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INTRODUCTION Tirzepatide is a synthetic peptide composed of 39 amino acids, which functions as a dual receptor agonist (RA) binding both the glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors and this unique mechanism of action resulted in the nickname twincretin. The structure of tirzepatide is based on that of the native GIP with the addition of a 20-carbon fatty diacid moiety, which increases its half-life to 5 days allowing for once-weekly administration.1 Studies using animal models of obesity and diabetes have shown that the co-administration of GIP and GLP-1 has synergistic effects in reducing body weight, food consumption, and fat mass.1 Tirzepatides dual agonist activity may result in these benefits in humans as well, as evidenced the significant reductions in glycated hemoglobin (HbA1c) levels and body weight in patients with type 2 diabetes mellitus (T2DM) observed in phase 3 clinical trials (such as, SURPASS
May 2007;5(5):550-5
BMC Pharmacol Toxicol 15:40, 2014
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