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It is classified as a nonpeptide small-molecule GLP-1 receptor agonist (GLP-1 RA), developed to overcome some of the limitations of peptide-based GLP-1 medications, including poor oral bioavailability and rapid enzymatic breakdown in the gut

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Tirzepatide activates GIP receptor with potency comparable to native GIP, but activates GLP-1 receptor with potency lower than native GLP-1