Quick answer
A dual GIP/GLP-1 receptor agonist marketed by Eli Lilly as Mounjaro (T2D) and Zepbound (weight management, OSA). The first dual incretin agonist approved in the US.
Full definition
Tirzepatide is a 39-amino-acid synthetic peptide that activates both the GIP and GLP-1 receptors, providing dual incretin agonism. It has a half-life of about 5 days and is dosed once weekly subcutaneously at 2.5, 5, 7.5, 10, 12.5, or 15 mg. Marketed as Mounjaro for type 2 diabetes (FDA approval May 2022) and Zepbound for chronic weight management (Nov 2023) and moderate-to-severe obstructive sleep apnea in adults with obesity (Dec 2024). In SURPASS-2 it outperformed semaglutide on HbA1c and weight loss.
Deep dive
Tirzepatide: complete reference
Tirzepatide is a synthetic dual GIP/GLP-1 receptor agonist developed by Eli Lilly, distinguished from earlier GLP-1 monotherapies by its simultaneous activation of two incretin receptors. Structurally, tirzepatide is a 39-amino-acid linear peptide based on the GIP sequence with modifications (including a C20 fatty diacid chain via gamma-glutamic-acid linker) that enable albumin binding and a circulating half-life of approximately 5 days — supporting once-weekly subcutaneous dosing. The dual mechanism is believed to drive its superior weight-loss outcomes vs single-receptor GLP-1 agonists, though the precise contribution of GIP receptor activation is still being characterized. FDA approval came in 2022 (Mounjaro for type 2 diabetes), with Zepbound following in 2023 for chronic weight management and 2024 for moderate-to-severe obstructive sleep apnea. Pivotal trials (SURPASS for diabetes, SURMOUNT for weight, SURMOUNT-OSA for sleep apnea) have produced the highest weight-loss outcomes seen in any FDA-approved anti-obesity medication: 22.5% average body weight reduction at 72 weeks (SURMOUNT-1, 15mg dose). Cardiovascular outcomes are being studied in the ongoing SURPASS-CVOT trial.
- In practice
- Tirzepatide is the same molecule whether sold as Mounjaro (diabetes label) or Zepbound (weight + OSA label). Same Eli Lilly factory, same doses (2.5-15mg weekly), same side effects — only the FDA indication and brand name differ.
- Clinical context
- Tirzepatide is the only FDA-approved dual GIP/GLP-1 agonist as of 2026. Clinicians often choose tirzepatide over semaglutide when maximum weight loss is the priority and the patient tolerates it.
Medications
Tirzepatide is most directly relevant to the following GLP-1 medications:
Related terms
- Semaglutide — A long-acting GLP-1 receptor agonist marketed by Novo Nordisk as Ozempic (T2D), Wegovy (weight manag…
- GIP (Glucose-Dependent Insulinotropic Polypeptide) — GIP is a gut hormone (incretin) released after eating that, with GLP-1, accounts for the bulk of pos…
- Dual Agonist — A drug that activates two different receptors simultaneously. Tirzepatide is a dual GIP/GLP-1 recept…
- GLP-1 Receptor Agonist (GLP-1 RA) — A class of injectable or oral drugs that activate the GLP-1 receptor to control blood sugar, slow di…
- Compounded Tirzepatide — A non-FDA-approved version of tirzepatide prepared by a compounding pharmacy. The FDA shortage was r…
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GLP1Zoom glossary is educational reference. Definitions are summary interpretations of clinical sources and not a substitute for prescribing-information detail. Full disclaimer.
References
Glucagon-Like Peptide-1 Receptor Agonists: Mechanisms и Clinical Use (Drucker, Cell Metabolism)(2018)
Tirzepatide GIP/GLP-1 Dual Agonism: Mechanism Review (Lancet Diabetes & Endocrinology)(2021)
GLP-1 Effects on Gastric Emptying: Pharmacology Review (American J Physiology)(2020)
Endocrine Society Clinical Practice Guideline: Pharmacological Management of Obesity(2015)
STEP-1 trial: Once-Weekly Semaglutide in Adults with Overweight or Obesity (Wilding et al., NEJM)(2021)
SURMOUNT-1 trial: Tirzepatide Once Weekly для Treatment of Obesity (Jastreboff et al., NEJM)(2022)
SUSTAIN-6 trial: Semaglutide and Cardiovascular Outcomes (Marso et al., NEJM)(2016)
SURPASS-2 trial: Tirzepatide vs Semaglutide в Type 2 Diabetes (Frias et al., NEJM)(2021)
LEADER trial: Liraglutide and Cardiovascular Outcomes в T2D (Marso et al., NEJM)(2016)