胰高血糖素样肽-1受体激动剂的新时代。

Q3 Medicine
Revue medicale de Liege Pub Date : 2023-01-01
M F Neuville, N Paquot, A J Scheen
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引用次数: 0

摘要

胰高血糖素样肽-1 (GLP-1)受体激动剂在2型糖尿病(T2D)的治疗中具有特殊的地位。它们不仅改善血糖控制而不引起低血糖和引发体重减轻,而且还可以预防动脉粥样硬化性心血管疾病。增加其中三种药物(利拉鲁肽、西马鲁肽、杜拉鲁肽)的剂量可以获得更好的血糖效果,并可能有更大的减肥效果。利拉鲁肽的日剂量为3.0 mg,西马鲁肽的周剂量为2.4 mg是治疗肥胖的指征。最近的一项创新包括开发针对GLP-1和GIP(“葡萄糖依赖性胰岛素多肽”)受体(替西肽)或GLP-1和胰高血糖素受体(余肽)的双单分子激动剂。在exceed项目中,替西帕肽显示糖化血红蛋白水平和体重的显著降低,比dulaglutide或semaglutide观察到的更大。替西帕肽获得了治疗T2D的适应症,目前正在肥胖症中进行测试(SURMOUNT项目)。有趣的是,triagonists GIP/GLP-1/胰高血糖素目前被开发用于治疗T2D和肥胖,也有治疗代谢相关脂肪肝疾病的前景。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
[A new era for glucagon-like peptide-1 receptor agonists].

Glucagon-like peptide-1 (GLP-1) receptor agonists have a privileged place in the management of type 2 diabetes (T2D). They not only improve glucose control without inducing hypoglycaemia and trigger weight loss, but also protect against atherosclerotic cardiovascular disease. Increasing the dose of three of them (liraglutide, semaglutide, dulaglutide) allows better glycaemic results and of potential interest a greater weight reduction. Liraglutide at a daily dose of 3.0 mg and semaglutide at a weekly dose of 2.4 mg received the indication for the therapy of obesity. A recent innovation consists in the development of dual unimolecular agonists that target GLP-1 and GIP («glucose-dependent insulinotropic polypeptide») receptors (tirzepatide) or GLP-1 and glucagon receptors (cotadutide). Tirzepatide, in the SURPASS programme, showed impressive reductions in glycated haemoglobin level and body weight, greater than those observed with dulaglutide or semaglutide. Tirzepatide received the indication of the treatment of T2D and is currently tested in obesity (SURMOUNT programme). Interestingly, triagonists GIP/GLP-1/glucagon are currently developed for the management of T2D and obesity, with also perspectives for treating metabolic-associated fatty liver disease.

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来源期刊
Revue medicale de Liege
Revue medicale de Liege Medicine-Medicine (all)
CiteScore
0.80
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期刊介绍: The Medical Review of Liege is a tool for continuous medical training being addressed to students, general practitioners, and specialists
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