Department of Internal Medicine & Radboud Institute for Health Sciences, Radboud University Medical Center, Nijmegen, the Netherlands.
Department of Internal Medicine & Radboud Institute for Health Sciences, Radboud University Medical Center, Nijmegen, the Netherlands.
Drug Discov Today. 2022 Oct;27(10):103332. doi: 10.1016/j.drudis.2022.07.017. Epub 2022 Aug 3.
Despite the improved safety-profile of direct oral anticoagulants (DOACs), bleeding complications remain an important side effect of anticoagulant treatment. Although anticoagulant-specific antidotes are available, an universal anticoagulant reversal agent in case of life-threatening bleeding or emergency surgery is not yet available. Ciraparantag, a synthetic small molecule that inactivates heparins and DOAC, is a promising new reversal agent that has been investigated in phase 2 trials. In this short review we provide an overview of the preclinical and clinical evidence of ciraparantag, and compare strengths and weaknesses of ciraparantag and the currently available anticoagulant reversal strategies.
尽管直接口服抗凝剂 (DOACs) 的安全性有所提高,但出血并发症仍然是抗凝治疗的一个重要副作用。虽然有抗凝剂特异性解毒剂可用,但在发生危及生命的出血或紧急手术时,仍然没有通用的抗凝逆转剂。Ciraparantag 是一种合成的小分子,可使肝素和 DOAC 失活,是一种很有前途的新型逆转剂,已在 2 期临床试验中进行了研究。在这篇简短的综述中,我们提供了 Ciraparantag 的临床前和临床证据概述,并比较了 Ciraparantag 和目前可用的抗凝逆转策略的优缺点。