Medizinische Klinik IV, Eberhard-Karls University, Tübingen, Germany.
Drugs. 2011 Sep 10;71(13):1675-88. doi: 10.2165/11592810-000000000-00000.
Novel therapeutic options for type 2 diabetes mellitus based on the action of the incretin hormone glucagon-like peptide (GLP)-1 were introduced in 2005. As injectable GLP-1 receptor agonists acting on the GLP-1 receptor, exenatide and liraglutide are available in many countries. In type 2 diabetes treatment, incretin-based therapies are attractive and more commonly used because of their mechanism of action and safety profile. Stimulation of insulin secretion and inhibition of glucagon secretion by these agents occur in a glucose-dependent manner. Therefore, incretin-based therapies have no intrinsic risk for hypoglycaemia. Furthermore, GLP-1 receptor agonists allow weight loss and lower systolic blood pressure. This review gives a brief overview of the mechanism of action and summarizes the clinical data available on exenatide and liraglutide as established substances. It further highlights the clinical study data of exenatide once weekly as the first long-acting GLP-1 receptor agonist and covers other new long acting GLP-1 receptor agonists currently in clinical development. The placement of GLP-1 receptor agonists in the treatment algorithm of type 2 diabetes is discussed.
2005 年，基于肠促胰岛素激素胰高血糖素样肽-1（GLP-1）作用的新型 2 型糖尿病治疗选择被引入。艾塞那肽和利拉鲁肽作为可注射的 GLP-1 受体激动剂，在许多国家都有应用。在 2 型糖尿病治疗中，基于肠促胰岛素的治疗因其作用机制和安全性而具有吸引力，也更为常用。这些药物通过葡萄糖依赖的方式刺激胰岛素分泌和抑制胰高血糖素分泌。因此，基于肠促胰岛素的治疗不会产生低血糖的内在风险。此外，GLP-1 受体激动剂还可减轻体重并降低收缩压。本文简要概述了其作用机制，并总结了已确立的艾塞那肽和利拉鲁肽的临床数据。此外，本文还重点介绍了作为首个长效 GLP-1 受体激动剂的每周一次艾塞那肽的临床研究数据，并涵盖了目前处于临床开发阶段的其他新型长效 GLP-1 受体激动剂。本文还讨论了 GLP-1 受体激动剂在 2 型糖尿病治疗方案中的定位。
