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Approved medicineGLP-1 / incretin

Tirzepatide

A first-in-class dual agonist of the GIP and GLP-1 receptors, approved as Mounjaro for type 2 diabetes and as Zepbound for chronic weight management. Its dual mechanism delivers some of the largest weight reductions reported in registrational obesity trials.

CompoundTirzepatide
CategoryDual GIP/GLP-1 receptor agonist
ClassGLP-1 and Incretin Therapies
Evidence tierApproved medicine
WADA statusNot individually listed; verify current status if subject to testing
Sold on this siteNo — this is a reference database

Overview

This entry covers Tirzepatide, a dual gip/glp-1 receptor agonist, graded "Approved medicine" in this catalog's evidence system. This compound exists as an approved medicine in at least one major jurisdiction. Approval applies to specific, labeled indications and to the regulated product — not to compounded or research-grade copies.

A first-in-class dual agonist of the GIP and GLP-1 receptors, approved as Mounjaro for type 2 diabetes and as Zepbound for chronic weight management. Its dual mechanism delivers some of the largest weight reductions reported in registrational obesity trials.

Mechanism of Action

Tirzepatide activates both the GLP-1 receptor and the glucose-dependent insulinotropic polypeptide (GIP) receptor. The GIP component is thought to contribute additional effects on adipose tissue insulin sensitivity and energy handling beyond GLP-1-driven appetite suppression, though the exact interaction of the two pathways in humans remains an active research question.

Research and Evidence

In the SURMOUNT-1 trial (n=2,539), the highest dose produced a mean weight reduction of about 20.9% over 72 weeks, versus 3.1% for placebo. SURPASS trials in type 2 diabetes showed robust HbA1c reductions.

Evidence in context: the GLP-1 and Incretin Therapies class page collects the shared evidence themes and study-reading guidance for this category.

Safety and Side Effects

As with GLP-1 agonists, gastrointestinal effects (nausea, vomiting, diarrhea) predominate and are dose-related. Labeled warnings cover gallbladder disease, pancreatitis, and hypoglycemia when combined with insulin secretagogues; the same medullary thyroid carcinoma/MEN2 contraindication applies.

Educational notice: this entry describes published research and, where they exist, regulator labels. It is not medical advice and not a recommendation for use. Research-grade compounds have no verified human-safety data.

Frequently Asked Questions

What is the evidence tier of Tirzepatide?

Tirzepatide is graded "Approved medicine" on this site. This compound exists as an approved medicine in at least one major jurisdiction. Approval applies to specific, labeled indications and to the regulated product — not to compounded or research-grade copies.

Is Tirzepatide an approved medicine?

Tirzepatide exists as an approved medicine in at least one major jurisdiction — but approval covers the regulated product and its labeled indications only. Compounded or research-grade versions of the same molecule are not the approved product.

Where can I read the primary studies for Tirzepatide?

The references section at the end of this entry links the key primary sources — regulator labels, trial registrations, and peer-reviewed papers. Our "How to Read a Peptide Study" guide explains how to evaluate them.

References

  1. Jastreboff AM, et al. Tirzepatide Once Weekly for the Treatment of Obesity (SURMOUNT-1). N Engl J Med 2022. [source]
  2. ClinicalTrials.gov — registered tirzepatide studies. [source]
EM
Dr. Elena Marsh, PhDMolecular Pharmacology · Lead Editor

Written and maintained by the editorial team. Medically reviewed by Dr. James Okafor, MD (Internal Medicine).

Evidence tier: Approved medicine · Last reviewed: 2026-09-05 · Sources cited below.

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