What is Tirzepatide?
Tirzepatide is a medication used to treat type 2 diabetes and for weight loss. It is administered via subcutaneous injections (under the skin). Tirzepatide is sold under the brand name Mounjaro for diabetes treatment and Zepbound for weight loss and treatment of obstructive sleep apnea.
Mechanism of Action
Tirzepatide works by activating both GIP (glucose-dependent insulinotropic polypeptide) and GLP-1 (glucagon-like peptide-1) hormone receptors. This dual agonist behavior has been shown to produce greater reductions of hyperglycemia compared to a selective GLP-1 receptor agonist. Tirzepatide has a greater affinity to GIP receptors than to GLP-1 receptors.
Medical Uses
Tirzepatide (as Mounjaro) is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes. Tirzepatide (as Zepbound) is indicated, alongside a reduced-calorie diet and increased physical activity, for long-term weight reduction in adults with obesity or overweight with at least one weight-related comorbidity. Zepbound is also approved for the treatment of moderate-to-severe obstructive sleep apnea in adults with obesity.
Contraindications
Tirzepatide is contraindicated for use in people with a personal or family history of medullary thyroid cancer and people with multiple endocrine neoplasia syndrome type 2.
Side Effects
The most common side effects of tirzepatide include nausea, vomiting, diarrhea, decreased appetite, constipation, upper abdominal discomfort, and abdominal pain. Serious side effects include severe stomach problems, acute kidney damage, gallbladder disease, inflamed pancreas (acute pancreatitis), serious allergic reactions, low blood sugar levels (hypoglycemia), diabetic retinopathy issues in type 2 diabetics, suicidal behavior or thoughts, and food or liquid getting into the lungs during anesthesia or deep sedation.
Clinical Trials
Tirzepatide has been shown to be effective in reducing HbA1c and body weight in people with type 2 diabetes. In a phase III trial, tirzepatide demonstrated clinically significant benefits among participants with obesity and heart failure with preserved ejection fraction.
Approval and Availability
Tirzepatide was approved for treatment of diabetes in the US in May 2022, in the European Union in September 2022, in Canada in November 2022, and in Australia in December 2022. The FDA approved it for weight loss in November 2023 . In December 2024, the FDA approved tirzepatide (Zepbound) as the first medication to be used in the treatment of moderate to severe obstructive sleep apnea .
Tirzepatide is a dual GIP and GLP-1 receptor agonist used to treat type 2 diabetes and for weight loss, with brand names Mounjaro and Zepbound, respectively.
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