上海交通大学学报(医学版) ›› 2018, Vol. 38 ›› Issue (3): 339-.doi: 10.3969/j.issn.1674-8115.2018.03.018

• 综述 • 上一篇    下一篇

前蛋白转化酶枯草溶菌素 9 单克隆抗体治疗冠状动脉粥样硬化性心脏病的临床研究进展

罗聪聪 1 ,鲍春荣 2 ,何斌 1   

  1. 上海交通大学 医学院附属新华医院 1. 麻醉与重症医学科,2. 心胸外科,上海 200092
  • 出版日期:2018-03-28 发布日期:2018-05-03
  • 通讯作者: ?何 斌,电子信箱:hebinicu@xinhuamed.com.cn。
  • 作者简介:?罗聪聪(1992—),男,壮族,硕士生;电子信箱:luocongcong1@163.com。
  • 基金资助:
    国家自然科学基金(81470390);上海市教育委员会高峰高原学科建设计划(20152218);上海交通大学医工交叉项目(YG2013MS21)

Clinical advances in monoclonal antibody against PCSK9 for coronary atherosclerotic heart disease

LUO Cong-cong1 , BAO Chun-rong2 , HE Bin1   

  1. 1. Department of Anesthesiology and SICU, 2. Department of Cardiothoracic Surgery, Xinhua Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200092, China
  • Online:2018-03-28 Published:2018-05-03
  • Supported by:
    Natural Science Foundation of China, 81470390; Shanghai Municipal Education Commission—Gaofeng Clinical Medicine Grant Support, 20152218; Biomedical Engineering Cross Research Foundation of Shanghai Jiao Tong University, YG2013MS21

摘要: 冠状动脉粥样硬化性心脏病(coronary atherosclerotic heart disease,CHD)的发病率及病死率居全球首位,而低密度脂蛋白胆固醇(low density lipoprotein-cholesterol,LDL-C)的升高是 CHD 的主要危险因素,因此降低 LDL-C 水平可有效减少 CHD 的发病风险。临床上降脂药物如他汀类虽能够有效降低 LDL-C 水平,但仍有部分患者无法达到降脂目标或者无法耐受。前蛋白转化酶枯草溶菌素 9(proprotein convertase subtilisin/kexin type 9,PCSK9)抑制剂作为新一代的降脂药物,越来越受到重视。其通过对 PCSK9 的抑制作用,增加低密度脂蛋白受体的循环利用,能够显著降低血清中 LDL-C 水平。目前 PCSK9 抑制剂已进入Ⅲ期临床试验,试验结果显示其具有良好的降脂效果和耐受性。该文就 PCSK9 抑制剂最新进展和面临的问题作一综述。

关键词: &ensp, 前蛋白转化酶枯草溶菌素 9;抑制剂;单克隆抗体;低密度脂蛋白胆固醇;冠状动脉粥样硬化性心脏病;高脂血症

Abstract: Coronary atherosclerotic heart disease (CHD) remains the leading cause of morbidity and mortality in the world, with elevated low density lipoprotein-cholesterol (LDL-C) levels as a major risk factor. Lower levels of LDL-C can effectively reduce the risk of CHD. To date, lipid-lowering medicines such as statins are effective in lowering LDL-C, but a proportion of patients do not achieve lipid reduction target with statins or are intolerant to statins. Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors are a new class of agents reducing LDL-C which gain more and more concerns. Through inhibitory effect on PCSK9 and increasing low-density lipoprotein receptors recycling, they can significantly reduce serum LDL-C levels. PCSK9 inhibitors are currently in phase Ⅲ of clinical trials, and the results showed that they had good lipid-lowering effects and tolerability. This review provided an overview of the latest advances and challenges about PCSK9 inhibitors.

Key words: proprotein convertase subtilisin/kexin type 9 (PCSK9), inhibitor, monoclonal antibody, low-density lipoprotein-cholesterol (LDL-C), coronary atherosclerotic heart disease (CHD), hyperlipidemia