Retatrutide is an active compound called retaglutide released by Eli Lilly in June 2023. It is a triple (GLP-1/GIP/Gcg) agonist based on the GLP/GI dual receptor agonist Tirzepatide through a hybrid glucagon (GlucagonGcg) related structure, and is a drug for the development of obesity and type 2 diabetes. This active compound can activate receptor agonists in our body, which helps control blood sugar and weight loss management. Its sequence is H-Tyr-Aib-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-Aib-Leu-Asp-Lys-Ile-Ala-Gln-{20diacid-gamma-Glu-(AEEA)2-Lys}-Ala-Phe-Val-Gln-Trp-Leu-Ile-Ala-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2
The third position of the Retatrutide peptide chain is a glycine (G) residue, and the 13th position is an unnatural amino acid aMeL (a-methyl-L-leucine) residue. The use of the unnatural amino acid aMeL enhances the activity of the peptide chain for GIP and glucagon receptors. The 17th position is a lysine (K) residue, and a dibasic fatty acid side chain is introduced on this residue through AEEA and y-glutamic acid (yGlu) linkers to achieve a prolonged in vivo action time. At the 20th position of the Retatrutide peptide chain, the non-natural amino acid Aib is used to prevent the peptide chain from being degraded by dipeptidyl peptidase 4 (DDP4) at this position. The 24th and 28th positions of the peptide chain are optimized to glutamic acid (E) residues, and the 25th position is optimized to tyrosine (Y) residues.
A 12-week Phase 1b clinical trial conducted from December 18, 2018 to December 28, 2020 on patients with type 2 diabetes showed that the three high-dose groups of Retatrutide were significantly better than the placebo control group in reducing blood sugar and glycosylated hemoglobin (HbA1c), and showed a dose-related weight loss effect.
On June 23, 2023, Eli Lilly published online the results of the Phase 2 clinical trial of Retatrutide for obese and overweight patients published in The New England Journal of Medicine. The 12mg dose group of Retatrutide achieved a weight loss effect of 17.5% at week 24 and 24.2% at week 48.
The results of a phase 2 clinical trial of Retatrutide for patients with type 2 diabetes were published in The Lancet on August 12, 2023. The 12mg dose group of Retatrutide was significantly superior to 1.5mg of dulaglutide in reducing sugar HbA1c and weight loss in the 4mg and above dose groups.
Although Retatrutide's triple agonist has outstanding results in the field of obesity, Retatrutide has not yet obtained the US FDA. Studies have shown that Retatrutide also has adverse reactions. The most common adverse events are gastrointestinal reactions. These events are dose-related and are mostly mild to moderate in severity. Lower starting doses (2mg vs. 4mg) can partially alleviate them. The dose-dependent increase in heart rate peaks at 24 weeks and then declines.
Obesity is a chronic disease (similar to hypertension), so it is necessary to control it through long-term treatment. Simple medication or injections will undoubtedly help some patients, but it is not the only way to solve the complex problem of obesity. Instead, a variety of measures should be taken to curb the environment that causes obesity, including effectively guiding the high-calorie, high-fat, ultra-processed food industry and market, as well as creating a more convenient and safer walking and cycling environment to promote physical exercise.
Our company can provide custom peptide class
