利伐沙班药物代谢及基因多态性研究现状

Research progress of rivaroxaban drug metabolism and gene polymorphism

利伐沙班是目前非瓣膜性心房颤动患者预防卒中和全身性栓塞的主要新型口服抗凝药物之一,明确的药物代谢动力学参数、稳定的血浆浓度、较少的药物相互作用以及较高的患者依从性是它的优势。但临床上观察到用药个体之间药物代谢动力学的差异,以及药物导致的大出血事件,使利伐沙班基因多态性对药物代谢的影响成为研究热点。现简述利伐沙班的药物代谢动力学特点,着重讨论基因组学的主要研究进展,为利伐沙班的个体化合理用药提供参考。

Rivaroxaban is one of the new oral anticoagulants(NOAC)for preventing stroke and systemic embolism in patients with non-valvular atrial fibrillation.It has clear pharmacokinetic parameters,stable plasma concentration,less drug-drug interaction and higher compliance of patients.However,the discrepancy of pharmacokinetics between individuals and drug-induced hemorrhage events frequently occur clinically,therefore the association of gene polymorphism with drug metabolism has become a research hotspot.This article reviews the research progress on pharmacokinetic characteristics of rivaroxaban and its relationship with gene polymorphism,to provide a reference for the individualized rational use of rivaroxaban.