天津医药

天津医药 ›› 2018, Vol. 46 ›› Issue (7): 765-770.doi: 10.11958/20171266

• 综述 • 上一篇    下一篇

新型降脂药PCSK9抑制剂的临床研究进展

崔丽，李广平△   

  1. 天津医科大学第二医院心脏科；天津心脏病学研究所；天津市心血管病离子与分子机能重点实验室（邮编300211）
  • 收稿日期:2017-11-14 修回日期:2018-03-16 出版日期:2018-07-15 发布日期:2018-07-15
  • 通讯作者: 崔丽 E-mail:drcuili@126.com
  • 作者简介:崔丽（1981），女，医学博士，主治医师，主要从事冠心病的基础和临床研究
  • 基金资助:
    天津医科大学第二医院重点实验室科研基金项目

Clinical research progress of proprotein convertase subtilisin/kexin type 9 inhibitors

CUI Li, LI Guang-ping△   

  1. Tianjin Key Laboratory of Ionic-Molecular Function of Cardiovascular Disease, Department of Cardiology, Tianjin Institute of Cardiology, the Second Hospital of Tianjin Medical University, Tianjin 300211, China △Corresponding Author and Revisor E-mail: tic_tjcardiol@126.com
  • Received:2017-11-14 Revised:2018-03-16 Published:2018-07-15 Online:2018-07-15

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摘要： 前蛋白转化酶枯草溶菌素9（PCSK9）抑制剂可通过阻断PCSK9-低密度脂蛋白受体（LDLR）途径介导的 LDLR降解，降低循环中低密度脂蛋白胆固醇（LDL-C）水平。目前PCSK9抑制剂已成为心血管领域降脂治疗的热 点，多种PCSK9抑制剂已进入了临床试验阶段。本文主要对PCSK9的分子结构及功能、PCSK9抑制剂的分类，尤其 是单克隆抗体药物的临床研究进展进行综述，评价PCSK9抑制剂对降低LDL-C水平的有效性及其应用的安全性。

关键词: 脂蛋白类, LDL, 抗体, 单克隆, 前蛋白转化酶枯草溶菌素9, 综述

Abstract: Proprotein convertase subtilisin / kexin type 9 (PCSK9) inhibitors can reduce the low density lipoprotein cholesterol (LDL-C) level in circulatory system by blocking PCSK9-low density lipoprotein receptor (LDLR) pathway to mediate the degradation of LDLR. At present, PCSK9 inhibitors have become the focus of cardiovascular lipid-lowering therapy. A variety of PCSK9 inhibitors have entered the clinical trial stage. This paper mainly reviews the molecular structure and mechanism of PCSK9, the classification of PCSK9 inhibitors, and recent clinical study of the monoclonal antibodies of PCSK9 inhibitors in order to evaluate the effectiveness and long-term safety of cardiovascular risk reduction.

Key words: lipoproteins, LDL, antibodies, monoclonal, proprotein convertase subtilisin/kexin type 9, review