柳叶刀:在健康志愿者中达比加群酯逆转剂效果显著
-在健康人群中,特异性逆转剂idarucizumab[1] 可以迅速、完全、持久地逆转泰毕全® 的抗凝效应。
-通过五分钟单次idarucizumab输注即刻达到完全逆转,且耐受良好。
-Idarucizumab已提交美国食品药品监督管理局(FDA)、欧洲药品管理局(EMA)和加拿大卫生部进行上市审批。
2015年6月17日柳叶刀发表了特异性逆转剂idarucizumab逆转达比加群酯抗凝效应的研究结果。研究结果显示,idarucizumab可迅速、完全、持久地逆转泰毕全®的抗凝效应。研究数据表明,针对需要逆转抗凝效应的情况,例如需紧急干预治疗时,特异性拮抗剂可以提供一种具有高度靶向作用的治疗选择。1美国FDA2认定Idarucizumab为突破性治疗药物。目前,勃林格殷格翰公司已将Idarucizumab提交至FDA、EMA和加拿大卫生部进行上市审批。 3
在柳叶刀现已发表的健康志愿者研究中,参与者首先接受泰毕全®治疗,然后接受idarucizumab治疗。该实验在泰毕全®末次给药后2小时给予特异性逆转剂,此时达比加群酯的浓度处于峰值。输注idarucizumab五分钟后,抗凝作用即刻逆转至基线水平。2g或以上剂量可使逆转效应持续超过24小时。在研究参与者中,Idarucizumab耐受良好。1
“柳叶刀发表的数据表明,在健康志愿者中,idarucizumab对达比加群酯的逆转效果惊人,” 勃林格殷格翰心血管治疗领域医学副总裁Jörg Kreuzer教授表示,“一旦获批,意味着特异性新型口服抗凝药逆转剂的诞生,对于抗凝治疗具有里程碑式的意义。”
在2014年12月的美国血液学会年会上,曾公布idarucizumab在老年志愿者及肾损害志愿者人群中表现出的相似结果。4勃林格殷格翰正在开展idarucizumab在患者人群研究——RE-VERSE ADTM研究。5
更多信息
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3. Boehringer Ingelheim Press Release – 3 March 2015. Boehringer Ingelheim submits applications for approval of idarucizumab, specific reversal agent to dabigatran etexilate (Pradaxa®), to EMA, FDA and Health Canada. http://www.boehringer-ingelheim.com/news/news_releases/press_releases/2015/03_march_2015_dabigatranetexilate.html Last accessed April 2015.
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5. Pollack C, et al. A Phase III Clinical Trial to Evaluate the Reversal Effects of Idarucizumab on Active Dabigatran (RE-VERSE AD™). Poster presentation at the International Stroke Conference, Nashville, TN, USA, 11-13 February 2015.
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