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.
作者
吴乾杰
刘洋
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)
出处
《临床药物治疗杂志》
2019年第5期1-6,共6页
Clinical Medication Journal
