研究动态
Articles below are published ahead of final publication in an issue. Please cite articles in the following format: authors, (year), title, journal, DOI.

瑞他鲁肽在肥胖症(和 2 型糖尿病)方面显示出前景。

Retatrutide showing promise in obesity (and type 2 diabetes).

发表日期:2023 Nov 10
作者: Sheila A Doggrell
来源: EXPERT OPINION ON INVESTIGATIONAL DRUGS

摘要:

肥胖是心血管疾病、糖尿病、骨关节炎和某些癌症的主要危险因素。瑞他鲁肽可刺激胰高血糖素样肽1(GLP-1)、葡萄糖依赖性促胰岛素多肽(GIP)受体和胰高血糖素受体,正在开发用于治疗肥胖和2型糖尿病。瑞他鲁肽的2期临床试验(LY3437943) )治疗肥胖症。主要终点是体重从基线到 24 周的百分比变化,随着瑞他鲁肽的剂量从 1mg 增加到 12mg,变化范围为 -7.2% 到 -~18%。最常见的不良事件是胃肠道(恶心、腹泻、呕吐)。瑞他鲁肽治疗肥胖(和糖尿病)的第 2 期研究结果大多令人鼓舞。与作为 GLP-1 受体激动剂一致,瑞他鲁肽可使心率增加高达 6.7 次/分钟,这可能是有害的,并抵消了减肥的一些好处。据推测,瑞他鲁肽正在被开发作为最近开发的减肥药物的挑战者;索马鲁肽和/或替泽帕肽。因此,需要在瑞他鲁肽和这些药物之间进行比较研究,但目前没有一项研究正在进行中,在我看来,这种缺乏是瑞他鲁肽开发中的一个重大遗漏。
Obesity is a major risk factor for cardiovascular disease, diabetes, osteoarthritis, and some cancers. Retatrutide stimulates Glucagon-like peptide 1 (GLP-1), Glucose-dependent insulinotropic polypeptide (GIP) receptors, and glucagon receptors, and is being developed for the treatment of obesity and type 2 diabetes.A phase 2 clinical trial of retatrutide (LY3437943) in the treatment of obesity. The primary end point was percentage change in weight from baseline to 24 weeks, which ranged from -7.2% to -~18% as the dose of retatrutide increased from 1 mg to 12 mg. The most frequent adverse events were gastrointestinal (nausea, diarrhea, vomiting).The results for retatrutide in phase 2 for obesity (and diabetes) are mostly encouraging. Consistent with being a GLP-1 receptor agonist, heart rate was increased by up to 6.7 beats/min by retatrutide, which may be detrimental and offset some of the benefits of weight loss. Presumably, retatrutide is being developed as a challenger to the recently developed weight loss medicines; semaglutide and/or tirzepatide. Thus, comparator studies are needed between retatrutide and these drugs, but none are ongoing and, in my opinion, this lack is a major omission in the development of retatrutide.