Tirzepatide: Uses and Mechanism of Action

Tirzepatide is a medication that is FDA approved for the treatment of type 2 diabetes mellitus

. It is a synthetic linear peptide molecule containing 39 amino acids, based on the sequence of endogenous gastric inhibitory polypeptide (GIP)

. Tirzepatide is a dual GIP and glucagon-like peptide-1 (GLP-1) receptor agonist, which means that it works by stimulating both the GIP and GLP-1 receptors in the body

.The GIP receptor is considered the dominant insulinotropic hormone when compared with GLP-1 and has demonstrated a stronger role in postprandial insulin secretion

. Tirzepatide works to stimulate first- and second-phase insulin secretion, and reduces glucagon levels, both in a glucose-dependent manner

. It also delays gastric emptying, lowers fasting and postprandial glucose levels, and reduces food intake

.Tirzepatide has been shown to be effective in reducing body weight in overweight and obese patients with type 2 diabetes. In a global phase 3 trial, patients with obesity and type 2 diabetes or with overweight and type 2 diabetes lost an estimated 34.4 pounds (15.7%) of body weight with 10 mg and 15 mg of tirzepatide

. The SURMOUNT-2 study found that individuals with type 2 diabetes and obesity lost an average of 15% of their body weight after 72 weeks of treatment with tirzepatide

.Tirzepatide is administered as a once-a-week subcutaneous injectable

. It is currently implemented as a second-line diabetes medication, similar to GLP-1 medications

. Tirzepatide is also being studied for its potential use in treating obesity

.In summary, tirzepatide is a medication that works as a dual GIP and GLP-1 receptor agonist to stimulate insulin secretion, reduce glucagon levels, delay gastric emptying, lower glucose levels, and reduce food intake. It has been shown to be effective in reducing body weight in overweight and obese patients with type 2 diabetes. Tirzepatide is administered as a once-a-week subcutaneous injectable.

Citations:

[1] https://pubmed.ncbi.nlm.nih.gov/33325008/

[2] https://go.drugbank.com/drugs/DB15171

[3] https://www.ncbi.nlm.nih.gov/books/NBK585056/

[4] https://pubmed.ncbi.nlm.nih.gov/36050763/

[5] https://pubmed.ncbi.nlm.nih.gov/32730231/

[6] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9268041/

[7] https://www.frontiersin.org/articles/10.3389/fendo.2022.1004044/full

[8] https://en.wikipedia.org/wiki/Tirzepatide

[9] https://investor.lilly.com/news-releases/news-release-details/lillys-tirzepatide-achieved-157-weight-loss-adults-obesity-or

[10] https://investor.lilly.com/news-releases/news-release-details/fda-approves-lillys-mounjarotm-tirzepatide-injection-first-and

[11] https://cardiab.biomedcentral.com/articles/10.1186/s12933-022-01604-7

[12] https://www.nejm.org/doi/full/10.1056/NEJMoa2206038

[13] https://www.thelancet.com/journals/lancet/article/PIIS0140-6736(21)01324-6/fulltext

[14] https://diabetesjournals.org/clinical/article-pdf/40/3/371/685512/diaclincd220038.pdf

[15] https://diabetesjournals.org/clinical/article/40/3/371/146993/An-Introduction-to-Tirzepatide

[16] https://www.nature.com/articles/s42255-023-00811-0

[17] https://www.pharmacytimes.com/view/clinical-overview-tirzepatide-for-type-2-diabetes

[18] https://www.sciencedirect.com/science/article/pii/S1056872722002446

[19] https://academic.oup.com/ajhp/article/80/14/879/7127416

[20] https://www.sciencedirect.com/topics/medicine-and-dentistry/tirzepatide

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