♔ Brief Introduction:
Retatrutide is an active compound 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 treatment 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.
♔ Sequence:
H-Tyr-Aib-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-α-Me-Leu-Leu-Asp-Lys-{diacid-C20-gamma-Glu-(AEEA)-Lys}-Ala-Gln-Aib-Ala-Phe-Ile-Glu-Tyr-Leu-Leu-Glu-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2
♔ Mechanism of Action:
Retatrutide achieves comprehensive metabolic regulation through triple receptor activation:
GLP-1R: Slows gastric emptying, enhances satiety, and reduces appetite.
GIPR: Regulates hunger signals in the central nervous system, further suppresses appetite and improves energy metabolism.
GCGR: Promotes glucagon secretion, accelerates fat and glycogenolysis, and increases basal metabolic rate.
♔ Indications and Efficacy:
1) Obesity Treatment:
In the Phase II clinical trial, patients in the highest dose group (12 mg) lost an average of 24.2% weight after 48 weeks, and some patients lost more than 30%.
2) Metabolic Dysfunction-Associated Fatty Liver Disease (MASLD):
Retatrutide can reduce liver fat content by 86%, and more than 85% of patients achieve regression of liver steatosis.
3) Type 2 Diabetes:
Significantly reduce glycated hemoglobin (HbA1c) and improve blood sugar control.
4) Potential Cardiovascular Benefits:
Animal studies have shown that it may indirectly protect cardiovascular health by improving blood pressure and heart function, but further clinical verification is needed.