批准用于预防全髋关节或全膝关节置换术后静脉血栓栓塞症（VTE）的药物，或处于先进开发阶段并已通过 II 期（原理验证）测试的药物。最先进的药物是阿哌沙班、贝曲沙班、依度沙班、艾力班沙、利伐沙班、LY517717、TAK-442 和 YM150。利伐沙班（Xareltoâ）是第一种直接 FXa 抑制剂，最近已在包括欧盟和加拿大在内的几个国家获得批准，用于预防择期髋关节或膝关节置换术后成年患者的 VTE。利伐沙班具有剂量依赖性的抗凝反应，治疗窗宽，药物相互作用和药物-食物相互作用的潜力低。利伐沙班可以固定剂量给药，无需凝血监测。本文描述了 FXa 抑制剂在预防和治疗血栓栓塞性疾病中的药效学和药代动力学特征以及临床试验结果。
