Dumont Bénédicte, Faille Dorothée, Ajzenberg Nadine
Département d'hématologie et d'immunologie biologiques, Hôpital Bichat, APHP, 46, rue Henri Huchard, 75877 Paris Cedex 18, France.
Med Sci (Paris). 2011 May;27(5):493-500. doi: 10.1051/medsci/2011275014. Epub 2011 May 25.
For years, prevention and treatment of thromboembolic events have been restricted to the use of heparins and vitamin K antagonists. These treatments, in spite of their unquestioned efficacy, present numerous limits (hemorrhagic risk, need for regular laboratory controls). These limits call for the development of new antithrombotic drugs. This review briefly reports on three new molecules, in very advanced phases of clinical research: dabigatran (Pradaxa®), rivaroxaban (Xarelto®) and apixaban. These molecules represent new oral anticoagulants, which directly inhibit a coagulation factor (thrombin for dabigatran, factor Xa for rivaroxaban and apixaban) and do not need regular anticoagulant monitoring or dose adjustment. The approval is still restricted in France to the prophylaxis of venous thromboembolism in orthopaedics. Dabigratran will be soon available in the prevention of stroke in atrial fibrillation. With the forthcoming phase III studies to prevent and treat venous thromboembolism, anticoagulant therapy management will be most probably improved in the coming years.
多年来，血栓栓塞事件的预防和治疗一直局限于使用肝素和维生素K拮抗剂。尽管这些治疗方法疗效确凿，但存在诸多局限性（出血风险、需要定期进行实验室检查）。这些局限性促使人们研发新型抗血栓药物。本综述简要介绍了三种处于临床研究非常后期阶段的新分子：达比加群（Pradaxa®）、利伐沙班（Xarelto®）和阿哌沙班。这些分子代表新型口服抗凝剂，它们直接抑制一种凝血因子（达比加群抑制凝血酶，利伐沙班和阿哌沙班抑制Xa因子），无需定期进行抗凝监测或剂量调整。在法国，其批准范围仍仅限于骨科手术中静脉血栓栓塞的预防。达比加群很快将可用于预防房颤患者的中风。随着即将开展的预防和治疗静脉血栓栓塞的III期研究，抗凝治疗管理在未来几年很可能会得到改善。
