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Tirzepatide

Tirzepatide
Clinical data
Pronunciation/tɜːrˈzɛpətaɪd/
tur-ZEP-ə-tyde
Trade namesMounjaro, Zepbound
Other namesLY3298176, GIP/GLP-1 RA
AHFS/Drugs.comMonograph
MedlinePlusa622044
License data
Pregnancy
category
Routes of
administration		Subcutaneous
Drug classAntidiabetic, GLP-1 receptor agonist
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability80%
Protein bindingAlbumin
MetabolismProteolytic cleavage, β-oxidation of fatty diacid section and amide hydrolysis
Elimination half-life5 days
ExcretionUrine and faeces
Identifiers
  • (2S)-2-[[20-[[(5S)-6-[[(2S,3S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[2-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[(2S)-2-[(2S)-2-[(2S)-2-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-5-[[(2S)-2-[[(2S)-2-[[2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylpentanoyl]amino]-2-methylpropanoyl]amino]-4-methylpentanoyl]amino]-3-carboxypropanoyl]amino]-6-oxohexyl]amino]-20-oxoicosanoyl]amino]-5-[2-[2-[2-[2-[2-(carboxymethoxy)ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-5-oxopentanoic acid
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
FormulaC225H348N48O68
Molar mass4813.527 g·mol−1
3D model (JSmol)
  • C[C@@H](O)[C@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)CC1C=CC(O)=CC=1)C(=O)N[C@@H](CC1C=CC=CC=1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC1C=CC(O)=CC=1)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)CC)C(=O)NC(C)(C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@@H](NC(=O)CCCCCCCCCCCCCCCCCCC(O)=O)C(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC1C=CC=CC=1)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC1=CNC2C=CC=CC1=2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O
  • InChI=1S/C225H348N48O68/c1-23-126(10)183(264-198(311)146(64-50-52-88-226)246-202(315)157(109-180(297)298)252-199(312)152(103-124(6)7)261-223(337)225(21,22)269-217(330)185(128(12)25-3)266-209(322)163(120-278)257-200(313)153(107-138-74-78-141(282)79-75-138)250-203(316)158(110-181(299)300)253-207(320)162(119-277)259-216(329)187(134(18)280)267-206(319)155(106-136-60-44-41-45-61-136)254-215(328)186(133(17)279)262-174(289)114-237-193(306)147(83-87-179(295)296)260-222(336)224(19,20)268-192(305)143(227)104-137-72-76-140(281)77-73-137)214(327)242-131(15)190(303)244-148(80-84-168(228)283)196(309)245-145(65-51-53-89-231-175(290)121-340-100-99-339-97-91-233-176(291)122-341-101-98-338-96-90-232-170(285)86-82-150(221(334)335)243-171(286)70-46-38-36-34-32-30-28-26-27-29-31-33-35-37-39-47-71-178(293)294)195(308)240-130(14)191(304)248-154(105-135-58-42-40-43-59-135)205(318)263-182(125(8)9)212(325)247-149(81-85-169(229)284)197(310)251-156(108-139-111-234-144-63-49-48-62-142(139)144)201(314)249-151(102-123(4)5)204(317)265-184(127(11)24-2)213(326)241-129(13)189(302)236-112-172(287)235-115-177(292)270-92-54-66-164(270)210(323)258-161(118-276)208(321)256-160(117-275)194(307)238-113-173(288)239-132(16)218(331)272-94-56-68-166(272)220(333)273-95-57-69-167(273)219(332)271-93-55-67-165(271)211(324)255-159(116-274)188(230)301/h40-45,48-49,58-63,72-79,111,123-134,143,145-167,182-187,234,274-282H,23-39,46-47,50-57,64-71,80-110,112-122,226-227H2,1-22H3,(H2,228,283)(H2,229,284)(H2,230,301)(H,231,290)(H,232,285)(H,233,291)(H,235,287)(H,236,302)(H,237,306)(H,238,307)(H,239,288)(H,240,308)(H,241,326)(H,242,327)(H,243,286)(H,244,303)(H,245,309)(H,246,315)(H,247,325)(H,248,304)(H,249,314)(H,250,316)(H,251,310)(H,252,312)(H,253,320)(H,254,328)(H,255,324)(H,256,321)(H,257,313)(H,258,323)(H,259,329)(H,260,336)(H,261,337)(H,262,289)(H,263,318)(H,264,311)(H,265,317)(H,266,322)(H,267,319)(H,268,305)(H,269,330)(H,293,294)(H,295,296)(H,297,298)(H,299,300)(H,334,335)/t126-,127-,128-,129-,130-,131-,132-,133+,134+,143-,145-,146-,147-,148-,149-,150+,151-,152-,153-,154-,155-,156-,157-,158-,159-,160-,161-,162-,163-,164-,165-,166-,167-,182-,183-,184-,185-,186-,187-/m0/s1
  • Key:BTSOGEDATSQOAF-SMAAHMJQSA-N

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]

  1. ^ a b "Australian prescription medicine decision summaries: Mounjaro". Therapeutic Goods Administration. Archived from the original on 5 February 2023. Retrieved 28 February 2023.
  2. ^ 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.
  3. ^ "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.
  4. ^ https://www.tga.gov.au/resources/auspar/auspar-mounjaro
  5. ^ "Details for: Mounjaro". Health Canada. 24 November 2022. Archived from the original on 10 March 2024. Retrieved 3 March 2024.
  6. ^ "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.
  7. ^ "Summary Basis of Decision - Mounjaro". Health Canada. 17 March 2023. Archived from the original on 25 April 2023. Retrieved 24 April 2023.
  8. ^ a b "Mounjaro 5mg solution for injection in pre-filled pen". (emc). 16 November 2023. Archived from the original on 27 June 2023. Retrieved 17 November 2023.
  9. ^ "Mounjaro 2.5mg solution for injection in pre-filled pen". (emc). 16 November 2023. Archived from the original on 6 August 2023. Retrieved 17 November 2023.
  10. ^ a b c d e "Mounjaro- tirzepatide injection, solution". DailyMed. 13 May 2022. Archived from the original on 3 July 2022. Retrieved 27 May 2022.
  11. ^ a b c "Zepbound- tirzepatide injection, solution". DailyMed. 9 November 2023. Archived from the original on 20 November 2023. Retrieved 20 November 2023.
  12. ^ 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.
  13. ^ a b c d e f "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. Public Domain This article incorporates text from this source, which is in the public domain.
  14. ^ Cite error: The named reference moa was invoked but never defined (see the help page).
  15. ^ 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.
  16. ^ a b Cite error: The named reference FDA Zepbound PR was invoked but never defined (see the help page).
  17. ^ 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.
  18. ^ "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.
  19. ^ "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. Public Domain This article incorporates text from this source, which is in the public domain.
  20. ^ New Drug Therapy Approvals 2022 (PDF). U.S. Food and Drug Administration (FDA) (Report). January 2024. Archived from the original on 14 January 2024. Retrieved 14 January 2024. Public Domain This article incorporates text from this source, which is in the public domain.
  21. ^ 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.
  22. ^ "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.
  23. ^ Constantino AK (17 April 2024). "Most doses of Eli Lilly's Zepbound, Mounjaro in short supply through June, FDA says". CNBC. Retrieved 18 April 2024.

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