Tirzepatide

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, for the treatment of adults with type 2 diabetes, making it the first and only GIP and GLP-1 receptor agonist for this indication. On September 15, 2022, tirzepatide was also approved by the European Commission.

Tirzepatide is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. In Europe, it may be used as monotherapy or in combination with other drugs used to treat diabetes.

This drug has not been studied in patients with a history of pancreatitis. Tirzepatide is not indicated for use in patients with type 1 diabetes mellitus.