Cabozantinib

Cabozantinib
Clinical data
Trade names	Cometriq, Cabometyx, others
Other names	XL184, BMS907351, cabozantinib s-malate
AHFS/Drugs.com	Monograph
MedlinePlus	a613015
License data	US DailyMed: Cabozantinib;
Pregnancy; category	AU: D;
Routes of; administration	By mouth
ATC code	L01EX07 (WHO) ;
Legal status
Legal status	AU: S4 (Prescription only); CA: ℞-only; UK: POM (Prescription only); US: ℞-only; EU: Rx-only;
Pharmacokinetic data
Protein binding	≥99.7%
Metabolism	Liver (CYP3A4-mediated)
Elimination half-life	110 hours
Excretion	Feces (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 ;
ECHA InfoCard	100.221.147
Chemical and physical data
Formula	C28H24FN3O5
Molar mass	501.514 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. It is a small-molecule tyrosine-kinase inhibitor (TKI) of c-Met (HGFR) and VEGFR2, and also inhibits AXL, RET, and FLT3. 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. The capsule form was approved in the European Union for the same purpose in 2014. In April 2016, the FDA granted approval for marketing the tablet formulation (Cabometyx) as a second line treatment for kidney cancer and the same was approved in the European Union in September of that year. The brands Cometriq and Cabometyx have different formulations and are not interchangeable.