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替尔泊肽:用于 2 型糖尿病的治疗。

Tirzepatide: A Review in Type 2 Diabetes.

机构信息

Springer Nature, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand.

出版信息

Drugs. 2024 Feb;84(2):227-238. doi: 10.1007/s40265-023-01992-4. Epub 2024 Feb 23.

Abstract

Tirzepatide (Mounjaro), a first-in-class dual incretin agonist of the glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors, is approved for use as an adjunct to diet and exercise to improve glycaemic control in adults with type 2 diabetes mellitus (T2DM) in the USA, EU, Japan and other countries. It comes as single-dose prefilled pens and single-dose vials. In phase III SURPASS trials, once-weekly subcutaneous tirzepatide, as monotherapy or add-on-therapy to oral glucose-lowering medications and insulin, was superior to the GLP-1 receptor agonists (RAs) dulaglutide 0.75 mg and semaglutide 1 mg as well as basal and prandial insulin for glycaemic control and weight loss in adults with inadequately controlled T2DM. Tirzepatide was generally well tolerated, with a safety profile consistent with that of GLP-1 RAs. Tirzepatide was associated with a low risk of clinically significant or severe hypoglycaemia and no increased risk of major adverse cardiovascular events. Adverse events were mostly mild to moderate in severity, with the most common being gastrointestinal events including nausea, diarrhoea, decreased appetite and vomiting. In conclusion, tirzepatide is a valuable addition to the treatment options for T2DM.

摘要

替尔泊肽(Mounjaro),一种新型的葡萄糖依赖性胰岛素促泌多肽(GIP)和胰高血糖素样肽-1(GLP-1)受体双重激动剂,已在美国、欧盟、日本和其他国家批准用于辅助饮食和运动,改善 2 型糖尿病(T2DM)成人的血糖控制。它有预填充笔和单剂量小瓶两种剂型。在 III 期 SURPASS 试验中,每周一次皮下注射替尔泊肽作为单药或联合口服降糖药和胰岛素治疗,在血糖控制和体重减轻方面优于 GLP-1 受体激动剂(RAs)度拉糖肽 0.75mg 和司美格鲁肽 1mg 以及基础和餐时胰岛素,适用于血糖控制不佳的 T2DM 成人。替尔泊肽总体耐受性良好,安全性与 GLP-1 RAs 一致。替尔泊肽与临床显著或严重低血糖的风险低,与主要不良心血管事件的风险增加无关。不良反应大多为轻至中度,最常见的是胃肠道事件,包括恶心、腹泻、食欲下降和呕吐。总之,替尔泊肽是 T2DM 治疗选择的有价值的补充。

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