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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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Chemical and physical data | |
Formula | C225H348N48O68 |
Molar mass | 4813.527 g·mol−1 |
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Tirzepatide, sold under the brand names Mounjaro and Zepbound, is an antidiabetic medication used for the treatment of type 2 diabetes[10][13][14][15] and for weight loss.[11][16] Tirzepatide is administered via subcutaneous injections (under the skin).[10][13]
The most common side effects include nausea, vomiting, diarrhea, decreased appetite, constipation, upper abdominal discomfort, and abdominal pain.[10][13][17]
Glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) are hormones involved in blood-sugar control.[13] After a person has eaten, these hormones are secreted by cells of the intestines, and in turn cause the secretion of insulin. Tirzepatide is a long-acting GIP-analogue that activates both the GLP-1 and GIP receptors, leading to improved blood-sugar control.[13][11]
Tirzepatide was approved for treatment of diabetes in the United States in May 2022,[10][13] in the European Union in September 2022,[12] in Canada in November 2022,[18] and in Australia in December 2022.[2] The US Food and Drug Administration (FDA) considers it to be a first-in-class medication.[19][20] It was approved by the FDA for weight loss in November 2023, under the brand name Zepbound.[16][21] In November 2023, the UK Medicines and Healthcare products Regulatory Agency revised the indication for tirzepatide to include treatment for weight loss.[8][22]
In April 2024, the Food and Drug Administration’s drug shortage database indicates most doses of Zepbound and diabetes counterpart Mounjaro will be in short supply through the second quarter 2024.[23]
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