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口服司美格鲁肽的疗效和安全性评价

A Review on the Efficacy and Safety of Oral Semaglutide.

机构信息

East Coast Institute for Research, LLC, 3550 University Blvd. South, Suite 101, Jacksonville, FL, 32216, USA.

College of Pharmacy, University of Florida, Jacksonville, FL, USA.

出版信息

Drugs R D. 2021 Jun;21(2):133-148. doi: 10.1007/s40268-021-00341-8. Epub 2021 Mar 26.

Abstract

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.

摘要

目前有许多治疗 2 型糖尿病患者的方案可供选择;然而,许多患者的血糖水平仍未得到充分控制,其当前的抗高血糖方案也是如此。此外,美国糖尿病协会指南越来越强调多因素管理的重要性,以及优化药物治疗方案,包括心血管、肾脏和/或体重获益,适用于 2 型糖尿病患者。胰高血糖素样肽-1 受体激动剂属于 2 型糖尿病药物的一个新类别,由于其能够改善血糖状况而不会导致低血糖风险,因此越来越受欢迎。目前,有三种美国食品和药物管理局批准的胰高血糖素样肽-1 受体激动剂,即皮下注射的司美格鲁肽、度拉糖肽和利拉鲁肽,也被批准用于降低 2 型糖尿病和已确诊心血管疾病患者的主要不良心血管事件。然而,由于这些药物需要皮下注射,它们通常不是首选药物。然而,口服司美格鲁肽与吸收增强剂的联合使用已经表明可以提高其生物利用度,并使其口服吸收成为可能。在 PIONEER 试验中,口服司美格鲁肽有效地降低了血糖水平,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,尚未获得食品和药物管理局的批准。与皮下制剂相比,口服司美格鲁肽的这些特性可能会改善并增加其使用,并可能在实现血糖控制的同时更早地提供心血管保护。

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A Review on the Efficacy and Safety of Oral Semaglutide.口服司美格鲁肽的疗效和安全性评价
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