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药丸中的肽——口服司美格鲁肽用于2型糖尿病的管理

A Peptide in a Pill - Oral Semaglutide in the Management of Type 2 Diabetes.

作者信息

Selvarajan Raja, Subramanian Rashmi

机构信息

Department of Diabetes and Research Kaveri Healthcare, Bangalore, Karnataka, India.

Department of Research and Development, Kaveri Healthcare, Bangalore, Karnataka, India.

出版信息

Diabetes Metab Syndr Obes. 2023 Jun 8;16:1709-1720. doi: 10.2147/DMSO.S385196. eCollection 2023.

Abstract

T2DM (type 2 diabetes mellitus) is a chronic and progressive illness with high morbidity and death rates. Oral semaglutide (Rybelsus®) is a combination of semaglutide, a glucagon-like peptide-1 receptor agonist (GLP-1 RA), and sodium N- (8- [2-hydroxybenzoyl] amino) caprylate (SNAC), an absorption enhancer that facilitates semaglutide absorption across the gastric epithelium in a concentration-dependent manner. This family of drugs apart from glucose lowering effects causes significant weight loss with lower risk of hypoglycemia, and some of them have been linked to a significant reduced major adverse cardiovascular events. GLP-1 RAs may assist persons with T2DM and chronic kidney disease (CKD), a major microvascular consequence of T2DM, in ways other than lowering blood sugar. Several large clinical studies, the bulk of which are cardiovascular outcome trials, show that GLP-1 RA treatment is safe and tolerated for persons with T2DM and impaired renal function and that it may potentially have renoprotective characteristics. This article focuses on the advances of oral GLP1-RA and describes the key milestones and predicted advantages.

摘要

2型糖尿病(T2DM)是一种发病率和死亡率都很高的慢性进行性疾病。口服司美格鲁肽(Rybelsus®)是司美格鲁肽(一种胰高血糖素样肽-1受体激动剂(GLP-1 RA))与N-(8- [2-羟基苯甲酰基]氨基)辛酸钠(SNAC,一种吸收促进剂)的组合,SNAC以浓度依赖的方式促进司美格鲁肽跨胃上皮的吸收。这类药物除了具有降血糖作用外,还能显著减轻体重,低血糖风险较低,其中一些药物还与主要不良心血管事件的显著减少有关。GLP-1 RA可能通过降低血糖以外的方式帮助患有T2DM和慢性肾脏病(CKD,T2DM的主要微血管并发症)的患者。几项大型临床研究,其中大部分是心血管结局试验,表明GLP-1 RA治疗对患有T2DM和肾功能受损的患者是安全且耐受性良好的,并且它可能具有潜在的肾脏保护特性。本文重点介绍口服GLP-1 RA的进展,并描述其关键里程碑和预期优势。

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The integrative biology of type 2 diabetes.2 型糖尿病的综合生物学。
Nature. 2019 Dec;576(7785):51-60. doi: 10.1038/s41586-019-1797-8. Epub 2019 Dec 4.

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