Tirzepatide: A novel, first-in-class, dual GIP/GLP-1 receptor agonist
- PMID: 36375235
- DOI: 10.1016/j.jdiacomp.2022.108332
Tirzepatide: A novel, first-in-class, dual GIP/GLP-1 receptor agonist
Abstract
The objective of this article is to review the efficacy and safety of tirzepatide and discuss its potential role in the treatment of type 2 diabetes. Tirzepatide is a novel once-weekly dual GIP and GLP-1 receptor agonist which has been studied in the SURPASS clinical trials in doses of 5 mg, 10 mg, and 15 mg. Tirzepatide phase III clinical trials, SURPASS-1 through SURPASS-5, demonstrate that this medication is safe and effective in treating type 2 diabetes both with and without a variety of background medications versus placebo, semaglutide, insulin degludec, and insulin glargine in different patient populations. Most adverse events were gastrointestinal in nature, with a relatively low withdrawal rate in the active treatment arms. It seems likely that tirzepatide will be recommended as a preferred option in the American Diabetes Association treatment algorithm for high glucose lowering effects in patients with a compelling need for low hypoglycemia risk and weight loss. However, the positioning of tirzepatide in the treatment algorithm will ultimately be dependent on the results of the cardiovascular outcomes trial (CVOT) or other outcome-based trials. Tirzepatide is effective for treating type 2 diabetes by lowering glycated hemoglobin and contributing to significant weight loss.
Keywords: Antihyperglycemics; Diabetes; Drug information; Medication safety; Tirzepatide; Type 2.
Copyright © 2022. Published by Elsevier Inc.
Conflict of interest statement
Declaration of competing interest The authors declared the following potential conflicts of interest with respect to the research, authorship, and/or publication of this article: Dr. Jennifer Trujillo serves as an advisory board member for Sanofi, Inc. Dr. Tall Bull and Dr. Nuffer have no conflicts to disclose.
Similar articles
-
Tirzepatide, the Newest Medication for Type 2 Diabetes: A Review of the Literature and Implications for Clinical Practice.Ann Pharmacother. 2023 Jul;57(7):822-836. doi: 10.1177/10600280221134127. Epub 2022 Nov 11. Ann Pharmacother. 2023. PMID: 36367094 Review.
-
Tirzepatide, a dual GIP/GLP-1 receptor co-agonist for the treatment of type 2 diabetes with unmatched effectiveness regrading glycaemic control and body weight reduction.Cardiovasc Diabetol. 2022 Sep 1;21(1):169. doi: 10.1186/s12933-022-01604-7. Cardiovasc Diabetol. 2022. PMID: 36050763 Free PMC article. Review.
-
Tirzepatide versus Semaglutide Once Weekly in Patients with Type 2 Diabetes.N Engl J Med. 2021 Aug 5;385(6):503-515. doi: 10.1056/NEJMoa2107519. Epub 2021 Jun 25. N Engl J Med. 2021. PMID: 34170647 Clinical Trial.
-
Model-based simulation of glycaemic effect and body weight loss when switching from semaglutide or dulaglutide to once weekly tirzepatide.Curr Med Res Opin. 2024 Apr;40(4):567-574. doi: 10.1080/03007995.2024.2322072. Epub 2024 Mar 12. Curr Med Res Opin. 2024. PMID: 38407177
-
Achievement of glycaemic targets with weight loss and without hypoglycaemia in type 2 diabetes with the once-weekly glucose-dependent insulinotropic polypeptide and glucagon-like peptide-1 receptor agonist tirzepatide: A post hoc analysis of the SURPASS-1 to -5 studies.Diabetes Obes Metab. 2023 Apr;25(4):965-974. doi: 10.1111/dom.14943. Epub 2022 Dec 27. Diabetes Obes Metab. 2023. PMID: 36514843 Clinical Trial.
Cited by
-
Efficacy and Safety of Tirzepatide Compared with GLP-1 RAs in Patients with Type 2 Diabetes Treated with Basal Insulin: A Network Meta-analysis.Diabetes Ther. 2025 Jun;16(6):1279-1311. doi: 10.1007/s13300-025-01728-5. Epub 2025 Apr 11. Diabetes Ther. 2025. PMID: 40214900 Free PMC article.
-
Treatment Options and Continuity of Care in Metabolic-associated Fatty Liver Disease: A Multidisciplinary Approach.Eur Cardiol. 2024 Jun 19;19:e06. doi: 10.15420/ecr.2023.34. eCollection 2024. Eur Cardiol. 2024. PMID: 38983581 Free PMC article. Review.
-
Novel Dual Incretin Receptor Agonists in the Spectrum of Metabolic Diseases with a Focus on Tirzepatide: Real Game-Changers or Great Expectations? A Narrative Review.Biomedicines. 2023 Jul 1;11(7):1875. doi: 10.3390/biomedicines11071875. Biomedicines. 2023. PMID: 37509514 Free PMC article. Review.
-
Pharmacotherapy for obesity: are we ready to select, tailor and combine pharmacotherapy to achieve more ambitious goals?Front Endocrinol (Lausanne). 2025 Jun 18;16:1569468. doi: 10.3389/fendo.2025.1569468. eCollection 2025. Front Endocrinol (Lausanne). 2025. PMID: 40607226 Free PMC article. Review.
-
US Population Eligibility and Estimated Impact of Tirzepatide Treatment on Obesity Prevalence and Cardiovascular Disease Events.Cardiovasc Drugs Ther. 2025 Aug;39(4):837-847. doi: 10.1007/s10557-024-07583-z. Epub 2024 Jun 8. Cardiovasc Drugs Ther. 2025. PMID: 38850368 Free PMC article.
Publication types
MeSH terms
Substances
LinkOut - more resources
Full Text Sources
Medical