抑制三磷酸腺苷柠檬酸裂解酶的降胆固醇新药——bempedoic acid  

A new cholesterol-lowering drug that inhibits adenosine triphosphate citrate lyase—bempedoic acid

作　　者：吴乾杰 刘洋[1] WU Qian-jie;LIU Yang(School of Pharmaceutical Engineering,Shenyang Pharmaceutical University,Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education,Shenyang 110016,China)

机构地区：[1]沈阳药科大学制药工程学院基于靶点的药物设计与研究教育部重点实验室

出　　处：《临床药物治疗杂志》2019年第5期1-6,共6页Clinical Medication Journal

摘　　要：Bempedoic acid(ETC-1002)是由美国生物制药公司Esperion公司研发的一种新型口服降脂药物,目前正在进行临床Ⅲ期研究。Bempedoic acid通过抑制三磷酸腺苷柠檬酸裂解酶来降低胆固醇合成。该药单独或与阿托伐他汀、依泽替米贝进行二联或者三联用药,可将低密度脂蛋白降低17%~45%,同时还可以降低非高密度脂蛋白胆固醇、C-反应蛋白和载脂蛋白B的水平。与他汀类药物相比,bempedoic acid仅在肝脏中代谢为活性形式,而在非骨骼肌中不代谢转化。因此不会导致他汀类药物使用过程中经常出现的肌肉不良反应。本文对其基本信息、作用机制、临床试验信息进行概述。Bempedoic acid(ETC-1002)is a new oral lipid-lowering drug developed by Esperion.Now it′s under Phase Ⅲ clinical studies.It can reduce cholesterol synthesis through inhibition of adenosine triphosphate citrate lyase.When used alone or in various combinations with atorvastatin and/or ezetimibe,the LDL-C lowering effect of this drug ranged from 17% to 45%.Meanwhile it can reduce levels of non-high-density lipoprotein cholesterol,C-reactive protein,and apo-lipoprotein B.In contrast to statins,bempedoic acid is converted to the active agent only in the liver and not in non-skeletal muscle,thus without the muscle side effects of statins.In this paper,the basic information,mechanisms,clinical trials are summarized.

关 键 词：bempedoic ACID 三磷酸腺苷柠檬酸裂解酶 低密度脂蛋白胆固醇 

分 类 号：R741[医药卫生—神经病学与精神病学]