Laux Volker, Perzborn Elisabeth, Kubitza Dagmar, Misselwitz Frank
Cardiovascular Research, Bayer Schering Pharma, Aprather Weg 18A, D-42096 Wuppertal, Germany.
Semin Thromb Hemost. 2007 Jul;33(5):515-23. doi: 10.1055/s-2007-982083.
There are several novel anticoagulants in development that target factor Xa(FXa)-the pivotal point of the coagulation cascade. One promising agent is rivaroxaban (a highly selective, oral, direct FXa inhibitor), which is in advanced clinical development for the prevention and treatment of thromboembolic disorders. Oral rivaroxaban may be given in fixed once-daily doses, with the potential for no coagulation monitoring. These properties, along with results from preclinical and clinical studies, suggest that rivaroxaban may have advantages over current treatments. Studies in arterial and venous animal models demonstrated that rivaroxaban has potent antithrombotic effects, without prolonging bleeding times. In healthy subjects, rivaroxaban was well tolerated, with a predictable pharmacological profile and a low propensity for clinically relevant drug-drug interactions. Phase II studies of rivaroxaban for the prevention of venous thromboembolism (VTE) after major orthopedic surgery support these findings. The results also suggested that a total daily dose range of 5 to 20 mg rivaroxaban had similar efficacy and safety to enoxaparin, and that 10 mg rivaroxaban once daily was the optimal dose. This review assesses the preclinical and clinical characteristics of rivaroxaban, and discusses phase II findings with rivaroxaban for the prevention of VTE after major orthopedic surgery.
目前有几种新型抗凝剂正在研发中,它们作用于凝血因子Xa(FXa)——凝血级联反应的关键点。一种有前景的药物是利伐沙班(一种高度选择性的口服直接FXa抑制剂),它正处于预防和治疗血栓栓塞性疾病的临床研发后期阶段。口服利伐沙班可以采用固定的每日一次给药剂量,可能无需进行凝血监测。这些特性,连同临床前和临床研究的结果,表明利伐沙班可能比目前的治疗方法具有优势。在动脉和静脉动物模型中的研究表明,利伐沙班具有强大的抗血栓作用,且不会延长出血时间。在健康受试者中,利伐沙班耐受性良好,具有可预测的药理学特征,且发生临床相关药物相互作用的倾向较低。利伐沙班用于预防大型骨科手术后静脉血栓栓塞(VTE)的II期研究支持了这些发现。结果还表明,利伐沙班每日总剂量范围为5至20毫克时,其疗效和安全性与依诺肝素相似,且利伐沙班每日一次10毫克是最佳剂量。这篇综述评估了利伐沙班的临床前和临床特征,并讨论了利伐沙班用于预防大型骨科手术后VTE的II期研究结果。