Selvarajan Raja, Subramanian Rashmi
Department of Diabetes and Research Kaveri Healthcare, Bangalore, Karnataka, India.
Department of Research and Development, Kaveri Healthcare, Bangalore, Karnataka, India.
Diabetes Metab Syndr Obes. 2023 Jun 8;16:1709-1720. doi: 10.2147/DMSO.S385196. eCollection 2023.
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.
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。