Scheen André J, Radermecker Régis P, Paquot Nicolas
Service de diabétologie, nutrition et maladies métaboliques, Centre hospitalier universitaire de Liège, 4000 Liège, Belgique.
Unité de pharmacologie clinique, Centre interdisciplinaire de recherche sur le médicament (CIRM), Liège Université, 4000 Liège, Belgique.
Rev Med Suisse. 2022 Aug 24;18(792):1539-1544. doi: 10.53738/REVMED.2022.18.792.1539.
Tirzepatide is a unimolecular dual agonist of both glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors, which is developed as once-weekly injection for the treatment of type 2 diabetes. Because of the complementarity of action of the two incretins, tirzepatide showed, in a dose-dependent manner (5, 10 and 15 mg), a better efficacy (greater reduction in HbA1c and body weight) compared with placebo, basal insulin and two GLP-1 analogues (dulaglutide and semaglutide) in the SURPASS program. Its cardiovascular protection (versus dulaglutide) is currently tested in SURPASS-CVOT. Finally, studies for the treatment of obesity and metabolic associated fatty liver disease are also ongoing. Gastrointestinal tolerance of tirzepatide appears comparable to that of GLP-1 analogues, except more diarrhoea.
替尔泊肽是一种葡萄糖依赖性促胰岛素多肽（GIP）和胰高血糖素样肽-1（GLP-1）受体的单分子双重激动剂，它被开发为每周一次注射剂用于治疗2型糖尿病。由于这两种肠促胰岛素作用的互补性，在SURPASS项目中，替尔泊肽以剂量依赖性方式（5、10和15毫克）显示出比安慰剂、基础胰岛素和两种GLP-1类似物（度拉糖肽和司美格鲁肽）更好的疗效（糖化血红蛋白和体重降低幅度更大）。其心血管保护作用（与度拉糖肽相比）目前正在SURPASS-CVOT中进行测试。最后，治疗肥胖症和代谢相关脂肪性肝病的研究也在进行中。替尔泊肽的胃肠道耐受性似乎与GLP-1类似物相当，只是腹泻更多。
