前蛋白转化酶枯草杆菌蛋白酶/kexin 9型抑制剂

Proprotein Convertase Subtilisin Kexin 9 Inhibitors.

作者信息

Pirillo Angela, Catapano Alberico Luigi

机构信息

Center for the Study of Atherosclerosis, E. Bassini Hospital, Via M. Gorki, 50, Cinisello Balsamo, Milan 20092, Italy; IRCCS MultiMedica, Via Milanese, 300, Sesto S. Giovanni, Milan 20099, Italy.

IRCCS MultiMedica, Via Milanese, 300, Sesto S. Giovanni, Milan 20099, Italy; Department of Pharmacological and Biomolecular Sciences, University of Milan, Via Balzaretti, 9, Milan 20133, Italy.

出版信息

Cardiol Clin. 2018 May;36(2):241-256. doi: 10.1016/j.ccl.2017.12.006.

DOI:10.1016/j.ccl.2017.12.006

PMID:29609754

Abstract

High levels of low-density lipoprotein cholesterol (LDL-C) are directly associated with an increased risk of cardiovascular disease. Reducing LDL-C levels reduces the incidence of cardiovascular events. Several lipid-lowering approaches are available to achieve the LDL-C levels recommended by current guidelines, statins being the first-line therapy. However, many patients cannot achieve the recommended LDL-C levels with current therapies. The discovery of the role of proprotein convertase subtilisin kexin 9 (PCSK9) in the regulation of plasma LDL-C levels suggested it as a potential pharmacologic target and led to the development of PCSK9 inhibitors for the management of LDL-C levels.

摘要

高水平的低密度脂蛋白胆固醇（LDL-C）与心血管疾病风险增加直接相关。降低LDL-C水平可降低心血管事件的发生率。有几种降脂方法可用于达到当前指南推荐的LDL-C水平，他汀类药物是一线治疗药物。然而，许多患者使用当前疗法无法达到推荐的LDL-C水平。前蛋白转化酶枯草溶菌素9（PCSK9）在调节血浆LDL-C水平中的作用的发现表明它是一个潜在的药理学靶点，并促使开发用于管理LDL-C水平的PCSK9抑制剂。