[9][13][18] Tirzepatide was approved for treatment of diabetes in the United States in May 2022,[9][13] in the European Union in September 2022,[11] in Canada in November 2022,[19] and in Australia in December 2022.

[8][23] In December 2024, the FDA revised the indication for tirzepatide (as Zepbound) to include the treatment of moderate to severe obstructive sleep apnea.

[10][17] Tirzepatide (as Mounjaro) is indicated to improve blood sugar control in adults with type 2 diabetes, as an addition to diet and exercise.

[10] Tirzepatide has demonstrated significant benefits in obese patients with a common type of heart failure, preserved ejection fraction (HFpEF) in a phase III trial.

[24][25] Over two years, tirzepatide reduced the risk of major complications, including urgent heart failure visits, hospitalizations, increased diuretic treatment, and cardiovascular-related deaths, by 38% compared to placebo.

Tirzepatide is a linear polypeptide of 39 amino acids that has been chemically modified by lipidation to improve its uptake into cells and its stability to metabolism.

[35] At the GLP-1 receptor, though, tirzepatide shows bias towards cAMP (a messenger associated with regulation of glycogen, sugar, and lipid metabolism) generation, rather than β-arrestin recruitment.

This combination of preference towards GIP receptor and distinct signaling properties at GLP-1 suggest this biased agonism increases insulin secretion.

[14] Tirzepatide is an analog of the human GIP hormone with a C20 fatty diacid portion attached, used to optimise the uptake and metabolism of the compound.

[37] After passing phase III clinical trials, Eli Lilly applied to the US Food and Drug Administration (FDA) for approval in October 2021, with a priority review voucher.

[39] Following the completion of the SURPASS-2 trial (NCT03987919), the company announced in April 2022, that tirzepatide had successfully met their clinical endpoints in obese and overweight participants without diabetes.

[16] In August 2024, the SURMOUNT-1 three-year study (176-week treatment period) revealed that tirzepatide reduced the risk of developing type 2 diabetes by 94% in adults with pre-diabetes and obesity or overweight.

[11][49] In December 2024, the FDA approved tirzepatide (Zepbound) as the first medication to be used in the treatment of moderate to severe obstructive sleep apnea.

[17][50][51] The FDA granted the application for tirzepatide (Zepbound) fast track, priority review, and breakthrough therapy designations for the treatment of moderate to severe obstructive sleep apnea.

[60] A systematic review and meta-analysis, published in 2024, found that tirzepatide demonstrates benefits in the management of metabolic dysfunction–associated steatotic liver disease.