Toceranib

Toceranib

Systematic (IUPAC) name
5-[(5Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-N-[2-(pyrrolidin-1-yl)ethyl]-1H-pyrrole-3-carboxamide
Clinical data
Trade names	Palladia
AHFS/Drugs.com	International Drug Names
Legal status	US: ℞-only
Routes of administration	Oral
Pharmacokinetic data
Bioavailability	77%
Protein binding	91%-93%
Biological half-life	16 h
Identifiers
CAS Number	356068-94-5
ATCvet code	QL01XE91
PubChem	CID 8034466
ChemSpider	4486268
UNII	59L7Y0530C
ChEMBL	CHEMBL13608
Chemical data
Formula	C22H25FN4O2
Molar mass	396.46 g/mol 494.46 g/mol (phosphate)
SMILES Fc1ccc2c(c1)/C(C(=O)N2)=C/c4c(c(C(=O)NCCN3CCCC3)c(n4)C)C

Toceranib is a receptor tyrosine kinase inhibitor and is used in the treatment^[1] of canine mast cell tumor also called mastocytoma. Together with masitinib (Kinavet (US)/Masivet (EU/ROW) by AB Science), toceranib is the only dog-specific anti-cancer drug^[2] approved by the U.S. Food and Drug Administration.^[3] It is marketed as Palladia as its phosphate salt, toceranib phosphate (INN) by Pfizer. It was developed by SUGEN as SU11654,^[4] a sister compound to sunitinib, which was later approved for human therapies. Toceranib is likely to act mostly through inhibition of the kit tyrosine kinase, though it may also have an anti-angiogenic effect.

References

1. London CA, Malpas PB, Wood-Follis SL, et al. (June 2009). "Multi-center, Placebo-controlled, Double-blind, Randomized Study of Oral Toceranib Phosphate (SU11654), a Receptor Tyrosine Kinase Inhibitor, for the Treatment of Dogs with Recurrent (Either Local or Distant) Mast Cell Tumor Following Surgical Excision.". Clin Cancer Res 15 (11): 3856–65. doi:10.1158/1078-0432.CCR-08-1860. PMID 19470739.
2. CBS News FDA Approves First-Ever Dog Cancer Drug
3. FDA NEWS RELEASE
4. In Trials for New Cancer Drugs, Family Pets Are Benefiting, Too, New York Times

External links

• Official Site for Palladia