tizepatide (Mounjaro®):用于治疗2型糖尿病的GIP/GLP-1受体双重激动剂。

Revue medicale de Liege Pub Date : 2025-09-01
André Scheen
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引用次数: 0

摘要

Tirzepatide是胰高血糖素样肽-1 (GLP-1)和葡萄糖依赖性胰岛素性多肽(GIP)受体的单分子双激动剂,最近在比利时商业化并用于治疗2型糖尿病(T2D)。由于两种肠促胰岛素的互补性,在六项研究中,替西帕肽以剂量依赖性的方式(5、10和15毫克,每周一次皮下注射)与安慰剂、西马鲁肽1毫克、基础胰岛素和餐前胰岛素利斯pro相比,显示出更好的疗效(更大程度地降低HbA1c和体重)。替西肽的耐受性几乎与纯GLP-1受体激动剂相似,有消化不良事件,最常发生在开始治疗后的第一周,这证明了每四周逐步滴定的建议是合理的。tizepatide现在在比利时的条件下被退回,用于治疗体重指数≥30 kg/m²,HbA1c水平bbb7.5 %的抗高血糖治疗患者,包括二甲双胍。这些报销条件与纯GLP-1受体激动剂类似,但比欧洲药品管理局和国际科学协会最新指南验证的适应症更具限制性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
[Tirzepatide (Mounjaro®) : a GIP/GLP-1 receptor dual agonist for the treatment of type 2 diabetes].

Tirzepatide is a unimolecular dual agonist of both glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) receptors, recently commercialized and reimbursed in Belgium for the treatment of type 2 diabetes (T2D). Because of the complementarity of action of the two incretins, tirzepatide showed, in a dose-dependent manner (5, 10 and 15 mg as a once-weekly subcutaneous injection), a better efficacy (greater reduction in HbA1c and body weight) compared with placebo, semaglutide 1 mg, basal insulin and preprandial boluses of insulin lispro in six studies of the SURPASS programme. Tirzepatide tolerance is almost similar to that of pure GLP-1 receptor agonists, with digestive adverse events, most often during the first weeks after initiation, which justifies the recommendation of progressive titration every four weeks. Tirzepatide is now refunded under conditions in Belgium for the treatment of TD2 in patients with a body mass index ≥ 30 kg/m² and a HbA1c level > 7.5 % with antihyperglycaemic therapy including metformin. These reimbursement conditions are similar to those of pure GLP-1 receptor agonists but are more restrictive than the indications validated by the European Medicines Agency and the latest guidelines by international scientific societies.

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