胰高血糖素样肽-1受体激动剂研究进展  

Research progress of glucagon-like receptor agonists

作　　者：程速远 李小静 罗建辉 CHENG Su-yuan;LI Xiao-jing;LUO Jian-hui(Center for Drug Evaluation,National Medical Products Administration,Beijing 100022,China)

机构地区：[1]国家药品监督管理局药品审评中心,北京100022

出　　处：《中国新药杂志》2020年第22期2580-2585,共6页Chinese Journal of New Drugs

摘　　要：胰高血糖素样肽-1(GLP-1)是一种肠促胰岛素分泌剂,在维持人体血糖稳定中发挥着重要作用。与目前临床使用的药物相比,胰高血糖素样肽-1受体激动剂(GLP-1RA)在治疗2型糖尿病(T2DM)中显示出更好的应用前景,低血糖风险低,不会导致体重增加。但是,由于人体自身GLP-1的半衰期很短(约2 min),容易被二肽基肽酶-4(DPP-4)降解,这限制了它在糖尿病治疗领域的应用。本文梳理了具有抗DPP-4酶活性的GLP-1RA,如艾塞那肽、利拉鲁肽、索马鲁肽、度拉鲁肽、利司那肽等已上市产品的概况。另外还汇总了GLP-1RA在中国以及美国用药指南中的变化。近年,随着对GLP-1RA认识的逐步深入,GLP-1RA在T2DM治疗中的地位稳步提升。未来,随着GLP-1RA口服制剂的开发,GLP-1RA与胰岛素、GLP-1RA与其他激素的联合应用,都将使GLP-1RA在T2DM治疗中发挥更大的作用。Glucagon-like peptide-1 (GLP-1) is an incretin that plays important physiological roles in glucose homeostasis.GLP-1 receptor agonists (GLP-1RA) have shown better potential to treat type-2 diabetes mellitus (T2DM) as compared to currently used drugs in clinic without causing the side effects of hypoglycemia and weight gain.But,the short half-life (around 2 minutes) and degradation by dipeptidyl peptidase-4 enzyme (DPP-4) limit the therapeutic utility of GLP-1.In this review,we discussed DPP-4 resistant GLP-1RA drugs currently on market such as exenatide,liraglutide,semaglutide,dulaglutide,lixisenatide,etc.We also summarized the changes in the guidelines for GLP-1RA drugs in China and the United States.In recent years,with the deepening of people’s understanding of GLP-1RA,the therapeutic status of GLP-1RA drugs in the treatment of T2DM has been steadily improved.In the future,with the development of oral preparations for GLP-1RA,the combinational therapy of GLP-1RA with insulin or other hormones will make GLP-1RA play a greater role in the treatment of T2DM.

关 键 词：胰高血糖素样肽-1 受体激动剂 2型糖尿病 

分 类 号：R971.43[医药卫生—药品]