Back to Registry

Tirzepatide

Also known as: Mounjaro, Zepbound

FDA Approved

Molecular Formula

C225 H348 N48 O68

Molecular Weight

4,813.53 Da

Half-Life

~120 hours (5 days)

Sequence

YXEGTFTSDYSIXLDKIAQKAFVQWLIAGGPSSGAPPPS (X = α-aminoisobutyric acid [Aib]; K20 modified with C20 fatty diacid; C-terminus: L-serinamide)

Clinical Applications & Evidence

Mechanism of Action

Tirzepatide operates as an imbalanced dual incretin receptor agonist. It selectively binds to the GIP receptor with an affinity comparable to native GIP, while binding to the GLP-1 receptor with a deliberately weaker affinity than native GLP-1. This action stimulates glucose-dependent insulin secretion from pancreatic beta cells, suppresses inappropriate postprandial glucagon secretion from alpha cells, significantly delays gastric emptying to blunt postprandial glucose excursions, and modulates hypothalamic pathways to induce profound satiety and reduce caloric intake.

Investigated Uses

  • Type 2 Diabetes Mellitus
  • Chronic weight management
  • Heart failure with preserved ejection fraction (HFpEF)
  • Metabolic dysfunction-associated steatohepatitis (MASH)
  • Obstructive sleep apnea (OSA)
Extensive Clinical Data

Regulatory & Safety Status

FDA Status

FDA Approved

WADA / Athletic Status

Not Prohibited

Known Side Effects

NauseaDiarrheaDecreased appetiteVomitingConstipationDyspepsia

Contraindications

  • Personal or family history of medullary thyroid carcinoma
  • Multiple endocrine neoplasia syndrome type 2

Drug Interactions

  • Insulin secretagogues (e.g., sulfonylureas)
  • Exogenous insulin
  • Narrow therapeutic index oral medications (e.g., warfarin)
  • Oral hormonal contraceptives

Citations & Clinical Trials

PubMed Tirzepatide: A Systematic Update FDA FDA clarifies policies for compounders as national GLP-1 supply begins to stabilize New England Journal of Medicine Tirzepatide for Metabolic Dysfunction–Associated Steatohepatitis with Liver Fibrosis American College of Cardiology Tirzepatide for Heart Failure with Preserved Ejection Fraction and Obesity (SUMMIT) Eli Lilly Investor Relations Tirzepatide Reduced Obstructive Sleep Apnea Severity