摘要
血栓栓塞性疾病的长期抗凝治疗一直是临床中的重要问题,新型口服抗凝药的问世,首次为房颤、深静脉血栓形成患者卒中和肺栓塞的预防提供了除华法林之外的选择。其中,达比加群酯为直接凝血酶抑制剂,多项研究已证实其疗效相较于华法林,具有起效快、相互作用少、无需定期监测等优势。但也存在一些劣势,如出现重大出血事件时缺乏相应的拮抗剂。idarucizumab是一种人源化单克隆抗体片段,可与达比加群特异性结合,从而逆转其抗凝效应,同时该抗体没有促凝作用。临床研究表明,静脉输注idarucizumab可在数分钟内逆转达比加群抗凝作用,主要不良反应包括头痛、低血钾、谵妄、便秘、发热和肺炎等。本文就idarucizumab的药理作用、药动学、临床研究及安全性作一阐述。
Anticoagulant agents are a beadstone on thromboembolic disease therapy. Besides warfarin, novel oral anticoagulants had emerged for the prevention of stroke in nonvalvular atrial fibrillation, recurrent deep vein thrombosis, and pulmonary embolism. Dabigatran etexilate, as a direct and competitive inhibitor of thrombin, had demonstrated the effect and safty in several large randomized trials. However, bleeding was still a concerned side effect due to the lack of a reliable reversible agent. Idarucizumab, as a humanized monoclonal antibody fragment, could completely reverses the anticoagulant effects in several minutes by means of the binding with dabigatran. In recent clinical trials, idarucizumab-induced adverse events was involved in multiple organ and the most frequent ad- verse events were headache, hypokalemia, delirium, constipation, pyrexia, and pneumonia. In this review paper, we summarized the mechanism, pharmacokinetics, effectand safety of idarucizumab in clinical trials.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2016年第4期361-365,共5页
Chinese Journal of New Drugs
基金
上海医院药学科研项目(2014-YY-01-20)
