| Retatrutide Basic information |
| Retatrutide Usage And Synthesis |
| Description | Retpeptide is a novel triple agonist peptide of the glucagon receptor (GCGR), glucose-dependent insulinotropic polypeptide receptor (GIPR) and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide inhibits human GCGR, GIPR and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively and mouse GCGR, GIPR, and GLP-1R with EC50 values of 2.32, 0.191 and 0.794 nM, respectively. It is an important tool for obesity research. Retatrutide potently activates the GLP-1R signaling pathway to stimulate glucose-dependent insulin secretion through activity at the GIP receptor (GIPR) or the GLP-1R. Retatrutide is a synthetic peptide with glucose-lowering effects. It is an antidiabetic agent against type 2 diabetes (T2D), stimulating insulin and suppressing glucagon secretion in a glucose-dependent manner. Retatrutide was also shown to delay gastric emptying, lower fasting and postprandial glucose concentration, decrease food intake and reduce body weight in patients with type 2 diabetes. |
| References | 1. LY3437943, a novel triple glucagon, GIP, and GLP-1 receptor agonist for glycemic control and weight loss: From discovery to clinical proof of concept: T. Coskun, et al.; Cell Metab. 34, 1234 (2022) DOI:10.1016/j.cmet.2022.07.013 2. The novel GIP, GLP-1 and glucagon receptor agonist retatrutide delays gastric emptying: S. Urva, et al.; Diabetes Obes. Metab. 25, 2784 (2023) DOI:10.1111/dom.15167 3. LY3437943, a novel triple GIP, GLP-1, and glucagon receptor agonist in people with type 2 diabetes: a phase 1b, multicentre, double-blind, placebo-controlled, randomised, multiple-ascending dose trial: S. Urva, et al.; Lancet 400, 1869 (2022) DOI:10.1016/S0140-6736(22)02033-5 4. Is retatrutide (LY3437943), a GLP-1, GIP, and glucagon receptor agonist a step forward in the treatment of diabetes and obesity? S.A. Doggrell; Expert Opin. Investig. Drugs 32, 355 (2023) DOI:10.1080/13543784.2023.2206560 5. Differentiation of human subcutaneous adipocytes and measurement of lipolytic function induced by GIP or LY3437943: A. Regmi & W. Roell; STAR Protoc. 4, 102304 (2023) DOI:10.1016/j.xpro.2023.102304 6. Gut hormone co-agonists for the treatment of obesity: from bench to bedside: R. Nogueiras, et al.; Nature Metab. 5, 933 (2023) (Review) DOI:10.1038/s42255-023-00812-z |
