Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist

• Published in: JCI insight Vol. 5; no. 17
• Main Authors: Willard, Francis S., Douros, Jonathan D., Gabe, Maria B.N., Showalter, Aaron D., Wainscott, David B., Suter, Todd M., Capozzi, Megan E., van der Velden, Wijnand J.C., Stutsman, Cynthia, Cardona, Guemalli R., Urva, Shweta, Emmerson, Paul J., Holst, Jens J., D’Alessio, David A., Coghlan, Matthew P., Rosenkilde, Mette M., Campbell, Jonathan E., Sloop, Kyle W.
• Format: Journal Article
• Language: English
• Published: United States American Society for Clinical Investigation 03.09.2020; American Society for Clinical investigation
• Subjects: Animals; beta-Arrestin 1 - physiology; Blood Glucose - metabolism; Gastric Inhibitory Polypeptide - pharmacology; Glucagon-Like Peptide-1 Receptor - agonists; Hypoglycemic Agents - pharmacology; Insulin - metabolism; Islets of Langerhans - drug effects; Islets of Langerhans - metabolism; Islets of Langerhans - pathology; Male; Mice; Mice, Knockout; Receptors, Gastrointestinal Hormone - agonists; Therapeutics; Therapeutics; Diabetes

Tirzepatide (LY3298176) is a dual GIP and GLP-1 receptor agonist under development for the treatment of type 2 diabetes mellitus (T2DM), obesity, and nonalcoholic steatohepatitis. Early phase trials in T2DM indicate that tirzepatide improves clinical outcomes beyond those achieved by a selective GLP...