降糖新药exenatide的研究进展

Advances on the research of exenatide

exenatide是首个获FDA批准的肠促胰岛素样类似物,主要通过增加葡萄糖依赖性胰岛素分泌、抑制胰高血糖素分泌等作用调节血糖,可降低健康受试者和2型糖尿病患者的空腹和餐后血糖,同时降低糖化血红蛋白A1c(HbA1c),体重也呈进行性减低。本品可模拟人体内天然的胃肠激素促进胰岛素分泌的过程,用于改善对二甲双胍、磺酰脲类药物联合治疗不满意的2型糖尿病。文中主要从糖尿病动物模型和临床研究两方面,对exenatide的药理作用、作用机制、体内外研究、药物代谢、临床疗效以及不良反应等方面的研究进展进行综述。

Exenatide is the first approved incretin mimetic analogue. It can regulate blood glucose mainly by increasing glucose dependent insulin secretion, inhibiting glucagons secretion and so on. Exenatide may decrease fasting and postprandial plasma glucose in healthy volunteers and type 2 diabetes patients. Glycosylated hemoglobin A1 c （HbA1 c） and body weights are also reduced. It can simulate the process of natural gut hormone promote insulin secretion in vivo. Exenatide is effective for the type 2 diabetes patients who are unsatisfied with the combined treatment of dimethyldiguanide or sulfonylurea. The research advance of exenatide on its pharmacological action, mechanism of action, in vivo and in vitro study, drug metabolism and clinical therapeutic effect was reviewed.