Diabetes Research Group, Ulster University, Coleraine, UK.
Br J Pharmacol. 2022 Feb;179(4):526-541. doi: 10.1111/bph.15485. Epub 2021 May 10.
Glucagon-like peptide-1 (GLP-1) is an incretin hormone that has undergone a revolutionary turnaround from discovery to clinically approved therapeutic. Rapid progress in drug design and formulation has led from initial development of short- and long-acting drugs suitable for daily or weekly parenteral administration, respectively, through to the most recent approval of an orally active GLP-1 agent. The current review outlines the biological action profile of GLP-1 including the various beneficial metabolic responses in pancreatic and extra-pancreatic tissues, including the gastrointestinal tract, liver, bone and kidney as well as the reproductive cardiovascular and CNS. We then briefly consider clinically approved GLP-1 receptor ligands and recent advances in this field. Given the sustained evolution in the area of GLP-1 drug development and excellent safety profile, as well as the plethora of metabolic benefits, clinical approval for use in diseases beyond diabetes and obesity is very much conceivable. LINKED ARTICLES: This article is part of a themed issue on GLP1 receptor ligands (BJP 75th Anniversary). To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v179.4/issuetoc.
胰高血糖素样肽-1(GLP-1)是一种肠促胰岛素激素,经历了从发现到临床批准治疗的革命性转变。药物设计和配方的快速发展,使得最初开发的短效和长效药物分别适合每日或每周的皮下注射,进而到最近批准的一种口服活性 GLP-1 药物。本综述概述了 GLP-1 的生物学作用谱,包括在胰腺和胰腺外组织(包括胃肠道、肝脏、骨骼和肾脏以及生殖、心血管和中枢神经系统)中的各种有益代谢反应。然后我们简要讨论了临床批准的 GLP-1 受体配体和该领域的最新进展。鉴于 GLP-1 药物开发领域的持续发展和出色的安全性,以及众多代谢益处,在糖尿病和肥胖症以外的疾病中使用的临床批准是非常可以想象的。
本文是 GLP1 受体配体专题的一部分(BJP 75 周年纪念)。要查看本节中的其他文章,请访问 http://onlinelibrary.wiley.com/doi/10.1111/bph.v179.4/issuetoc.