PMID- 35830001 OWN - NLM STAT- MEDLINE DCOM- 20220826 LR - 20220826 IS - 1179-1950 (Electronic) IS - 0012-6667 (Linking) VI - 82 IP - 11 DP - 2022 Jul TI - Tirzepatide: First Approval. PG - 1213-1220 LID - 10.1007/s40265-022-01746-8 [doi] AB - Tirzepatide (Mounjaro) is a single molecule that combines dual agonism of glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors. Native GIP and GLP-1 are incretin hormones that stimulate insulin secretion and decrease glucagon secretion. GIP also plays a role in nutrient and energy metabolism, while GLP-1 also delays gastric emptying, supresses appetite and improves satiety. Eli Lilly is developing tirzepatide for the treatment of type 2 diabetes mellitus (T2DM), obesity, cardiovascular disorders in T2DM, heart failure, non-alcoholic steatohepatitis, obstructive sleep apnoea and for reducing mortality/morbidity in obesity. In May 2022, tirzepatide received its first approval in the USA to improve glycaemic control in adults with T2DM, as an adjunct to diet and exercise. Tirzepatide is in phase III development for heart failure, obesity and cardiovascular disorders in T2DM, and in phase II development for non-alcoholic steatohepatitis. This article summarizes the milestones in the development of tirzepatide leading to this first approval for T2DM. CI - (c) 2022. The Author(s), under exclusive licence to Springer Nature Switzerland AG. FAU - Syed, Yahiya Y AU - Syed YY AD - Springer Nature, Mairangi Bay, Private Bag 65901, Auckland, 0754, New Zealand. dru@adis.com. LA - eng PT - Journal Article PT - Review PL - New Zealand TA - Drugs JT - Drugs JID - 7600076 RN - 0 (Glucagon-Like Peptide-1 Receptor) RN - 59392-49-3 (Gastric Inhibitory Polypeptide) RN - 89750-14-1 (Glucagon-Like Peptide 1) RN - OYN3CCI6QE (tirzepatide) SB - IM MH - Adult MH - *Diabetes Mellitus, Type 2/drug therapy/metabolism MH - *Fatty Liver MH - Gastric Inhibitory Polypeptide MH - Glucagon-Like Peptide 1 MH - Glucagon-Like Peptide-1 Receptor MH - *Heart Failure/drug therapy MH - Humans MH - Obesity/drug therapy/metabolism EDAT- 2022/07/14 06:00 MHDA- 2022/08/27 06:00 CRDT- 2022/07/13 11:25 PHST- 2022/07/14 06:00 [pubmed] PHST- 2022/08/27 06:00 [medline] PHST- 2022/07/13 11:25 [entrez] AID - 10.1007/s40265-022-01746-8 [pii] AID - 10.1007/s40265-022-01746-8 [doi] PST - ppublish SO - Drugs. 2022 Jul;82(11):1213-1220. doi: 10.1007/s40265-022-01746-8.