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A Review on the Efficacy and Safety of Oral Semaglutide
Drugs in R&D ( IF 3 ) Pub Date : 2021-03-26 , DOI: 10.1007/s40268-021-00341-8
Stephanie Niman 1 , Jennifer Hardy 1 , Rebecca F Goldfaden 1 , Jessica Reid 1, 2 , Mae Sheikh-Ali 3 , David Sutton 3 , Rushab Choksi 1
Affiliation  

There are numerous treatment options currently available for patients with type 2 diabetes mellitus; however, a multitude of patients continue to have inadequately controlled glycemic levels with their current antihyperglycemic regimen. Furthermore, the American Diabetes Association guidelines increasingly highlight the importance of multifactorial management and optimizing medication regimens that include cardiovascular, renal, and/or weight benefits in patients with type 2 diabetes mellitus. Glucagon-like peptide-1 receptor agonists belong to a novel class of type 2 diabetes mellitus agents that are becoming increasingly prevalent owing to their ability to improve glycemic status without the risk of hypoglycemia. Currently, there are three US Food and Drug Administration-approved glucagon-like peptide-1 receptor agonists, subcutaneous semaglutide, dulaglutide, and liraglutide, that also have an indication for reducing major adverse cardiovascular events in patients with type 2 diabetes mellitus and established cardiovascular disease. However, these agents are not often the first options because of their subcutaneous administration. Nevertheless, co-formulation of oral semaglutide with an absorption enhancer has shown to increase its bioavailability and has made its oral absorption possible. In the PIONEER trials, oral semaglutide effectively lowered blood glucose levels, and showed benefits on weight and cardiovascular outcomes; however, there is no Food and Drug Administration indication approved yet as the SOUL trial is still ongoing. Such characteristics of oral semaglutide may improve and increase its use compared to subcutaneous agents and possibly lead to earlier cardiovascular protection in addition to achieving glycemic control.



中文翻译:

口服司美鲁肽的疗效和安全性综述

目前有多种治疗选择可用于 2 型糖尿病患者;然而,许多患者通过目前的抗高血糖方案仍无法充分控制血糖水平。此外,美国糖尿病协会指南越来越强调多因素管理和优化药物治疗方案的重要性,包括对 2 型糖尿病患者的心血管、肾脏和/或体重益处。胰高血糖素样肽 1 受体激动剂属于一类新型 2 型糖尿病药物,由于它们能够改善血糖状态而没有低血糖风险,因此变得越来越流行。目前,美国食品和药物管理局批准了三种胰高血糖素样肽-1受体激动剂,皮下注射semaglutide、dulaglutide和liraglutide,也有减少2型糖尿病和已确诊心血管疾病患者主要不良心血管事件的适应症。然而,这些药物通常不是首选,因为它们是皮下给药。尽管如此,口服司美鲁肽与吸收促进剂的复合制剂已显示增加其生物利用度并使其口服吸收成为可能。在 PIONEER 试验中,口服司美鲁肽可有效降低血糖水平,并显示出对体重和心血管结局的益处;然而,由于 SOUL 试验仍在进行中,因此尚无食品和药物管理局批准的适应症。

更新日期:2021-03-27
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