Product Name

Cabozantinib

CAS Number

849217-68-1

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Product Name:
Cabozantinib
CAS Number:
849217-68-1
Indication:
For the treatment of metastatic medullary thyroid cancer.
Mode of Action:

Cabozantinib inhibits specific receptor tyrosine kinases such as VEGFR-1, -2 and -3, KIT, TRKB, FLT-3, AXL, RET, MET, and TIE-2.

Pharmacodynamics:

Cabozantinib suppresses metastasis, angiogenesis, and oncognesis by inhibiting receptor tyrosine kinases.

Metabolism:

Cabozantinib is metabolized mostly by CYP3A4 and, to a minor extent, by CYP2C9. Both enzyme produce an N-oxide metabolite.

Toxicity:

Cabozantinib has a black box warning of serious gastrointestinal fistulas and perforations, and potentially fatal hemoptysis and gastrointestinal hemorrhage.

IUPAC:
1, 1-Cyclopropanedicarboxamide, N'-(4-((6, 7-dimethoxy-4-quinolinyl)oxy]phenyl]-N-(4- fluorophenyl)-
DrugBank:
DB08875
Formula:
C28H24FN3O5
Molecular Mass:
501.5
Synonyms:
BMS 907351, Cabozantinib, Cometriq, UNII-1C39JW444G, XL 184, XL-184, XL184
SMILES:
COc1cc2c(ccnc2cc1OC)Oc3ccc(cc3)NC(=O)C4(CC4)C(=O)Nc5ccc(cc5)F
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)
General Reference:
General Reference:

 

  1. Durante C, Russo D, Verrienti A, Filetti S: XL184 (cabozantinib) for medullary thyroid carcinoma. Expert Opin Investig Drugs. 2011 Mar;20(3):407-413. doi: 10.1517/13543784.2011.559163. Pubmed

 

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