Tirzepatide Peptide Profile

Overview:
Tirzepatide is a synthetic dual‑agonist peptide medication that targets both the glucose‑dependent insulinotropic polypeptide (GIP) receptor and the glucagon‑like peptide‑1 (GLP‑1) receptor, often described as a “twincretin.” This dual receptor activity enhances glucose‑dependent insulin secretion, suppresses inappropriate glucagon release, slows gastric emptying, reduces appetite, and improves overall metabolic regulation. It has a long half‑life due to structural modification (lipidation enabling albumin binding) that allows once‑weekly subcutaneous dosing. Tirzepatide is approved in many regions (e.g., USA, Europe) for type 2 diabetes (as Mounjaro®) and chronic weight management (as Zepbound®) in adults with obesity or overweight with comorbid conditions. (Wikipedia)

Mechanism of Action:
Tirzepatide simultaneously stimulates GIP and GLP‑1 receptors, producing synergistic effects:

  • Enhances insulin secretion in response to meals and improves β‑cell function. (NCBI)
  • Reduces glucagon levels and slows gastric emptying, promoting better glycemic control. (Drugs.com)
  • Suppresses appetite through central hypothalamic pathways and supports weight loss. (TAF Clinic)

Clinical Effects:
In clinical trials (e.g., SURPASS, SURMOUNT), tirzepatide produced significant reductions in body weight (up to ~22–23 % over 72 weeks) and improved glycemic control compared with comparators including semaglutide and insulin therapies. (Drugs.com)

Side Effects & Safety:
Common adverse effects include nausea, vomiting, diarrhea, constipation, abdominal pain, and decreased appetite, typically mild to moderate and dose‑dependent, and often improve over time. (Nuvance Health)

Tirzepatide Dosing Chart (Approved Clinical Guidelines)
| Dose | Frequency | Indication | Notes |
| 2.5 mg | Once weekly | Initiation (type 2 diabetes/weight management) | Not effective long term; starting dose to improve tolerability. (Medscape) |
| 5 mg | Once weekly | Maintenance (T2D/weight) | Standard maintenance; increase after 4 weeks. (Medscape) |
| 7.5 mg | Once weekly | Maintenance escalation | Optional higher dose if needed and tolerated. (kentandmedwayformulary.nhs.uk) |
| 10 mg | Once weekly | Maintenance escalation | Frequently used mid‑range dose in trials. (kentandmedwayformulary.nhs.uk) |
| 12.5 mg | Once weekly | Higher dose | Optional escalation for further control/weight loss. (kentandmedwayformulary.nhs.uk) |
| 15 mg | Once weekly | Maximum approved dose | Highest recommended maintenance dose. (U.S. Food and Drug Administration) |

References (APA):
Tirzepatide. (n.d.). Wikipedia. https://en.wikipedia.org/wiki/Tirzepatide (Wikipedia)
Tirzepatide – StatPearls. (2024). NCBI Bookshelf. https://www.ncbi.nlm.nih.gov/books/NBK585056/ (NCBI)
Tirzepatide (Zepbound): Uses, Dosage, Side Effects. (n.d.). Drugs.com. https://www.drugs.com/tirzepatide.html (Drugs.com)
Tirzepatide (Mounjaro®) Injection, for subcutaneous use. (2022). FDA Label. (Lilly Insights)
Jastreboff, A. M., et al. (2022). Tirzepatide Once Weekly for Obesity. New England Journal of Medicine. (New England Journal of Medicine)
Tirzepatide – Uses & Side Effects. (n.d.). WebMD. (webmd.com)