Tirzepatide
Above: Tirzepatide molecular structure
Below: structure using peptide 3-letter code | |
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| Pronunciation | /tɜːrˈzɛpətaɪd/ tur-ZEP-ə-tyde |
| Trade names | Mounjaro, Zepbound |
| Other names | LY3298176, GIP/GLP-1 RA |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a622044 |
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| Routes of administration | Subcutaneous |
| Drug class | Antidiabetic, GLP-1 receptor agonist |
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| Bioavailability | 80% |
| Protein binding | Albumin |
| Metabolism | Proteolytic cleavage, β-oxidation of fatty diacid section and amide hydrolysis |
| Elimination half-life | 5 days |
| Excretion | Urine and faeces |
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| Formula | C225H348N48O68 |
| Molar mass | 4813.527 g·mol−1 |
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Tirzepatide[12] is an antidiabetic medication used to treat type 2 diabetes[9][13][14][15] and for weight loss.[10][16] Tirzepatide is administered via subcutaneous injections (under the skin).[9][13] In the United States, it is sold under the brand name Mounjaro for diabetes treatment[9] and Zepbound for weight loss and treatment of obstructive sleep apnea.[10][17]
Tirzepatide is a gastric inhibitory polypeptide (GIP) analog and a GLP-1 receptor agonist.[10] The most common side effects include nausea, vomiting, diarrhea, decreased appetite, constipation, upper abdominal discomfort, and abdominal pain.[9][13][18]
Developed by Eli Lilly and Company, tirzepatide was approved for treatment of diabetes in the US in May 2022,[9][13] in the European Union in September 2022,[11] in Canada in November 2022,[19] and in Australia in December 2022.[2] The US Food and Drug Administration (FDA) considers it a first-in-class medication.[20][21] The FDA approved it for weight loss in November 2023.[16][22] 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.[8][23] In December 2024, the FDA revised the indication for tirzepatide (as Zepbound) to include the treatment of moderate to severe obstructive sleep apnea.[10][17]
- ^ a b "Australian prescription medicine decision summaries: Mounjaro". Therapeutic Goods Administration. Archived from the original on 5 February 2023. Retrieved 28 February 2023.
- ^ a b "Mounjaro tirzepatide 15 mg/0.5 mL solution for injection pre-filled pen (379334)". Therapeutic Goods Administration. Archived from the original on 3 January 2023. Retrieved 28 February 2023.
- ^ "Public Summary: Mounjaro tirzepatide 15 mg/0.5 mL solution for injection pre-filled pen". Therapeutic Goods Administration. Archived from the original on 18 November 2023. Retrieved 28 February 2023.
- ^ "Mounjaro (Eli Lilly Australia Pty Ltd)". Therapeutic Goods Administration (TGA). 13 September 2024. Archived from the original on 15 September 2024. Retrieved 15 September 2024.
- ^ "Details for: Mounjaro". Health Canada. 24 November 2022. Archived from the original on 10 March 2024. Retrieved 3 March 2024.
- ^ "Notice: Multiple Additions to the Prescription Drug List (PDL) [2023-03-08]". Health Canada. 8 March 2023. Archived from the original on 22 March 2023. Retrieved 21 March 2023.
- ^ "Summary Basis of Decision - Mounjaro". Health Canada. 17 March 2023. Archived from the original on 25 April 2023. Retrieved 24 April 2023.
- ^ a b "Mounjaro KwikPen 2.5mg solution for injection in pre-filled pen". (emc). 8 January 2025. Retrieved 20 January 2025.
- ^ a b c d e f "Mounjaro- tirzepatide injection, solution". DailyMed. 13 May 2022. Archived from the original on 3 July 2022. Retrieved 27 May 2022.
- ^ a b c d e "Zepbound- tirzepatide injection, solution". DailyMed. 9 November 2023. Archived from the original on 20 November 2023. Retrieved 20 November 2023.
- ^ a b "Mounjaro EPAR". European Medicines Agency (EMA). 18 July 2022. Archived from the original on 12 December 2022. Retrieved 2 January 2023. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
- ^ World Health Organization (2019). "International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 81". WHO Drug Information. 33 (1). hdl:10665/330896.
- ^ a b c d "FDA Approves Novel, Dual-Targeted Treatment for Type 2 Diabetes". U.S. Food and Drug Administration (FDA) (Press release). 13 May 2022. Archived from the original on 13 May 2022. Retrieved 13 May 2022. This article incorporates text from this source, which is in the public domain.
- ^ Cite error: The named reference
moawas invoked but never defined (see the help page). - ^ Coskun T, Sloop KW, Loghin C, Alsina-Fernandez J, Urva S, Bokvist KB, et al. (December 2018). "LY3298176, a novel dual GIP and GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus: From discovery to clinical proof of concept". Molecular Metabolism. 18: 3–14. doi:10.1016/j.molmet.2018.09.009. PMC 6308032. PMID 30473097.
- ^ a b Cite error: The named reference
FDA Zepbound PR 20231108was invoked but never defined (see the help page). - ^ a b Cite error: The named reference
FDA PR 20241220was invoked but never defined (see the help page). - ^ Forzano I, Varzideh F, Avvisato R, Jankauskas SS, Mone P, Santulli G (November 2022). "Tirzepatide: A Systematic Update". Int J Mol Sci. 23 (23): 14631. doi:10.3390/ijms232314631. PMC 9741068. PMID 36498958.
- ^ "Drug and Health Product Submissions Under Review (SUR): New drug submissions completed". Health Canada. 10 March 2021. Archived from the original on 5 January 2023. Retrieved 5 January 2023.
- ^ "Advancing Health Through Innovation: New Drug Therapy Approvals 2022". U.S. Food and Drug Administration (FDA). 10 January 2023. Archived from the original on 21 January 2023. Retrieved 22 January 2023. This article incorporates text from this source, which is in the public domain.
- ^ New Drug Therapy Approvals 2022. U.S. Food and Drug Administration (FDA) (Report). January 2024. Archived from the original (PDF) on 14 January 2024. Retrieved 14 January 2024. This article incorporates text from this source, which is in the public domain.
- ^ Kolata G (8 November 2023). "F.D.A. Approves New Obesity Drug Tirzepatide That Will Compete With Wegovy". The New York Times. Archived from the original on 9 November 2023. Retrieved 9 November 2023.
- ^ "MHRA authorises diabetes drug Mounjaro (tirzepatide) for weight management and weight loss". GOV.UK (Press release). 8 November 2023. Archived from the original on 16 November 2023. Retrieved 17 November 2023.