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Cabozantinib information


Cabozantinib
Clinical data
Trade namesCometriq, Cabometyx, others
Other namesXL184, BMS907351, cabozantinib s-malate
AHFS/Drugs.comMonograph
MedlinePlusa613015
License data
  • US DailyMed: Cabozantinib
Pregnancy
category
  • AU: D[1]
Routes of
administration
By mouth
ATC code
  • L01EX07 (WHO)
Legal status
Legal status
  • AU: S4 (Prescription only)[2][3][4]
  • CA: ℞-only[5][6]
  • UK: POM (Prescription only)[7][8]
  • US: ℞-only[9][10]
  • EU: Rx-only[11][12]
Pharmacokinetic data
Protein binding≥99.7%
MetabolismLiver (CYP3A4-mediated)
Elimination half-life110 hours
ExcretionFeces (54%), urine (27%)
Identifiers
IUPAC name
  • N-(4-((6,7-Dimethoxyquinolin-4-yl)oxy)phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
CAS Number
  • 849217-68-1
  • as salt: 1140909-48-3
PubChem CID
  • 25102847
DrugBank
  • DB08875
  • as salt: DBSALT001762
ChemSpider
  • 25948202
  • as salt: 25948203
UNII
  • 1C39JW444G
  • as salt: DR7ST46X58
KEGG
  • D10062
  • as salt: D10095
ChEBI
  • CHEBI:72317
  • as salt: CHEBI:72319
ChEMBL
  • ChEMBL2105717
  • as salt: ChEMBL2103868
CompTox Dashboard (EPA)
  • DTXSID10233968 Edit this at Wikidata
ECHA InfoCard100.221.147 Edit this at Wikidata
Chemical and physical data
FormulaC28H24FN3O5
Molar mass501.514 g·mol−1
3D model (JSmol)
  • Interactive image
SMILES
  • COc1cc2nccc(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3)c2cc1OC
InChI
  • InChI=1S/C28H24FN3O5/c1-35-24-15-21-22(16-25(24)36-2)30-14-11-23(21)37-20-9-7-19(8-10-20)32-27(34)28(12-13-28)26(33)31-18-5-3-17(29)4-6-18/h3-11,14-16H,12-13H2,1-2H3,(H,31,33)(H,32,34)
  • Key:ONIQOQHATWINJY-UHFFFAOYSA-N

Cabozantinib, sold under the brand names Cometriq and Cabometyx among others, is an anti-cancer medication used to treat medullary thyroid cancer, renal cell carcinoma, and hepatocellular carcinoma.[9][10] It is a small molecule inhibitor of the tyrosine kinases c-Met and VEGFR2, and also inhibits AXL and RET.[8][7] It was discovered and developed by Exelixis Inc.

In November 2012, cabozantinib in its capsule formulation was approved by the US Food and Drug Administration (FDA) under the name Cometriq for treating people with medullary thyroid cancer.[13][14] The capsule form was approved in the European Union for the same purpose in 2014.[11] In April 2016, the FDA granted approval for marketing the tablet formulation (Cabometyx) as a second line treatment for kidney cancer[15][16] and the same was approved in the European Union in September of that year.[12] The brands Cometriq and Cabometyx have different formulations and are not interchangeable.[17]

  1. ^ "Cabozantinib Use During Pregnancy". Drugs.com. 30 March 2020. Retrieved 23 September 2020.
  2. ^ "Cabometyx (Ipsen Pty Ltd)". Therapeutic Goods Administration (TGA). 13 January 2023. Retrieved 9 April 2023.
  3. ^ "Cabometyx cabozantinib (as (S)-malate) 20 mg film-coated tablet bottle (283800)". Therapeutic Goods Administration (TGA). 27 May 2022. Retrieved 9 April 2023.
  4. ^ "AusPAR: Cabozantinib". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 9 April 2023.
  5. ^ "Summary Basis of Decision (SBD) for Cabometyx". Health Canada. 23 October 2014. Retrieved 29 May 2022.
  6. ^ "Drug and medical device highlights 2018: Helping you maintain and improve your health". Health Canada. 14 October 2020. Retrieved 17 April 2024.
  7. ^ a b Cite error: The named reference UKlabelTablet was invoked but never defined (see the help page).
  8. ^ a b Cite error: The named reference UKlabelCapsule was invoked but never defined (see the help page).
  9. ^ a b "Cabometyx- cabozantinib tablet". DailyMed. 21 July 2020. Retrieved 23 September 2020.
  10. ^ a b "Cometriq- cabozantinib kit Cometriq- cabozantinib capsule". DailyMed. 11 February 2020. Retrieved 23 September 2020.
  11. ^ a b Cite error: The named reference Cometriq EPAR was invoked but never defined (see the help page).
  12. ^ a b Cite error: The named reference Cabometyx EPAR was invoked but never defined (see the help page).
  13. ^ Cite error: The named reference FDA2012 was invoked but never defined (see the help page).
  14. ^ Cite error: The named reference Cometriq FDA approval was invoked but never defined (see the help page).
  15. ^ Cite error: The named reference FDA2016-04 was invoked but never defined (see the help page).
  16. ^ Cite error: The named reference Cabometyx FDA approval was invoked but never defined (see the help page).
  17. ^ Cite error: The named reference FDA Cabometyx 20171219 was invoked but never defined (see the help page).

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Cabozantinib

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Exelixis

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partnered its lead cancer drug candidate, XL-184 (which would become called cabozantinib) and another cancer candidate, XL-281, with Bristol Myers Squibb; BMS...

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Beacon Pharmaceuticals

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Medullary thyroid cancer

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surgery. Cabozantinib, trade name Cometriq, was granted marketing approval (November 2012) by the U.S. FDA for this indication. Cabozantinib which is...

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Toni Choueiri

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Institute. His work has led to the establishment of several novel drugs (cabozantinib, avelumab, pazopanib and others including combinations) and prognostic...

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Ipsen

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spasticity in children aged two years and older. In 2016, Ipsen licensed cabozantinib from Exelixis, which received marketing authorization the same year for...

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cancer (MTC) who require systemic therapy following prior treatment with cabozantinib and/or vandetanib. Selpercatinib can cause serious side effects including...

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Insulin

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RET inhibitor

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that possess a broad range of targets along with RET. These included cabozantinib, lenvatinib, sunitinib and alectinib. Since they were not designed to...

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Trastuzumab deruxtecan

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Testosterone

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