Department of Endocrinology, Diabetology and Metabolism, Antwerp University Hospital, University of Antwerp, Edegem, Belgium.
Faculty of Medicine and Health Sciences, Laboratory of Experimental Medicine and Paediatrics (LEMP), University of Antwerp, Wilrijk, Belgium.
Diabetes Obes Metab. 2023 Jan;25(1):3-17. doi: 10.1111/dom.14831. Epub 2022 Aug 31.
Tirzepatide is a novel glucose-dependent insulinotropic polypeptide/glucagon-like peptide 1 (GLP-1) receptor agonist approved in the United States as an adjunct to diet and exercise to improve glycaemic control in adults with type 2 diabetes and under investigation for use in chronic weight management, major adverse cardiovascular events and the management of other conditions, including heart failure with preserved ejection fraction and obesity and non-cirrhotic non-alcoholic steatohepatitis. The Phase 3 SURPASS 1-5 clinical trial programme was designed to assess efficacy and safety of once-weekly subcutaneously injected tirzepatide (5, 10 and 15 mg), as monotherapy or combination therapy, across a broad spectrum of people with type 2 diabetes. Use of tirzepatide in clinical studies was associated with marked reductions of glycated haemoglobin (-1.87 to -2.59%, -20 to -28 mmol/mol) and body weight (-6.2 to -12.9 kg), as well as reductions in parameters commonly associated with heightened cardiometabolic risk such as blood pressure, visceral adiposity and circulating triglycerides. In SUPRASS-2, these reductions were greater than with the GLP-1 receptor agonist semaglutide 1 mg. Tirzepatide was well tolerated, with a low risk of hypoglycaemia when used without insulin or insulin secretagogues and showed a generally similar safety profile to the GLP-1 receptor agonist class. Accordingly, evidence from these clinical trials suggests that tirzepatide offers a new opportunity for the effective lowering of glycated haemoglobin and body weight in adults with type 2 diabetes.
替尔泊肽是一种新型葡萄糖依赖性胰岛素促泌多肽/胰高血糖素样肽 1（GLP-1）受体激动剂，已获美国批准与饮食和运动联合使用，以改善 2 型糖尿病成人的血糖控制，目前正在研究用于慢性体重管理、主要不良心血管事件以及其他疾病的治疗，包括射血分数保留型心力衰竭、肥胖症和非肝硬化非酒精性脂肪性肝炎。3 期 SURPASS 1-5 临床试验计划旨在评估每周一次皮下注射替尔泊肽（5、10 和 15mg）作为单药或联合治疗在 2 型糖尿病患者中的疗效和安全性。在临床试验中使用替尔泊肽与糖化血红蛋白显著降低（-1.87 至-2.59%，-20 至-28mmol/mol）和体重减轻（-6.2 至-12.9kg）有关，同时也降低了与心血管代谢风险升高相关的常见参数，如血压、内脏脂肪和循环甘油三酯。在 SUPRASS-2 中，这些降低的幅度大于 GLP-1 受体激动剂司美格鲁肽 1mg。替尔泊肽耐受性良好，与不使用胰岛素或胰岛素促泌剂时低血糖风险低，且与 GLP-1 受体激动剂类药物具有相似的安全性。因此，这些临床试验的证据表明，替尔泊肽为 2 型糖尿病成人有效降低糖化血红蛋白和体重提供了新的机会。
