Diabetes Research Center, Department of Medicine, Gentofte Hospital, University of Copenhagen, Denmark; Department of Biomedical Sciences, Faculty of Health Sciences, University of Copenhagen, Denmark.
Diabetes Research Center, Department of Medicine, Gentofte Hospital, University of Copenhagen, Denmark.
Eur J Intern Med. 2014 Jun;25(5):407-14. doi: 10.1016/j.ejim.2014.03.005. Epub 2014 Mar 30.
Glucagon-like peptide-1 (GLP-1) is a gastrointestinal hormone, secreted in response to ingestion of nutrients, and has important effects on several of the pathophysiological features of type 2 diabetes (T2D). The effects include potentiation of insulin secretion, suppression of glucagon secretion, slowing of gastric emptying and suppression of appetite. In circulation, GLP-1 has a half-life of approximately 2min due to rapid degradation by the enzyme dipeptidyl peptidase 4 (DPP-4). Because of this short half-life GLP-1 receptor (GLP-1R) agonists, resistant to degradation by DPP-4 have been developed. At the moment four different compounds are available for the treatment of T2D and many more are in clinical development. These compounds, although all based on the effects of native GLP-1, differ with regards to structure, pharmacokinetics and size, which ultimately leads to different clinical effects. This review gives an overview of the clinical data on GLP-1R agonists that have been compared in head-to-head studies and focuses on relevant differences between the compounds. Highlighting these similarities and differences could be beneficial for physicians in choosing the best treatment strategy for their patients.
胰高血糖素样肽-1(GLP-1)是一种胃肠激素,在摄入营养物质后分泌,对 2 型糖尿病(T2D)的多种病理生理特征有重要影响。其作用包括增强胰岛素分泌、抑制胰高血糖素分泌、减缓胃排空和抑制食欲。在循环中,由于二肽基肽酶 4(DPP-4)的快速降解,GLP-1 的半衰期约为 2 分钟。由于这种短半衰期,已经开发出了对 DPP-4 具有抗性的 GLP-1 受体(GLP-1R)激动剂。目前有四种不同的化合物可用于治疗 T2D,还有更多的化合物正在临床开发中。这些化合物虽然都基于天然 GLP-1 的作用,但在结构、药代动力学和大小方面存在差异,最终导致了不同的临床效果。本综述概述了在头对头研究中进行比较的 GLP-1R 激动剂的临床数据,并重点介绍了这些化合物之间的相关差异。强调这些相似性和差异可能对医生为患者选择最佳治疗策略有所帮助。