P Palthera
Hormone Analogues

Tirzepatide

LY3298176 / Mounjaro / Zepbound

Tirzepatide is a lipidated synthetic peptide that activates both the GIP and GLP-1 . It is FDA-approved as Mounjaro for type 2 diabetes mellitus and as Zepbound for chronic weight management in adults with obesity or overweight with at least one weight-related condition. The SURPASS (T2D) and SURMOUNT (obesity) Phase III trial programmes provide the primary efficacy and safety evidence base.

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Hormone Analogues
Classification
Dual GIP / GLP-1 receptor agonist · FDA-approved (Mounjaro / Zepbound)
Research stage
Phase III clinical evidence; FDA-approved for type 2 diabetes (Mounjaro) and chronic weight management (Zepbound)
Sequence
39-amino-acid lipidated peptide (C20 fatty diacid via γGlu-2xAEEA linker)
Molecular weight
4813.5 Da

Snapshot

Key takeaways

A three-bullet snapshot before reading the full dossier.

  1. 01

    Dual GIP/GLP-1 with extended via a C20 fatty diacid side chain.

  2. 02

    FDA-approved for two distinct indications across the Mounjaro and Zepbound brands.

  3. 03

    Phase III SURPASS and SURMOUNT programmes provide the primary clinical evidence.

Dossier overview

4

research areas

3

references

3

handling notes

01

Mechanism of action

Tirzepatide activates both glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) . The combined incretin activity is associated with improved glycaemic control and substantial weight reduction in clinical trials.

02

Research applications

  • Type 2 diabetes glycaemic-control clinical research
  • Obesity and weight-management clinical research
  • Incretin pharmacology
  • Cardiometabolic outcome research

Evidence at a glance

What's behind this profile

3 citations · 2021–2023

Human
3

Studies in human volunteers or patients (incl. early-phase trials).

Publication years

  1. 21
  2. 22
  3. 23
20212023

Counts are derived from the cited studies below. A study covering both in vivo and in vitro work is counted by its primary model. Sample size is reported in 3 of 3 citations. Findings remain model-specific and are not extrapolated to therapeutic use.

03

Study references

Each profile cites a minimum of two peer-reviewed sources, with model type and reported sample size where the source provides it. Findings are model-specific and must not be extrapolated to therapeutic use.

Efficacy and safety of a novel dual GIP and GLP-1 receptor agonist tirzepatide in patients with type 2 diabetes (SURPASS-1)

2021

Rosenstock J et al. · The Lancet

Model
Phase 3 double-blind randomised placebo-controlled trial in adults with type 2 diabetes
Sample
n=478

Tirzepatide monotherapy was associated with superior glycaemic control and weight reduction versus placebo, with a safety profile broadly consistent with GLP-1 .

PMID 34186022 DOI 10.1016/S0140-6736(21)01324-6

Tirzepatide Once Weekly for the Treatment of Obesity (SURMOUNT-1)

2022

Jastreboff AM et al. · New England Journal of Medicine

Model
Phase 3 double-blind randomised placebo-controlled trial in adults with obesity (without type 2 diabetes)
Sample
n=2539

Over 72 weeks, tirzepatide was associated with mean body weight reductions of approximately 15–21% across doses versus 3% with placebo; gastrointestinal adverse events were the most common.

PMID 35658024 DOI 10.1056/NEJMoa2206038

Tirzepatide once weekly for the treatment of obesity in people with type 2 diabetes (SURMOUNT-2)

2023

Garvey WT et al. · The Lancet

Model
Phase 3 double-blind randomised placebo-controlled trial in adults with obesity and type 2 diabetes
Sample
n=938

Tirzepatide 10–15 mg weekly was associated with mean body weight reductions of 12.8–14.7% over 72 weeks versus 3.2% with placebo, with a safety profile similar to other incretin agents.

PMID 37385275 DOI 10.1016/S0140-6736(23)01200-X

Evidence caveats

  • FDA approval covers specific indications (T2D, chronic weight management with eligibility criteria). Clinical use is a medical decision with a qualified healthcare professional.
  • Long-term cardiovascular and oncologic outcome trials are ongoing; this profile summarises the primary registrational evidence as published.

04

Storage and handling

Approved product follows manufacturer cold-chain instructions. Research-grade material must be stored under controlled laboratory conditions per protocol.

  • Approved product follows the manufacturer label and pharmacy cold-chain.
  • Research-grade material requires controlled laboratory storage and full batch documentation.
  • Clinical use of approved product is exclusively a medical decision made with a healthcare professional.

Common questions

Tirzepatide FAQ

Plain-English answers backed by the citations on this profile — what it is, what's been studied, regulatory status, evidence limits.

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