All-In Breakdown

Tirzepatide

Technology

A dual GLP-1/GIP receptor agonist developed by Eli Lilly, marketed as Mounjaro. In Q2, it became the bestselling drug in the world, surpassing Keytruda, with $8.1 billion in revenue for the quarter.

First Mentioned

9/29/2025, 5:01:45 AM

Last Updated

9/29/2025, 5:07:15 AM

Research Retrieved

9/29/2025, 5:07:15 AM

Summary

Tirzepatide is a groundbreaking dual-acting medication developed by Eli Lilly and Company, functioning as both a gastric inhibitory polypeptide (GIP) analog and a GLP-1 receptor agonist. Administered via subcutaneous injections, it is marketed in the United States as Mounjaro for type 2 diabetes and Zepbound for weight loss and obstructive sleep apnea. The medication received its initial US FDA approval for diabetes in May 2022, followed by approvals in the EU, Canada, and Australia later that year. Subsequent FDA approvals in November 2023 for weight loss and December 2024 for obstructive sleep apnea have expanded its indications. Tirzepatide has achieved significant commercial success, becoming the world's top-selling drug in Q2 and ranking as the 110th most commonly prescribed medication in the U.S. in 2023. While addressing challenges like counterfeit products and patent issues, Eli Lilly is heavily investing in supply chain expansion and exploring new applications for Tirzepatide in addictions and mental health, alongside developing an oral GLP-1 version.

Referenced in 1 Document
Research Data
Extracted Attributes
  • Developer

    Eli Lilly and Company

  • Chemical Class

    Synthetic polypeptide

  • Amino Acid Count

    39

  • Q2 Sales Ranking

    World's top-selling drug (surpassing Keytruda)

  • FDA Classification

    First-in-class medication

  • Common Side Effects

    Nausea, vomiting, diarrhea, decreased appetite, constipation, upper abdominal discomfort, abdominal pain

  • Mechanism of Action

    Dual agonist for gastric inhibitory polypeptide (GIP) and GLP-1 receptors

  • Ongoing Development

    Oral GLP-1 pill

  • Administration Route

    Subcutaneous injections

  • 2023 US Prescriptions

    Over six million

  • Chemical Modification

    Lipidation (to improve uptake and stability)

  • 2023 US Prescription Ranking

    110th most commonly prescribed

  • Potential Future Applications

    Addictions, mental health conditions

  • US Brand Name (Type 2 Diabetes)

    Mounjaro

  • Early Weight-Loss Study Location

    Singapore

  • US Brand Name (Weight Loss, Obstructive Sleep Apnea)

    Zepbound

Timeline
  • Completed Phase III trials globally. (Source: web_search_results)

    2021

  • Approved by US FDA for treatment of type 2 diabetes (marketed as Mounjaro). (Source: summary, wikipedia, web_search_results)

    2022-05

  • Approved in the European Union for diabetes treatment. (Source: summary, wikipedia)

    2022-09

  • Approved in Canada for diabetes treatment. (Source: summary, wikipedia)

    2022-11

  • Approved in Australia for diabetes treatment. (Source: summary, wikipedia)

    2022-12

  • Became the world's top-selling drug in Q2, surpassing Keytruda. (Source: summary, related_documents)

    2023

  • Was the 110th most commonly prescribed medication in the U.S., with over six million prescriptions. (Source: summary, wikipedia)

    2023

  • Approved by US FDA for weight loss (marketed as Zepbound). (Source: summary, wikipedia)

    2023-11

  • UK Medicines and Healthcare products Regulatory Agency (MHRA) revised its indication for weight management (as Mounjaro). (Source: summary, wikipedia)

    2023-11

  • US FDA revised its indication to include the treatment of moderate to severe obstructive sleep apnea (as Zepbound). (Source: summary, wikipedia)

    2024-12

Wikipedia
View on Wikipedia
Tirzepatide

Tirzepatide is an antidiabetic medication used to treat type 2 diabetes and for weight loss. Tirzepatide is administered via subcutaneous injections (under the skin). In the United States, it is sold under the brand name Mounjaro for diabetes treatment and Zepbound for weight loss and treatment of obstructive sleep apnea. Tirzepatide is a gastric inhibitory polypeptide (GIP) analog and a GLP-1 receptor agonist. The most common side effects include nausea, vomiting, diarrhea, decreased appetite, constipation, upper abdominal discomfort, and abdominal pain. Developed by Eli Lilly and Company, 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 US Food and Drug Administration (FDA) considers it a first-in-class medication. The FDA approved it for weight loss in November 2023. Also in November 2023, the UK Medicines and Healthcare products Regulatory Agency revised the indication for tirzepatide (as Mounjaro) to include the treatment for weight management and weight loss. In December 2024, the FDA revised the indication for tirzepatide (as Zepbound) to include the treatment of moderate to severe obstructive sleep apnea. In 2023, tirzepatide was the 110th-most commonly prescribed medication in the U.S., with more than six million prescriptions.

Web Search Results
  • Tirzepatide - StatPearls - NCBI Bookshelf

    Tirzepatide is a novel medication approved by the US Food and Drug Administration (FDA) in May 2022 for treating type 2 diabetes mellitus (T2DM).Tirzepatide is a synthetic polypeptide and dual agonist for the glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) receptors.Therefore, the drug leads to significantly improved glycemic control and weight reduction in patients with T2DM, maximizing benefits similar to GLP-1 medications such as semaglutide.( [...] Tirzepatide is a novel medication approved by the US Food and Drug Administration (FDA) for treating type 2 diabetes mellitus (T2DM). This medication also demonstrates efficacy in weight loss, leading to its off-label use for obesity treatment.Tirzepatide is a dual agonist for the glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) receptors. The drug leads to significantly improved glycemic control and weight reduction in patients with T2DM, maximizing [...] Tirzepatide is a synthetic polypeptide dual agonist for GLP-1 and GIP. Tirzepatide, "twincretin," exhibits distinct characteristics from GLP-1 receptor agonists.( medication comprises 39 amino acids and is an analog of the gastric inhibitory polypeptide. Functionally,tirzepatide stimulates insulin release from the pancreas and reduces hyperglycemia. In addition, tirzepatide also increases the levels of adiponectin.

  • Tirzepatide - Wikipedia

    Tirzepatide is an antidiabetic medication used to treat type 2 diabetes and for weight loss. Tirzepatide is administered via subcutaneous injections (under the skin). In the United States, it is sold under the brand name Mounjaro for diabetes treatment and Zepbound for weight loss and treatment of obstructive sleep apnea. [...] Tirzepatide is a gastric inhibitory polypeptide (GIP) analog and a GLP-1 receptor agonist. The most common side effects include nausea, vomiting, diarrhea, decreased appetite, constipation, upper abdominal discomfort, and abdominal pain. [...] Tirzepatide is an analogue of gastric inhibitory polypeptide (GIP), a human hormone that stimulates the release of insulin from the pancreas. Tirzepatide is a linear polypeptide of 39 amino acids that has been chemically modified by lipidation to improve its uptake into cells and its stability to metabolism. It completed phase III trials globally in 2021. ### Mechanism of action [edit]

  • Tirzepatide Once Weekly for the Treatment of Obesity

    Tirzepatide is a once-weekly subcutaneous injectable peptide (approved by the Food and Drug Administration [FDA] for type 2 diabetes) engineered from the native GIP sequence, with agonist activity at both the GIP and GLP-1 receptors.12 Preclinical data demonstrated that the affinity of tirzepatide for GIP receptors was equal to the affinity of native GIP for GIP receptors, whereas tirzepatide bound GLP-1 receptors with affinity approximately five times weaker than native GLP-1 bound GLP-1

  • Tirzepatide injection: MedlinePlus Drug Information

    Tirzepatide injection (Zepbound®) is used along with an individualized low-calorie, low-fat diet and exercise program to help with weight loss in obese adults or overweight adults who may also have high blood pressure, diabetes, sleep apnea, cardiovascular disease or high cholesterol. Tirzepatide is in a class of medications called glucose-dependent insulinotropic polypeptide (GIP) receptor and glucagon-like peptide-1 (GLP-1) receptor agonists. It works by increasing insulin available and [...] Tirzepatide injection (Mounjaro®) is used along with diet and exercise to lower blood sugar levels in people with type 2 diabetes (condition in which blood sugar is too high because the body does not produce or use insulin normally). Tirzepatide is not used to treat type 1 diabetes (condition in which the body does not produce insulin and therefore cannot control the amount of sugar in the blood) or diabetic ketoacidosis (a serious condition that may develop if high blood sugar is not treated). [...] Tirzepatide comes as a solution (liquid) in a pre-filled pen or vial to be injected subcutaneously (under the skin). It is usually given once a week with or without meals at any time of day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Use tirzepatide exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

  • Tirzepatide (subcutaneous route) - Side effects & dosage - Mayo Clinic

    Skip to content # Tirzepatide (subcutaneous route) ## On this page Brand names Description Before using Proper use Precautions Side effects ## Brand Name ### US Brand Name Mounjaro Zepbound Back to top ## Description Tirzepatide injection is used to treat type 2 diabetes. It is used together with diet and exercise to help control your blood sugar. Tirzepatide is a glucose-dependent insulinotropic polypeptide (GIP) receptor and glucagon-like peptide-1 (GLP-1) receptor agonist.