Clinical Research, National Research Institute , Los Angeles, CA, USA.
Expert Rev Endocrinol Metab. 2020 Nov;15(6):379-394. doi: 10.1080/17446651.2020.1830759. Epub 2020 Oct 8.
The glucagon-like peptide-1 (GLP-1) receptor agonists (RA) have increasingly gained prominence in the treatment of type 2 diabetes (T2D) based on their glycemic benefits and favorable body weight and cardiorenal effects. Despite this, continued development of therapeutics with superior efficacy is important to help address persistent challenges in the attainment of metabolic goals in many patients with T2D.
Tirzepatide is an unimolecular dual glucose-dependent insulinotropic polypeptide (GIP)/GLP-1 RA in development for the treatment of T2D. This review summarizes key characteristics of tirzepatide and Phase 1 and Phase 2 clinical trial efficacy and safety results. Additionally, it provides an overview of the ongoing Phase 3 clinical trial program in T2D and briefly summarizes recently initiated studies in patients with obesity and nonalcoholic steatohepatitis. Information in this review comes primarily from published clinical trials, manufacturer's websites, and ClinicalTrials.gov.
Based on data from Phase 2 trials, tirzepatide has the potential to be the most efficacious therapy in T2D with respect to both glucose and body weight control. Data from the ongoing Phase 3 clinical trial program should start to become available in late 2020 and will determine the future course of this promising therapeutic agent.
基于其血糖益处和有利的体重及心脏肾脏作用，胰高血糖素样肽-1（GLP-1）受体激动剂（RA）在 2 型糖尿病（T2D）的治疗中日益受到重视。尽管如此，继续开发疗效更优的治疗药物对于帮助解决许多 T2D 患者在实现代谢目标方面持续存在的挑战仍然很重要。
替尔泊肽是一种正在开发用于治疗 T2D 的单分子双重葡萄糖依赖性胰岛素促分泌多肽（GIP）/GLP-1 RA。这篇综述总结了替尔泊肽的关键特征以及 1 期和 2 期临床试验的疗效和安全性结果。此外，它还概述了正在进行的 T2D 3 期临床试验计划，并简要总结了最近在肥胖和非酒精性脂肪性肝炎患者中开展的研究。本综述中的信息主要来自已发表的临床试验、制造商的网站和 ClinicalTrials.gov。
基于 2 期试验数据，替尔泊肽有可能成为在控制血糖和体重方面最有效的 T2D 治疗药物。正在进行的 3 期临床试验计划的数据应于 2020 年末开始公布，这将决定这一有前途的治疗药物的未来走向。
