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While first-generation compounds primarily targeted the glucagon-like peptide-1 (GLP-1) receptor to suppress appetite and regulate insulin, and second-generation compounds like Tirzepatide added in the glucose-dependent insulinotropic polypeptide (GIP) receptor for enhanced effects, Retatrutide adds a third, crucial target: the glucagon (GCG) receptor

This distinction matters because treating metabolic dysfunction early prevents progression to overt disease