For healthcare professionals
Zepbound for healthcare professionals
Clinical reference for Zepbound (tirzepatide) — mechanism of action, pharmacokinetics, indications, contraindications, key drug interactions, NDC codes, and FDA approval history.
This page is for clinical reference. Patient-friendly version →
Mechanism of action
Pharmacology class
Dual GIP/GLP-1 receptor agonist
Tirzepatide is a dual GIP and GLP-1 receptor agonist. Co-activation of both incretin receptors produces stronger insulinotropic, glucagonostatic, and central anorectic effects than selective GLP-1 agonism alone, yielding superior weight-loss outcomes vs semaglutide in SURMOUNT-5 head-to-head data.
Pharmacokinetics
- Half-life
- ~5 days
- T-max
- 8–72 hours
- Metabolism
- Proteolytic cleavage and amide-bond hydrolysis
- Excretion
- Urine and feces
- Bioavailability
- 80% (subcutaneous)
Contraindications
- Personal or family history of medullary thyroid carcinoma
- Multiple Endocrine Neoplasia syndrome type 2
- Serious hypersensitivity to tirzepatide
Key drug interactions
Not exhaustive. See the FDA label for the full interaction list.
| Interacting drug | Severity | Note |
|---|---|---|
| Insulin | major | Hypoglycemia risk; reduce insulin dose when initiating. |
| Sulfonylureas | major | Additive hypoglycemia risk. |
| Oral contraceptives | moderate | Reduced exposure during initiation and dose escalation — backup contraception × 4 weeks recommended. |
| Oral medications | moderate | Delayed gastric emptying may slow absorption. |
NDC codes & AWP
Representative NDC codes
- 0002-2393-80 (2.5 mg)
- 0002-2394-80 (5 mg)
- 0002-2473-80 (7.5 mg)
- 0002-2476-80 (10 mg)
- 0002-2477-80 (12.5 mg)
- 0002-2478-80 (15 mg)
AWP per month (US, 2026 estimate)
~$1,086 AWP (LillyDirect cash vial $299–$699)
FDA approval history
2023
Initial FDA approval for chronic weight management (adults with BMI ≥30, or ≥27 with comorbidity).
2024
Supplemental approval for moderate-to-severe obstructive sleep apnea in adults with obesity (SURMOUNT-OSA).
2025
LillyDirect cash-vial program launched for patients without insurance coverage.
References
Sourcing Zepbound for your patients
Compare US telehealth and pharmacy partners that dispense Zepbound — useful when a patient asks about cash-pay options outside of their insurance formulary.
Compare GLP-1 telehealth providers
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