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.
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Tirzepatide is the first dual GLP-1 and GIP receptor agonist approved by the FDA for the treatment of both type 2 diabetes and obesity.
“Tirzepatide, a dual GLP-1 and GIP RA, is the first co-agonist targeting glucose-regulating peptides approved by the FDA for the treatment of both type 2 diabetes and obesity [22].”
From Delayed gastric emptying induced by glucagon-like peptide-1 receptor agonists and its implications for perioperative risk during anesthesia (2026) · cites this paper as [22]
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References 31 · Cited by 43
- Authors
- Tall Bull, S., Nuffer, W., & Trujillo, J. M.
- Affiliations
- University of Colorado System (US)
- Venue
- Journal of Diabetes and its Complications
- Publisher
- Elsevier BV
- Published
- 2022-12
- Volume
- 36
- Issue
- 12
- Pages
- 108332
- ISSN
- 0891-6632 (ISSN-L)
- 1056-8727
- OpenAlex
- W4302024172
- Cited by
- 43
- References
- 31
- Citations by year
- 2026: 13 · 2025: 14 · 2024: 10 · 2023: 6
- FWCI
- 1.07
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- Locations
- Journal of Diabetes and its Complications (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes Treatment and Management
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes Management and Research
- Health Sciences › Medicine › Pharmacology › Pharmacology and Obesity Treatment
- Keywords
- tirzepatide, type 2 diabetes, GIP/GLP-1 receptor agonist, SURPASS trials, HbA1c, weight loss, gastrointestinal adverse effects, hypoglycemia risk, treatment algorithm, semaglutide, insulin degludec, insulin glargine
- MeSH terms
- Glucagon-Like Peptide-1 Receptor, Glucagon-Like Peptide-1 Receptor Agonists, Tirzepatide, Diabetes Mellitus, Type 2, Gastric Inhibitory Polypeptide, Glycated Hemoglobin, Humans, Hypoglycemic Agents, Weight Loss, Clinical Trials, Phase III as Topic
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