艾塞那肽的抗糖尿病机制及临床应用进展  

Progress on antidiabetic mechanism and clinical application of exenatide

作　　者：刘延杰[1] 季虹[1] 林鲁霞[1] 荣海钦[1] 

机构地区：[1]山东省医学科学院山东省内分泌与代谢病研究所,山东济南250062

出　　处：《中国新药与临床杂志》2011年第6期407-411,共5页Chinese Journal of New Drugs and Clinical Remedies

基　　金：山东省科技攻关计划项目(2009GG20002046);山东省科技攻关计划项目(2009GG20002049)

摘　　要：艾塞那肽是首个获准上市的肠促胰素类似物药物,可模拟人体自身胰高糖素样肽1(GLP-1)的功能,降低健康受试者和2型糖尿病患者的体重、空腹和餐后血糖,降低糖化血红蛋白,同时促进胰岛β细胞新生、增殖,抑制β细胞凋亡,改善β细胞功能,促进胰岛素分泌,增加机体对胰岛素的敏感性,延缓胃排空和减少摄食量等,因而有着传统治疗糖尿病药物不可比拟的优点,近年来已经成为糖尿病治疗领域的研究热点,应用前景非常广阔。本文对艾塞那肽的药动学、临床疗效及抗糖尿病作用机制作一综述。Exenatide was the first-approved drug of incretin mimetics class, which acts like the naturally occurring hormone glucagon like peptide-1 （GLP-1） in vivo. Exenatide decreases fasting and postprandial plasma glucose levels and glycosylated hemoglobin Ale, as well as the bodyweights in healthy volunteers and type 2 diabetes patients. Present evidence suggests that the above effects of exenatide may obtain through a glucose-dependent stimulation of insulin secretion, and maintenance of β-cell mass by promotion of islet-cell proliferation and neogenesis, and inhibition of islet-cell apoptosis. Moreover, the randomized trials show that exenatide slows gastric emptying time and reduces food intake. In this article, the pharmacokinetic profiles and effective mechanisms of exenatide, as well as its clinical application were briefly reviewed.

关 键 词：糖尿病 2型 胰高血糖素样肽1 降血糖药 艾塞那肽 

分 类 号：R977.15[医药卫生—药品]