No. 022 · Metabolic · Weight Loss Peptide
Tirzepatide
Also known as: LY3298176MounjaroZepbound
- FDA approved 2022
- WADA — not listed
2D structure from PubChem CID 166567236 (CID 166567236), matched by molecular formula. Hydrogens on carbon are implied.
- Nonpolar 21
- Polar 11
- Positive charge 2
- Negative charge 3
- Modified / non-standard 2
Each dot is a residue placed around the ring from N- to C-terminus; its distance from the centre reflects its chemistry.
Quick answers
- What is Tirzepatide?
- A dual GIP/GLP-1 receptor agonist FDA-approved for type 2 diabetes (Mounjaro) and obesity (Zepbound).
- How strong is the evidence for Tirzepatide?
- Tier S (approved) on the peptidemeta evidence scale. Phase 3 RCT programmes (SURPASS, SURMOUNT); FDA-approved in 2022 for type 2 diabetes (Mounjaro) and in 2023 for weight management (Zepbound).
- Is Tirzepatide FDA-approved?
- Yes. The FDA approved Tirzepatide (Mounjaro, Zepbound) in 2022. Approved for type 2 diabetes (Mounjaro, 2022) and chronic weight management (Zepbound, 2023).
- Is Tirzepatide banned in sport?
- No. Tirzepatide is not on the World Anti-Doping Agency Prohibited List.
- How does Tirzepatide work?
- Tirzepatide is a dual GIP/GLP-1 receptor agonist built on a 39-amino-acid peptide backbone with a C20 fatty diacid moiety enabling albumin binding and once-weekly dosing. It enhances glucose-dependent insulin secretion, suppresses glucagon, slows gastric emptying, and acts on hypothalamic appetite centers to reduce food intake.
- What is known about the safety of Tirzepatide?
- FDA-approved with extensive Phase III safety data (SURPASS and SURMOUNT programs). Most common side effects are GI-related: nausea, diarrhea, decreased appetite, vomiting, constipation.
Last reviewed · editorial policy · markdown
Evidence
- D In vitro
- C Animal
- B Human pilot
- A RCT
- S Approved
TIER S — Approved by the FDA or EMA for at least one indication.
Phase 3 RCT programmes (SURPASS, SURMOUNT); FDA-approved in 2022 for type 2 diabetes (Mounjaro) and in 2023 for weight management (Zepbound).
Tiers rate the strength of published evidence — not effectiveness, safety, or a recommendation.
At a glance
- Residues
- 39 amino acids, N→C
- Molecular weight
- 4,813.5 Da
- Formula
- C225H348N48O68
- Discovered
- 2018 Discovery and first clinical data published by Eli Lilly as LY3298176 (Coskun et al., Mol Metab 2018).
- Routes studied
- Subcutaneous Routes used in published research
- FDA
- Approved (2022) Mounjaro, Zepbound Approved for type 2 diabetes (Mounjaro, 2022) and chronic weight management (Zepbound, 2023).
- WADA
- Not on the Prohibited List
Sequence
Note K20 carries a C-20 fatty diacid attached via a γ-Glu–2×AEEA linker.
Overview
A dual GIP/GLP-1 receptor agonist FDA-approved for type 2 diabetes (Mounjaro) and obesity (Zepbound). It delivers substantial weight loss and glycemic improvements in large-scale trials.
Research status FDA-approved as Mounjaro (T2D) and Zepbound (obesity); extensive Phase III trial data
Mechanism
Tirzepatide is a dual GIP/GLP-1 receptor agonist built on a 39-amino-acid peptide backbone with a C20 fatty diacid moiety enabling albumin binding and once-weekly dosing. It enhances glucose-dependent insulin secretion, suppresses glucagon, slows gastric emptying, and acts on hypothalamic appetite centers to reduce food intake.
Effects reported in research
Reported outcomes, not promises. Some come from controlled human trials; others may be from smaller or preclinical studies — check the studies below.
- Substantial sustained weight loss
- Improved insulin sensitivity
- Reduced HbA1c levels
- Decreased cardiovascular risk markers
Safety & unknowns
FDA-approved with extensive Phase III safety data (SURPASS and SURMOUNT programs). Most common side effects are GI-related: nausea, diarrhea, decreased appetite, vomiting, constipation. Boxed warning for thyroid C-cell tumors (preclinical rodent signal). Contraindicated in personal/family history of medullary thyroid carcinoma or MEN 2.
Unknowns. Trial safety data apply to the populations, formulations and conditions studied.
Informational only — not medical advice. peptidemeta publishes no dosing, protocols, or sourcing. Talk to a qualified clinician about any treatment decision.
Studies [3]
- Clinical trial 2022
Tirzepatide Once Weekly for the Treatment of Obesity
In the 72-week phase 3 SURMOUNT-1 RCT in 2539 adults with obesity, mean weight change was -15.0%, -19.5%, and -20.9% with 5, 10, and 15 mg versus -3.1% with placebo.
- Clinical trial 2021
Tirzepatide versus Semaglutide Once Weekly in Patients with Type 2 Diabetes
In the 40-week SURPASS-2 RCT, all three tirzepatide doses lowered HbA1c more than semaglutide 1 mg (differences -0.15 to -0.45 percentage points).
- Clinical trial 2021
Efficacy and safety of a novel dual GIP and GLP-1 receptor agonist tirzepatide in patients with type 2 diabetes (SURPASS-1): a double-blind, randomised, phase 3 trial
In the 40-week SURPASS-1 RCT in 478 adults with type 2 diabetes, tirzepatide monotherapy at all doses was superior to placebo for change in HbA1c.
Status sources
Sources behind the tier, regulatory status, sequence and dates on this page.
- Drugs@FDA — Mounjaro (NDA 215866) accessdata.fda.gov
- Drugs@FDA — Zepbound (NDA 217806) accessdata.fda.gov
- KEGG DRUG D11360 — tirzepatide (sequence, formula, MW) kegg.jp
- Jastreboff et al., NEJM 2022 (SURMOUNT-1 RCT) pubmed.ncbi.nlm.nih.gov
- Coskun et al., Mol Metab 2018 (discovery) pubmed.ncbi.nlm.nih.gov
Cite this entry
peptidemeta. (2026). Tirzepatide. In peptidemeta: The peptide library, ranked by evidence. Retrieved November 8, 2026, from https://peptidemeta.com/p/tirzepatide/
@misc{peptidemeta-tirzepatide,
title = {Tirzepatide},
author = {{peptidemeta}},
year = {2026},
howpublished = {\url{https://peptidemeta.com/p/tirzepatide/}},
note = {Accessed 2026-11-08}
} Accessed date reflects when you opened this page. Cite primary studies for scientific claims.