Kubitza Dagmar, Becka Michael, Mueck Wolfgang, Zuehlsdorf Michael
Clinical Pharmacology, Bayer HealthCare AG, Wuppertal, Germany.
J Clin Pharmacol. 2006 Sep;46(9):981-90. doi: 10.1177/0091270006292127.
Rivaroxaban (BAY 59-7939) is an oral, direct Factor Xa inhibitor in advanced clinical development for the prevention and treatment of thromboembolic disorders. This was a randomized, 2-way crossover study in healthy male subjects, with an aspirin run-in period, to examine whether aspirin influences the safety, tolerability, pharmacodynamics, and pharmacokinetics of rivaroxaban. All treatments were well tolerated; drug-related adverse events were mild and transient. Aspirin did not alter the effects of rivaroxaban on Factor Xa activity or clotting tests. Platelet aggregation and bleeding time were not affected by rivaroxaban, and rivaroxaban did not influence the effects of aspirin on these parameters to a clinically relevant extent. Aspirin did not affect the pharmacokinetics of rivaroxaban, including the fraction unbound. This study suggests that there is no clinically relevant interaction between rivaroxaban and aspirin and that the 2 drugs could be administered concomitantly at the doses used in this study.
利伐沙班（BAY 59-7939）是一种口服的直接Xa因子抑制剂，正处于预防和治疗血栓栓塞性疾病的晚期临床开发阶段。这是一项在健康男性受试者中进行的随机、双向交叉研究，设有阿司匹林导入期，以研究阿司匹林是否会影响利伐沙班的安全性、耐受性、药效学和药代动力学。所有治疗耐受性良好；与药物相关的不良事件轻微且短暂。阿司匹林未改变利伐沙班对Xa因子活性或凝血试验的影响。血小板聚集和出血时间不受利伐沙班影响，且利伐沙班在临床相关程度上未影响阿司匹林对这些参数的作用。阿司匹林不影响利伐沙班的药代动力学，包括游离分数。本研究表明，利伐沙班和阿司匹林之间不存在临床相关相互作用，且这两种药物可以按照本研究中使用的剂量同时给药。
