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中国临床药理学与治疗学 ›› 2023, Vol. 28 ›› Issue (2): 220-227.doi: 10.12092/j.issn.1009-2501.2023.02.014

• 综述与讲座 • 上一篇    下一篇

新型胰高血糖素样肽-1受体/葡萄糖依赖性促胰岛素多肽受体双重激动剂——Tirzepatide

赵世峰1,宋向明1,姚建平2   

  1. 1湖州市中心医院药剂科,2内分泌科,湖州 313000,浙江
  • 收稿日期:2022-10-31 修回日期:2023-01-11 出版日期:2023-02-26 发布日期:2023-03-10
  • 通讯作者: 姚建平,男,本科,主任医师,副教授,研究方向:糖尿病、内分泌罕见病。 E-mail: gtl52@163.com
  • 作者简介:赵世峰,男,本科,副主任药师,研究方向:临床药学。 E-mail: thecloudknows@yeah.net
  • 基金资助:
    浙江省卫生健康科技计划(新技术产品研发项目,2022PY092)

Tirzepatide: A new glucagon-like peptide-1 receptor/glucose-dependent insulinotropic peptide receptor dual agonist

ZHAO Shifeng1,  SONG Xiangming1, YAO Jianping2   

  1. 1Department of Pharmacy, 2Department of Endocrinology, Huzhou Central Hospital, Huzhou 313000, Zhejiang, China
  • Received:2022-10-31 Revised:2023-01-11 Online:2023-02-26 Published:2023-03-10

摘要: Tirzepatide为全球首个胰高血糖素样肽-1(glucagon-like peptide-1, GLP-1)受体和葡萄糖依赖性促胰岛素多肽(glucose-dependent insulinotropic peptide, GIP)受体双重激动剂,通过模拟天然GLP-1和GIP发挥多种生理效应。在已完成的SURPASS和SURMOUNT大型Ⅲ期系列临床研究中,Tirzepatide展现了优异的降低糖化血红蛋白、减轻体质量和改善血脂等代谢指标的效果,并且优于当前获批的GLP-1受体激动剂。胃肠道反应为该药最常见不良事件,一般为轻至中度,随着持续给药而减少。2022年5月13日,Tirzepatide由美国食品药品监督管理局(FDA)批准上市,当前适应症为作为饮食和运动的辅助,以改善成人2型糖尿病(type 2 diabetes, T2D)患者的血糖控制。除T2D和肥胖外,针对其他多种代谢领域目前也有着广泛而深入的研究开展。本文现对此作一系统综述。

关键词: Tirzepatide, 2型糖尿病, 肥胖, 胰高血糖素样肽-1, 葡萄糖依赖性促胰岛素多肽

Abstract: Tirzepatide is the first-in-class dual agonist of glucagon-like peptide-1 (GLP-1) receptor  and glucose-dependent insulinotropic peptide (GIP) receptor, which plays a variety of physiological effects by imitating natural GLP-1 and GIP. In the completed large phase Ⅲ series of clinical studies of SURPASS and SURMOUNT, Tirzepatide has demonstrated excellent effects in decreasing glycosylated hemoglobin, reducing weight, improving blood lipid and other metabolic indicators, and is superior to the currently approved GLP-1 receptor agonist. Gastrointestinal reaction is the most common adverse event of the drug, which is generally mild to moderate, and decreases with continuous administration. On May 13, 2022, Tirzepatide was approved for listing by FDA, the current indication is to improve glycemic control of adult patients with type 2 diabetes (T2D) as an adjunct of diet and exercise. In addition to T2D and obesity, there are also extensive and in-depth studies on other metabolic fields. This paper makes a systematic overview of this.

Key words: tirzepatide, type 2 diabetes, obesity, glucagon-like peptide-1, glucose-dependent insulinotropic peptide 

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