Tirzepatide: A Systematic Update.
Int J Mol Sci · 2022
Last updated 2026-06-16Tirzepatide is a new drug that helps control blood sugar by targeting two hormones, GIP and GLP-1, which are released after eating and stimulate insulin production. In phase III trials (SURPASS 1-5), tirzepatide also lowered blood pressure and reduced LDL cholesterol and triglycerides. The FDA has approved it as a once-weekly injection for diabetes, used alongside diet and exercise. Research is ongoing to explore its use in other conditions.
AI summary of the abstract below.
| Journal | Int J Mol Sci, 2022 |
|---|---|
| Citations | 80 |
| Relative citation ratio | 6.80 |
| NIH percentile | 95 |
| Molecules | tirzepatide |
Abstract
Tirzepatide is a new molecule capable of controlling glucose blood levels by combining the dual agonism of Glucose-Dependent Insulinotropic Polypeptide (GIP) and Glucagon-Like Peptide-1 (GLP-1) receptors. GIP and GLP1 are incretin hormones: they are released in the intestine in response to nutrient intake and stimulate pancreatic beta cell activity secreting insulin. GIP and GLP1 also have other metabolic functions. GLP1, in particular, reduces food intake and delays gastric emptying. Moreover, Tirzepatide has been shown to improve blood pressure and to reduce Low-Density Lipoprotein (LDL) cholesterol and triglycerides. Tirzepatide efficacy and safety were assessed in a phase III SURPASS 1-5 clinical trial program. Recently, the Food and Drug Administration approved Tirzepatide subcutaneous injections as monotherapy or combination therapy, with diet and physical exercise, to achieve better glycemic blood levels in patients with diabetes. Other clinical trials are currently underway to evaluate its use in other diseases. The scientific interest toward this novel, first-in-class medication is rapidly increasing. In this comprehensive and systematic review, we summarize the main results of the clinical trials investigating Tirzepatide and the currently available meta-analyses, emphasizing novel insights into its adoption in clinical practice for diabetes and its future potential applications in cardiovascular medicine.
Verbatim abstract via PubMed 36498958 ↗
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