What Is Retatrutide?
Retatrutide (LY3437943) is a triple agonist peptide targeting the glucagon receptor (GCGR), glucose-dependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R).
Retatrutide binds to human GCGR, GIPR and GLP-1R with EC₅₀ values of 5.79 nM, 0.0643 nM and 0.775 nM, respectively. It is a promising research agent for obesity studies.
Main Efficacy
1. Retatrutide is primarily indicated for the treatment of obesity. It can significantly reduce body weight, assist obese or overweight patients in weight management, and ameliorate metabolic disorders induced by obesity.
2. Retatrutide can markedly decrease hepatic fat content and improve various metabolic biomarkers associated with metabolic dysfunction-associated steatotic liver disease (MASLD), including enhanced insulin sensitivity and improved blood lipid profiles.
Mechanism of Action
Retatrutide exerts a simultaneous agonistic effect on three hormone receptors implicated in obesity and metabolism: glucose-dependent insulinotropic polypeptide (GIP) receptor, glucagon-like peptide-1 (GLP-1) receptor, and glucagon receptor (GCGR). These targeted mechanisms are recognized as the primary contributors to its high efficacy in weight reduction and metabolic improvement.
