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新型口服抗凝药的逆转

Reversal of novel oral anticoagulants.

作者信息

Abo-Salem Elsayed, Becker Richard C

机构信息

Division of Cardiovascular Health and Disease, University of Cincinnati College of Medicine, Heart, Lung and Vascular Institute, Cincinnati, OH, USA.

Division of Cardiovascular Health and Disease, University of Cincinnati College of Medicine, Heart, Lung and Vascular Institute, Cincinnati, OH, USA.

出版信息

Curr Opin Pharmacol. 2016 Apr;27:86-91. doi: 10.1016/j.coph.2016.02.008. Epub 2016 Mar 2.

Abstract

The development of a new generation of non-vitamin K oral anticoagulants represents a potential breakthrough in the management of patients with thrombotic diseases, disorders and conditions. While a large and growing body of evidence from large-scale clinical trials and registries supports a favorable safety profile, having a means to rapidly reverse their anticoagulant effects represents an unmet need among practicing clinicians. Several targeted reversal agents are currently in development and the early results are promising. Idarucizumab is a monoclonal antibody that can immediately and specifically reverse dabigatran. Andexanet alfa is a recombinant modified factor Xa that can bind and reverse oral and parenteral factor Xa inhibitors, including rivaroxaban, apixaban and edoxaban, and low molecular weight heparin. Aripazine is a small molecule that can reverse the action of factor Xa inhibitors and possibly dabigatran as well through non-covalent binding and charge-charge interactions.

摘要

新一代非维生素K口服抗凝剂的研发是血栓性疾病、紊乱和病症患者管理方面的一个潜在突破。尽管来自大规模临床试验和登记处的大量且不断增加的证据支持其良好的安全性,但有一种能够迅速逆转其抗凝作用的方法仍是执业临床医生尚未满足的需求。目前有几种靶向逆转剂正在研发中,早期结果很有前景。依达赛珠单抗是一种单克隆抗体,可立即特异性逆转达比加群的作用。安多凝血素α是一种重组修饰的Xa因子,可结合并逆转口服和胃肠外Xa因子抑制剂,包括利伐沙班、阿哌沙班和依度沙班,以及低分子量肝素。阿利帕嗪是一种小分子,可通过非共价结合和电荷相互作用逆转Xa因子抑制剂的作用,也可能逆转达比加群的作用。

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