GLP-1 explainers · Sponsored

What Is Tirzepatide? How the Dual GIP and GLP-1 Medication Works

5 min read · updated

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The brief

Tirzepatide is one of the most prescribed weight-management medications. Here is what it actually does.

Tirzepatide belongs to a class often called GLP-1 medications, but it is a little different from the others: it acts on two hormone receptors instead of one.

How it works

After you eat, the gut releases hormones called incretins, including GIP and GLP-1. They help regulate blood sugar and signal fullness. Tirzepatide activates the receptors for both.1 In practice that means slower stomach emptying, reduced appetite and better blood sugar control.

How it is taken

Tirzepatide is injected under the skin once a week. Treatment starts at a low dose that is increased step by step, mainly to limit stomach side effects.1

The evidence

Tirzepatide for weight management was studied in a large, 72-week randomized trial in adults with obesity, published in the New England Journal of Medicine, in which it was compared with placebo alongside diet and exercise.2 The FDA-approved labels describe the approved uses and the trial results in detail.1

Who it is for

FDA-approved tirzepatide for weight management is indicated for adults with obesity, or overweight with at least one weight-related condition, alongside diet and activity.1 A clinician weighs that against your history, including the boxed warning about thyroid cancer, pancreatitis and other risks.

Branded vs compounded

Tirzepatide is available as an FDA-approved branded medication and, through some telehealth providers, as a compounded medication prepared by a pharmacy for an individual patient. Compounded versions are not FDA-approved, and the FDA has published its concerns about unapproved GLP-1 drugs.3 See our explainer on compounded GLP-1s.

Bottom line. Tirzepatide activates two hormone receptors, GIP and GLP-1, involved in appetite and blood sugar.1
Important safety information. The FDA label for tirzepatide carries a boxed warning about thyroid C-cell tumors seen in rodents; it should not be used by anyone with a personal or family history of medullary thyroid carcinoma or Multiple Endocrine Neoplasia syndrome type 2.1 The most common side effects are nausea, diarrhea, vomiting and constipation.1 Serious risks include pancreatitis, gallbladder problems and low blood sugar when combined with insulin or sulfonylureas.1 Compounded versions are not FDA-approved.3 Only a licensed clinician should decide whether it is appropriate for you.

Quick questions

How does tirzepatide work?

It activates two gut hormone receptors, GIP and GLP-1, which slow stomach emptying, reduce appetite and help regulate blood sugar.

How often is tirzepatide taken?

Once a week, as an injection under the skin, starting at a low dose that is increased gradually.

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Sources

  1. Tirzepatide prescribing information. DailyMed, U.S. National Library of Medicine.
  2. Jastreboff AM, et al. Tirzepatide once weekly for the treatment of obesity. N Engl J Med. 2022. PubMed 35658024.
  3. U.S. Food and Drug Administration. FDA's Concerns with Unapproved GLP-1 Drugs Used for Weight Loss.