Tirzepatide

What it is and how it works

Mechanism of Action Tirzepatide is a GIP receptor and GLP-1 receptor agonist. It contains a C20 fatty diacid that enables albumin binding and prolongs the half-life. Tirzepatide selectively binds to and activates both the GIP and GLP-1 receptors, the targets for native GIP and GLP-1. GLP-1 is a physiological regulator of appetite and caloric intake. Nonclinical studies suggest the addition of GIP may further contribute to the regulation of food intake. Both GIP receptors and GLP-1 receptors are found in areas of the brain involved in appetite regulation.

Mechanism class: G-Protein-linked Receptor Interactions · Glucagon-like Peptide-1 (GLP-1) Agonists

Indications

® is indicated in combination with a reduced-calorie diet and increased physical activity: to reduce excess body weight and maintain weight reduction long term in adults with obesity or adults with overweight in the presence of at least one weight-related comorbid condition. to treat moderate to severe obstructive sleep apnea (OSA) in adults with obesity. ZEPBOUND is a glucose-dependent insulinotropic polypeptide (GIP) receptor and glucagon-like peptide-1 (GLP-1) receptor agonist indicated in combination with a reduced-calorie diet and increased physical activity: to reduce excess body weight and maintain weight reduction long term in adults with obesity or adults with overweight in the presence of at least one weight-related comorbid condition. to treat moderate to severe obstructive sleep apnea (OSA) in adults with obesity. Limitations of Use: Coadministration with other tirzepatide-containing products or with any GLP-1 receptor agonist is not recommended. Limitations of Use ZEPBOUND contains tirzepatide.

Dosage and administration (summary)

Recommended Dose Escalation Schedule The recommended starting dosage is 2.5 mg injected subcutaneously once weekly for 4 weeks. Increase the dosage in 2.5 mg increments after at least 4 weeks until recommended maintenance dosage is achieved. Consider treatment response and tolerability when selecting the maintenance dosage. Recommended Maintenance and Maximum Dosage Weight Reduction and Long-Term Maintenance: 5 mg, 10 mg, or 15 mg injected subcutaneously once weekly. Obstructive Sleep Apnea: 10 mg or 15 mg injected subcutaneously once weekly. Maximum Recommended Dosage: 15 mg injected subcutaneously once weekly.

Contraindications

is contraindicated in patients with: A personal or family history of MTC or in patients with MEN 2 . Known serious hypersensitivity to tirzepatide or any of the excipients in ZEPBOUND. Serious hypersensitivity reactions, including anaphylaxis and angioedema, have been reported with tirzepatide .

Warnings and precautions

Severe Gastrointestinal Adverse Reactions: Use has been associated with gastrointestinal adverse reactions, sometimes severe. ZEPBOUND is not recommended in patients with severe gastroparesis. Acute Kidney Injury Due to Volume Depletion: Monitor renal function in patients reporting adverse reactions that could lead to volume depletion. Acute Gallbladder Disease: Has been reported in clinical trials. If cholecystitis is suspected, gallbladder studies and clinical follow-up are indicated. Acute Pancreatitis: Has been observed in patients treated with GLP-1 receptor agonists, or ZEPBOUND.

Pregnancy

Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to ZEPBOUND (tirzepatide) during pregnancy. Pregnant patients exposed to ZEPBOUND and healthcare providers are encouraged to register by calling 1-844-524-0039 or emailing at MILEregistry@thermofisher.com.

Storage and supply

Storage and Handling Do not freeze ZEPBOUND. Do not use ZEPBOUND if frozen. Protect ZEPBOUND from heat and light. Store ZEPBOUND in the original carton to protect from light. ZEPBOUND Single-dose Pen and Single-dose Vial Store ZEPBOUND single-dose pen and single-dose vial in a refrigerator at 2°C to 8°C (36°F to 46°F).

Source: Tirzepatide (Zepbound) — US FDA prescribing information, 2026-08-28, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.