Clinical Pharmacology, Mannheim, Ruprecht-Karls-University Heidelberg, Mannheim, Germany.
Br J Pharmacol. 2012 Jan;165(2):363-72. doi: 10.1111/j.1476-5381.2011.01578.x.
New direct and indirect acting factor Xa (FXa) and thrombin inhibitors are being developed to overcome the downsides of the conventional anticoagulants - unfractionated and low molecular weight heparins and vitamin K antagonists. Ximelagatran and idraparinux failed to demonstrate an acceptable safety profile. Rivaroxaban and dabigatran are approved for the post-operative prevention of thromboembolic complications after elective hip or knee replacement surgery; dabigatran is approved for the prevention of embolism in patients with atrial fibrillation in an increasing number of countries. Several novel indirect antithrombin-dependent anticoagulants as well as antithrombin-independent oral direct FXa and thrombin inhibitors are investigated in multiple indications for the prophylaxis and treatment of venous thromboembolism and the prophylaxis of arterial thrombotic disorders. Quality-adjusted life years costs and incremental cost-effectiveness ratios are relatively high at present, but may decrease after approval of more new anticoagulants for additional indications.
新型直接和间接作用的因子 Xa（FXa）和凝血酶抑制剂正在被开发，以克服传统抗凝剂（未分级肝素和低分子量肝素以及维生素 K 拮抗剂）的缺点。西米拉坦和依达肝素未能表现出可接受的安全性特征。利伐沙班和达比加群获批用于择期髋关节或膝关节置换手术后预防血栓栓塞并发症；达比加群在越来越多的国家获批用于预防心房颤动患者的栓塞。多种新型间接抗凝血酶依赖性抗凝剂以及抗凝血酶非依赖性的口服直接 FXa 和凝血酶抑制剂正在多个适应证中被研究，用于预防和治疗静脉血栓栓塞以及预防动脉血栓性疾病。目前，质量调整生命年成本和增量成本效益比相对较高，但在更多新抗凝剂获批用于其他适应证后，可能会降低。
