胰高血糖素样肽-1受体激动剂类药物的临床应用

The clinical experience of GLP-1 receptor agonist drugs

对肠促胰素在维持葡萄糖稳定作用的认识,促进了对2型糖尿病患者以肠促胰素活性缺乏为靶向的药物研发。胰高血糖素样肽-1(GLP-1)是在营养物质的刺激下由小肠L细胞分泌的一种肽类激素。由于天然GLP-1循环半衰期短,需要开发新型GLP-1受体激动剂以便于临床应用。GLP-1受体激动剂以葡萄糖浓度依赖性刺激胰岛素分泌,还具有抑制胰高血糖素分泌和减慢胃排空,抑制食欲等作用。GLP-1受体激动剂作为治疗糖尿病的新型药物得到广泛应用。新的临床证据表明,GLP-1受体激动剂除了良好的血糖控制作用外还具有较好的安全性和心血管益处。文章综述GLP-1受体激动剂的临床疗效和安全性,剖析此类药物在2型糖尿病治疗中的地位。

Increased understanding of the role of incretin hormones in maintaining glucose homeostasis has enabled the development of pharmacotherapy that target deficient incretin activity in type 2 diabetes mellitus. Glucagon-like peptide-1 （ GLP-1 ） is a peptide hormone secreted from the small intestine in response to nutrient ingestion. Because of the short circu- lating half-life of the native GLP-1, novel GLP-1 receptor （GLP-1 R） agonists have been developed to facilitate clinical use. GLP-1R agonists stimulate insulin secretion in a glucose dependent manner. GLP-1R agonists can inhibit glueagon secretion and gastric emptying and reduce appetite. As new antidiabetic drugs, GLP-1R agonists have been widely used. BEmerging evidence indicate that GLP-l-based therapy are safe and may provide cardiovascular-benefits beyond glycemic control. This article reviews the clinical aspects of efficacy and safety of GLP-1R agonists and elucidates their roles in treating type 2 diabetes mellitus.