Digestive & weight Dual GIP + GLP-1 receptor agonist
Tirzepatide
Regulatory status
Status at a glance
503A compounding status
Not nominated
We found no pending nomination for the 503A bulks list. Unless the substance has another legal pathway (for example, a USP monograph or use in an FDA-approved drug), 503A pharmacies generally may not compound with it.
- FDA approval
- An FDA-approved product contains this peptide
- 503B outsourcing
- Not determined
- Anti-doping (WADA)
- Not on the WADA Prohibited List
- DEA schedule
- Not a controlled substance
About peptide status
Most peptides discussed here are not FDA-approved for any use, and products labeled “research use only” are not for human use. Removal from Category 2 does not authorize compounding. PCAC votes are non-binding recommendations; FDA and HHS make the final decisions.
This is not medical or legal advice, and we do not publish dosing, sourcing or reconstitution information. Talk with a licensed clinician before using any peptide.
If you think you are having a medical emergency, call 911.
Key takeaway
Tirzepatide is a once-weekly peptide that activates two gut-hormone receptors, GIP and GLP-1, made by Eli Lilly and sold as Mounjaro and Zepbound. It is FDA-approved for type 2 diabetes in adults and children 10 and older, cardiovascular risk reduction in adults with type 2 diabetes, weight management, and obstructive sleep apnea. In the SURMOUNT-1 trial it produced up to 20.9% average body-weight loss, among the largest results for an obesity medicine.
At a glance
- FDA status
- FDA-approved peptide, sold as Mounjaro for type 2 diabetes and cardiovascular risk reduction and as Zepbound for weight management and obstructive sleep apnea
- How it works
- Dual agonist that activates both the GIP and GLP-1 receptors, given as a once-weekly injection
- Research
- In trials, up to 20.9% average body-weight loss, among the largest results seen for an obesity medication
- Evidence strength
- FDA approved
Summary
Tirzepatide is an FDA-approved once-weekly peptide that activates GIP and GLP-1 receptors. Learn its approved uses, how it works, and trial results.
What is tirzepatide?
Tirzepatide is a synthetic peptide made of 39 amino acids that acts as a dual GIP and GLP-1 receptor agonist. GIP and GLP-1 are two hormones the gut releases after eating, and tirzepatide is engineered to activate both of their receptors at once, which is what distinguishes it from the single-hormone GLP-1 drugs.
It is made by Eli Lilly and sold under two brand names. Mounjaro is used for type 2 diabetes, and Zepbound is used for weight management and for obstructive sleep apnea. Both are given as a once-weekly subcutaneous injection.
How does it work?
Tirzepatide activates the GIP and GLP-1 receptors, mimicking two natural gut hormones at the same time. Through those receptors it prompts the pancreas to release insulin when blood sugar is high, reduces the release of glucagon (a hormone that raises blood sugar), slows the rate at which the stomach empties, and acts on appetite centers to reduce hunger and food intake. Together these effects lower blood sugar and reduce how much a person eats.
The trial results are large. In the SURMOUNT-1 obesity trial, adults without diabetes lost an average of between 15.0% and 20.9% of their body weight across the three doses over 72 weeks, compared with 3.1% for placebo. In its type 2 diabetes program, tirzepatide produced large reductions in blood sugar (A1c) along with weight loss.
Is tirzepatide FDA-approved?
Editor’s note
Status: FDA-approved peptide, sold as Mounjaro for type 2 diabetes and cardiovascular risk reduction and as Zepbound for weight management and obstructive sleep apnea
Category: FDA-approved · Primary body area: Digestive & weight
Yes, across five uses, approved in this order:
| Date | Brand | Approval |
|---|---|---|
| 2022 | Mounjaro | First approved for type 2 diabetes |
| 2023 | Zepbound | Approved for chronic weight management |
| December 2024 | Zepbound | The first medication approved for obstructive sleep apnea in adults with obesity |
| December 2025 | Mounjaro | Extended to children 10 and older |
| August 2026 | Mounjaro | Reducing major cardiovascular events in adults with type 2 diabetes at high risk |
What is tirzepatide prescribed for?
For type 2 diabetes, Mounjaro is prescribed to improve blood sugar control alongside diet and exercise in adults and children 10 and older, and to reduce the risk of major cardiovascular events in adults with type 2 diabetes at high risk. For weight management, Zepbound is approved for adults with obesity (a BMI of 30 or higher) or overweight (a BMI of 27 or higher) plus a weight-related condition such as high blood pressure or high cholesterol. Zepbound is also approved for moderate-to-severe obstructive sleep apnea in adults with obesity.
It should not be used by people with a personal or family history of medullary thyroid carcinoma or Multiple Endocrine Neoplasia syndrome type 2, or by anyone with a known allergy to tirzepatide.
What are the side effects?
The most common side effects are gastrointestinal, and they are usually strongest when the dose is increased:
- Nausea
- Diarrhea
- Vomiting
- Constipation
- Abdominal pain
- Decreased appetite
- Indigestion
- Fatigue
- Injection-site reactions
- Allergic reactions
- Belching
- Hair loss
- Heartburn
Less common but more serious risks include:
- Thyroid C-cell tumors: tirzepatide carries a boxed warning based on rodent studies. It is not known whether this happens in humans.
- Pancreatitis, or inflammation of the pancreas
- Gallbladder problems, including gallstones
- Acute kidney injury, usually from dehydration caused by vomiting or diarrhea
- Worsening of diabetic retinopathy in people with type 2 diabetes
- Low blood sugar, especially when combined with insulin or a sulfonylurea
- Delayed stomach emptying, which can raise the risk of aspiration during surgery or anesthesia
Sources: FDA prescribing information for Mounjaro and Zepbound (tirzepatide); the SURMOUNT-1 obesity trial in the New England Journal of Medicine (Jastreboff et al., 2022, DOI: 10.1056/NEJMoa2206038), indexed on PubMed; and the FDA approval announcement for obstructive sleep apnea. This document is educational and does not constitute medical advice.
Registered human trials
0 registered human trials on ClinicalTrials.gov that we reviewed
Sources
- [1]
receptor agonist (PDF)
- [2]
- [3]
Approved (PDF)
- [4]
- [5]
- [6]
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- [8]
- [9]
- [10]
- [11]
- [12]
- [13]
- [14]
- [15]
- [16]
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