Cabozantinib

Cabozantinib
Clinical data
Trade namesCometriq, Cabometyx, others
Other namesXL184, BMS907351, cabozantinib s-malate
AHFS/Drugs.comMonograph
MedlinePlusa613015
License data
Pregnancy
category
Routes of
administration		By mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Protein binding≥99.7%
MetabolismLiver (CYP3A4-mediated)
Elimination half-life110 hours
ExcretionFeces (54%), urine (27%)
Identifiers
  • N-(4-((6,7-Dimethoxyquinolin-4-yl)oxy)phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.221.147 Edit this at Wikidata
Chemical and physical data
FormulaC28H24FN3O5
Molar mass501.514 g·mol−1
3D model (JSmol)
  • COc1cc2nccc(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3)c2cc1OC
  • 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 tyrosine-kinase inhibitor (TKI) of c-Met (HGFR) and VEGFR2, and also inhibits AXL, RET, and FLT3.[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).