Tirzepatide - a dual GIP/GLP-1 receptor agonist - a new antidiabetic drug with potential metabolic activity in the treatment of type 2 diabetes.

IF 2 4区医学 Q3 ENDOCRINOLOGY & METABOLISM

Endokrynologia Polska Pub Date : 2022-05-20 DOI:10.5603/EP.a2022.0029

M. Nowak, W. Nowak, W. Grzeszczak

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引用次数: 4

Abstract

The incretin hormones glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) are responsible for up to 65% of postprandial insulin secretion. Tirzepatide, developed by Eli Lilly, is a dual GIP/GLP-1 receptor agonist in the form of a synthetic linear peptide; its acylation technology allows it to bind to albumin, thus making it possible to dose the drug once a week. This review summarizes the key characteristics and pharmacokinetics of tirzepatide. The authors present the results of a phase 1, 2, and 3 clinical trial on the effects of tirzepatide on glycaemic and lipid control and the beneficial effects on body weight in a dose-dependent manner in patients with type 2 diabetes mellitus (T2DM). Tirzepatide has the ability to reduce glycaemic levels, improve insulin sensitivity, reduce body weight, and improve lipid metabolism, which is critically important in T2DM. Tirzepatide administered by weekly subcutaneous injections appears to be a promising drug for the treatment of T2DM as well as cardiometabolic disorders. The mechanism of action and safety profile of tirzepatide potentially fills important gaps in the current treatment of T2DM.

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tizepatide -一种双GIP/GLP-1受体激动剂-一种治疗2型糖尿病具有潜在代谢活性的新型降糖药物。

肠促胰岛素激素胰高血糖素样肽1（GLP-1）和葡萄糖依赖性促胰岛素多肽（GIP）负责高达65%的餐后胰岛素分泌。礼来公司开发的替西帕肽是一种合成线性肽形式的双GIP/GLP-1受体激动剂；它的酰化技术使它能够与白蛋白结合，从而使每周给药一次成为可能。本文综述了替西帕肽的主要特点和药代动力学。作者介绍了一项1、2和3期临床试验的结果，该试验研究了替西帕肽对2型糖尿病（T2DM）患者血糖和脂质控制的影响，以及剂量依赖性对体重的有益影响。替西帕肽具有降低血糖水平、改善胰岛素敏感性、减轻体重和改善脂质代谢的能力，这在T2DM中至关重要。每周皮下注射替西帕肽似乎是一种治疗T2DM和心脏代谢紊乱的有前景的药物。替西帕肽的作用机制和安全性可能填补目前T2DM治疗的重要空白。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Endokrynologia Polska ENDOCRINOLOGY & METABOLISM-

CiteScore

2.60

自引率

9.50%

发文量

129

审稿时长

6-12 weeks

期刊介绍： "Endokrynologia Polska" publishes papers in English on all aspects of clinical and experimental endocrinology. The following types of papers may be submitted for publication: original articles, reviews, case reports, postgraduate education, letters to the Editor (Readers’ Forum) and announcements of scientific meetings, conferences and congresses.