Abed Hany S, Kilborn Michael J, Chen Vivien, Sy Raymond W
Department of Cardiology, Royal Prince Alfred Hospital, Sydney, NSW, Australia.
Department of Cardiology, Concord Repatriation General Hospital, Sydney, NSW, Australia.
J Atr Fibrillation. 2017 Dec 31;10(4):1634. doi: 10.4022/jafib.1634. eCollection 2017 Dec.
The incidence and prevalence of atrial fibrillation (AF) is expected to more than double between 2010 and 2030. Accordingly, the use of non-vitamin K oral anticoagulant (NOAC) agents for thromboembolic stroke prevention is anticipated to increase. The development of effective and safe antidotes is needed to address the unmet need for rapid anticoagulation reversal. The immediate role for these novel antidotes is for reversal of NOAC activity in life threatening bleeding and urgent surgical intervention. In addition, reversal agents may play an important role in simplifying bridging protocols in the peri-procedural period for catheter ablation of AF and elective surgery. Currently, novel reversal agents are either decoy drug receptors or small molecule non-specific anticoagulant activity inhibitors. These agents are at various stages of FDA investigation and approval, with emerging prospective data for safety and efficacy. The purpose of this review is to outline the currently developed NOAC molecular antagonists, their potential clinical roles and future directions.
预计2010年至2030年间，心房颤动（AF）的发病率和患病率将增加一倍以上。因此，预计用于预防血栓栓塞性中风的非维生素K口服抗凝剂（NOAC）的使用将会增加。需要开发有效且安全的解毒剂，以满足快速逆转抗凝作用这一未被满足的需求。这些新型解毒剂的直接作用是在危及生命的出血和紧急手术干预中逆转NOAC的活性。此外，逆转剂在简化房颤导管消融和择期手术围手术期的桥接方案中可能发挥重要作用。目前，新型逆转剂要么是诱饵药物受体，要么是小分子非特异性抗凝活性抑制剂。这些药物正处于美国食品药品监督管理局（FDA）调查和批准的不同阶段，有新出现的关于安全性和有效性的前瞻性数据。本综述的目的是概述目前已开发的NOAC分子拮抗剂、它们潜在的临床作用和未来方向。
