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本文引用的文献

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Addendum. 9. Pharmacologic Approaches to Glycemic Treatment: . Diabetes Care 2020;43(Suppl. 1):S98-S110.附录9. 血糖治疗的药理学方法:《糖尿病护理》2020年;43(增刊1):S98 - S110。
Diabetes Care. 2020 Aug;43(8):1979. doi: 10.2337/dc20-ad08a. Epub 2020 Jun 5.
2
Dose-response, efficacy, and safety of oral semaglutide monotherapy in Japanese patients with type 2 diabetes (PIONEER 9): a 52-week, phase 2/3a, randomised, controlled trial.口服司美格鲁肽单药治疗日本 2 型糖尿病患者的剂量反应、疗效和安全性(PIONEER 9):一项 52 周、2/3a 期、随机、对照试验。
Lancet Diabetes Endocrinol. 2020 May;8(5):377-391. doi: 10.1016/S2213-8587(20)30075-9.
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Oral semaglutide in type 2 diabetes.口服司美格鲁肽治疗 2 型糖尿病。
J Diabetes Complications. 2020 Apr;34(4):107520. doi: 10.1016/j.jdiacomp.2019.107520. Epub 2020 Jan 8.
4
8. Obesity Management for the Treatment of Type 2 Diabetes: .8. 肥胖症管理用于 2 型糖尿病的治疗: 。
Diabetes Care. 2020 Jan;43(Suppl 1):S89-S97. doi: 10.2337/dc20-S008.
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Glucagon-like peptide 1 (GLP-1).胰高血糖素样肽 1(GLP-1)。
Mol Metab. 2019 Dec;30:72-130. doi: 10.1016/j.molmet.2019.09.010. Epub 2019 Sep 30.
6
Efficacy, Safety, and Tolerability of Oral Semaglutide Versus Placebo Added to Insulin With or Without Metformin in Patients With Type 2 Diabetes: The PIONEER 8 Trial.在伴有或不伴有二甲双胍的胰岛素治疗基础上加用口服司美格鲁肽与安慰剂治疗 2 型糖尿病患者的疗效、安全性和耐受性:PIONEER 8 试验。
Diabetes Care. 2019 Dec;42(12):2262-2271. doi: 10.2337/dc19-0898. Epub 2019 Sep 17.
7
Oral Semaglutide Versus Empagliflozin in Patients With Type 2 Diabetes Uncontrolled on Metformin: The PIONEER 2 Trial.口服司美格鲁肽对比恩格列净在二甲双胍控制不佳的 2 型糖尿病患者中的疗效:PIONEER 2 研究。
Diabetes Care. 2019 Dec;42(12):2272-2281. doi: 10.2337/dc19-0883. Epub 2019 Sep 17.
8
Oral Semaglutide: A Review of the First Oral Glucagon-Like Peptide 1 Receptor Agonist.口服司美格鲁肽:首个口服胰高血糖素样肽-1 受体激动剂的综述。
Diabetes Technol Ther. 2020 Jan;22(1):10-18. doi: 10.1089/dia.2019.0185. Epub 2019 Oct 1.
9
Strategies for Appropriate Selection of SGLT2-i vs. GLP1-RA in Persons with Diabetes and Cardiovascular Disease.糖尿病合并心血管疾病患者中 SGLT2-i 与 GLP1-RA 的合理选择策略。
Curr Cardiol Rep. 2019 Jul 27;21(9):100. doi: 10.1007/s11886-019-1197-6.
10
Efficacy and safety of oral semaglutide with flexible dose adjustment versus sitagliptin in type 2 diabetes (PIONEER 7): a multicentre, open-label, randomised, phase 3a trial.口服司美格鲁肽灵活剂量调整与西格列汀治疗 2 型糖尿病的疗效和安全性(PIONEER 7):一项多中心、开放标签、随机、3a 期临床试验。
Lancet Diabetes Endocrinol. 2019 Jul;7(7):528-539. doi: 10.1016/S2213-8587(19)30194-9. Epub 2019 Jun 9.

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.

DOI:10.1007/s40268-021-00341-8
PMID:33772451
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8206300/
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。