一种调血脂的新型单抗药物evolocumab  

A monoclonal antibody drug for lowering LDL-cholesterol: evolocumab

作　　者：王艳[1] 刘兆鹏[1] 

机构地区：[1]山东大学药学院药物化学研究所教育部天然产物化学生物学重点实验室,山东济南250012

出　　处：《中国新药与临床杂志》2017年第4期190-195,共6页Chinese Journal of New Drugs and Clinical Remedies

摘　　要：evolocumab是首个用于调节血脂的前蛋白转化酶枯草溶菌素9(PCSK9)型抑制剂,用于治疗原发性高胆固醇血症和12岁及以上青少年和成年患者的纯合子家族性高胆固醇血症(Ho FH)。evolocumab通过与PCSK9特异性结合,从而减缓低密度脂蛋白受体的降解,显著降低体内低密度脂蛋白胆固醇(LDL-C)的水平。单独用药或联合他汀类药物可以使患者LDL-C水平降低55%~65%,特别适合于对他汀类不耐受以及高剂量他汀类(如阿托伐他汀、瑞舒伐他汀)调脂不达标的患者,为调脂治疗带来了新的选择。本文对其药理作用,在治疗和改善胆固醇高血脂的临床试验和安全性研究等方面的研究进展进行综述。Evolocumab is the first proprotein convertase subtilisin/kexin type 9 （PCSK9） inhibitor proved for the treatment of adults with primary hypercholesterolaemia, adults and children ≥ 12 years old with homozygous familial hypercholesterolaemia （HoFH）. Its main pharmacological action is to prevent PCSK9 interaction with the low-density lipoprotein receptors （LDLR） and thereby to restore the LDLR recycling and low-density lipoprotein cholesterol （LDL-C） uptake. Evolocumab is used independently or in combination with statin to reduce LDL-C by 55%-65%. For the patients who do not respond adequately to statins or who cannot meet their LDL- C reduction goals on the highest doses of atorvastatin and rosuvastatin, evolocumab may provide substantial LDL- C-lowering benefits. This article will make a review of its pharmacological action, its use in the treatment and improvement of hyperlipidemia, and safety issue.

关 键 词：evolocumab 前蛋白转化酶类 抗体 单克隆 PCSK9抑制剂 抗体 单克隆 调脂药 胆固醇 LDL 

分 类 号：R972.6[医药卫生—药品]