
Retatrutide (LY3437943) TFA is a triple agonist peptide that targets the glucagon receptor (GCGR), glucose-dependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). It exhibits inhibitory activity against human GCGR, GIPR, and GLP-1R with EC50 values of 5.79 nM, 0.0643 nM, and 0.775 nM, respectively. Retatrutide TFA is primarily investigated for its potential in obesity research. Beyond its effects on weight reduction, retatrutide has demonstrated significant benefits in glycemic regulation, with 72% of participants experiencing a reversion from prediabetes to normoglycemia. Furthermore, clinical data indicate favorable impacts on cardiovascular health, including notable decreases in systolic and diastolic blood pressure, as well as improvements in lipid profiles.