Gupta Vishal
Department of Endocrinology, Jaslok Hospital and Research Centre, 15 - Dr. Deshmukh Marg, Pedder Road, Mumbai, Maharashtra, India.
Indian J Endocrinol Metab. 2013 May;17(3):413-21. doi: 10.4103/2230-8210.111625.
Abnormalities of the incretin axis have been implicated in the pathogenesis of type 2 diabetes mellitus. Glucagon-like peptide-1 (GLP-1) and gastroinhibitory intestinal peptide constitutes >90% of all the incretin function. Augmentation of GLP-1 results in improvement of beta cell health in a glucose-dependant manner (post-prandial hyperglycemia) and suppression of glucagon (fasting hyperglycemia), amongst other beneficial pleiotropic effects. Native GLP-1 has a very short plasma half-life and novel methods have been developed to augment its half life, such that its anti-hyperglycemic effects can be exploited. They can be broadly classified as exendin-based therapies (exenatide, exenatide once weekly), DPP-4-resistant analogues (lixisenatide, albiglutide), and analogues of human GLP-1 (liraglutide, taspoglutide). Currently, commercially available analogues are exenatide, exenatide once weekly, and liraglutide. This review aims to provide an overview of most GLP-1 analogues.
肠促胰岛素轴异常与2型糖尿病的发病机制有关。胰高血糖素样肽-1（GLP-1）和胃抑制性肠肽构成了所有肠促胰岛素功能的90%以上。GLP-1的增加以葡萄糖依赖的方式（餐后高血糖）改善β细胞健康，并抑制胰高血糖素（空腹高血糖），以及产生其他有益的多效性作用。天然GLP-1的血浆半衰期非常短，现已开发出新方法来延长其半衰期，以便能够利用其降血糖作用。它们大致可分为基于艾塞那肽的疗法（艾塞那肽、每周一次的艾塞那肽）、二肽基肽酶-4（DPP-4）抗性类似物（利司那肽、阿必鲁肽）和人GLP-1类似物（利拉鲁肽、塔司鲁肽）。目前，市售的类似物有艾塞那肽、每周一次的艾塞那肽和利拉鲁肽。本综述旨在概述大多数GLP-1类似物。
