Tirzepatide is a novel dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist.

Dual GIP/GLP-1 agonists gained increasing attention as new therapeutic agents for glycemic and weight control as they demonstrated better glucose control and weight loss compared to selective GLP-1 receptor agonists in preclinical and clinical trials.

Tirzepatide comprises a 39 amino acid linear synthetic peptide conjugated to a C20 fatty diacid moiety. Its protein sequence was based on the sequence of endogenous GIP, and its pharmacological action on GLP-1 receptors is comparable to endogenous GIP; however, the long half-life of tirzepatide allows for once-weekly dosing.

Tirzepatide was approved by the FDA on May 13, 2022, under the brand name MOUNJARO by the FDA for the treatment of adults with type 2 diabetes, making it the first and only GIP and GLP-1 receptor agonist for this indication. Later, it was approved under a different brand name ZEPBOUND on November 8, 2023, for the chronic weight management in adults with obesity or overweight with at least one weight-related condition. On September 15, 2022, tirzepatide was also approved by the European Commission.