口服抗凝药解毒剂的研究进展

Research progress on antidotes for oral anticoagulants

近年来新型口服抗凝药(NOACs)取得很大的发展,逐渐取代传统抗凝药而成为临床一线的首选药物。尽管与传统抗凝药物相比,NOACs的出血副作用相当或更小,但依然存在着一定的出血风险。传统抗凝药物的解毒剂对NOACs的解毒效果不佳,为该类药物的使用带来很大的风险和不便。针对NOACs的特殊解毒剂正在开发当中,前期试验已取得不错的结果。这些解毒剂最具有代表性的药物包括Portola制药公司的andexanet alfa、勃林格殷格翰公司的idarucizumab以及Perosphere公司的aripazine,主要针对这3种NOACs解毒剂的研究进展以及存在的问题进行综述。

In recent years, new oral anticoagulants（NOACs） had made great development, and they gradually replaced the traditional anticoagulants to become the first-line drug of choice for clinic. Compared with conventional anticoagulants, their bleeding side effects were close to or less, but they still had a certain risk of bleeding. Traditional anticoagulant antidotes had poor detoxifying effect of NOACs, which led to a great deal of inconvenience and risk for the use of these drugs. Specific antidotes for NOACs were under development, and preliminary tests had achieved good results. Most representative drugs of these antidotes included andexanet alfa of Portola Pharmaceuticals, idarucizumab of Boehringer Ingelheim, and aripazine of Perosphere. This article reviewed research progress and problems of these three NOACs antidotes.