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PCSK9 抑制剂 2018:掀起冠状动脉预防的新浪潮。

PCSK9 inhibition 2018: riding a new wave of coronary prevention.

机构信息

School of Public Health, Curtin University, Perth, Australia.

School of Medicine, University of Western Australia, Perth, Australia.

出版信息

Clin Sci (Lond). 2019 Jan 22;133(2):205-224. doi: 10.1042/CS20171300. Print 2019 Jan 31.

Abstract

Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a hepatic enzyme that regulates the low-density lipoprotein cholesterol (LDL-c) receptor and thus circulating LDL-c levels. With overwhelming evidence now supporting the reduction in LDL-c to lower the risk of cardiovascular disease, PCSK9 inhibitors represent an important therapeutic target, particularly in high-risk populations. Here, we summarise and update the science of PCSK9, including its discovery and the development of various inhibitors, including the now approved monoclonal antibodies. In addition, we summarise the clinical applications of PCSK9 inhibitors in a range of patient populations, as well as the major randomised controlled trials investigating their use in coronary prevention.

摘要

前蛋白转化酶枯草溶菌素 9(PCSK9)是一种肝脏酶,可调节低密度脂蛋白胆固醇(LDL-c)受体,从而调节循环 LDL-c 水平。目前有大量证据支持降低 LDL-c 以降低心血管疾病风险,PCSK9 抑制剂代表了一个重要的治疗靶点,尤其是在高危人群中。在这里,我们总结并更新了 PCSK9 的科学知识,包括其发现和各种抑制剂的开发,包括现已批准的单克隆抗体。此外,我们还总结了 PCSK9 抑制剂在一系列患者人群中的临床应用,以及调查其在冠状动脉预防中的应用的主要随机对照试验。

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