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。
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 phaseⅢof 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.
作者
罗聪聪
鲍春荣
何斌
LUO Cong-cong;BAO Chun-rong;HE Bin(Department of Anesthesiology and SICU,Xinhua Hospital,Shanghai Jiao Tong University School of Medicine,Shanghai 200092,China;Department of Cardiothoracic Surgery,Xinhua Hospital,Shanghai Jiao Tong University School of Medicine,Shanghai 200092,China)
出处
《上海交通大学学报（医学版）》
CAS
CSCD
北大核心
2018年第3期339-342,共4页
Journal of Shanghai Jiao tong University:Medical Science
基金
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)~~
关键词
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
proprotein convertase subtilisin/kexin type 9(PCSK9)
inhibitor
monoclonal antibody
low-density lipoprotein-cholesterol(LDL-C)
coronary atherosclerotic heart disease(CHD)
hyperlipidemia
