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替尔泊肽:一种新型的、首创的、双重 GIP/GLP-1 受体激动剂。

Tirzepatide: A novel, first-in-class, dual GIP/GLP-1 receptor agonist.

机构信息

University of Colorado Skaggs School of Pharmacy and Pharmaceutical Sciences, United States of America.

Department of Clinical Pharmacy, University of Colorado Skaggs School of Pharmacy and Pharmaceutical Sciences, United States of America.

出版信息

J Diabetes Complications. 2022 Dec;36(12):108332. doi: 10.1016/j.jdiacomp.2022.108332. Epub 2022 Oct 5.

Abstract

The objective of this article is to review the efficacy and safety of tirzepatide and discuss its potential role in the treatment of type 2 diabetes. Tirzepatide is a novel once-weekly dual GIP and GLP-1 receptor agonist which has been studied in the SURPASS clinical trials in doses of 5 mg, 10 mg, and 15 mg. Tirzepatide phase III clinical trials, SURPASS-1 through SURPASS-5, demonstrate that this medication is safe and effective in treating type 2 diabetes both with and without a variety of background medications versus placebo, semaglutide, insulin degludec, and insulin glargine in different patient populations. Most adverse events were gastrointestinal in nature, with a relatively low withdrawal rate in the active treatment arms. It seems likely that tirzepatide will be recommended as a preferred option in the American Diabetes Association treatment algorithm for high glucose lowering effects in patients with a compelling need for low hypoglycemia risk and weight loss. However, the positioning of tirzepatide in the treatment algorithm will ultimately be dependent on the results of the cardiovascular outcomes trial (CVOT) or other outcome-based trials. Tirzepatide is effective for treating type 2 diabetes by lowering glycated hemoglobin and contributing to significant weight loss.

摘要

本文旨在回顾替西帕肽的疗效和安全性,并探讨其在 2 型糖尿病治疗中的潜在作用。替西帕肽是一种新型每周一次的双重 GIP 和 GLP-1 受体激动剂,已在 SURPASS 临床试验中进行了 5mg、10mg 和 15mg 剂量的研究。替西帕肽的 III 期临床试验(SURPASS-1 至 SURPASS-5)表明,该药物在治疗 2 型糖尿病方面是安全有效的,无论是否使用各种背景药物,与安慰剂、司美格鲁肽、德谷胰岛素和甘精胰岛素相比,在不同的患者人群中。大多数不良事件是胃肠道性质的,在活性治疗组中相对较低的退出率。替西帕肽似乎很可能被推荐为美国糖尿病协会治疗算法中的首选方案,以实现对低血糖风险和体重减轻有强烈需求的患者的高血糖降低效果。然而,替西帕肽在治疗算法中的定位最终将取决于心血管结局试验(CVOT)或其他基于结果的试验的结果。替西帕肽通过降低糖化血红蛋白和显著减轻体重对 2 型糖尿病有效。

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