Toceranib

Toceranib
Clinical data
Trade names	Palladia
AHFS/Drugs.com	International Drug Names
Routes of; administration	Oral
ATCvet code	QL01XE91 (WHO) ;
Legal status
Legal status	US: ℞-only;
Pharmacokinetic data
Bioavailability	77%
Protein binding	91%-93%
Elimination half-life	16 h
Identifiers
	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;
CAS Number	356068-94-5;
PubChem CID	8034466;
ChemSpider	4486268;
UNII	59L7Y0530C;
CompTox Dashboard (EPA)	DTXSID50189076 ;
Chemical and physical data
Formula	C22H25FN4O2
Molar mass	396.46 g/mol; 494.46 g/mol (phosphate) g·mol−1
3D model (JSmol)	Interactive image;
	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

^ 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. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)
^ CBS News FDA Approves First-Ever Dog Cancer Drug
^ FDA NEWS RELEASE
^ In Trials for New Cancer Drugs, Family Pets Are Benefiting, Too, New York Times

External links

Official Site for Palladia

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[pmid17227978-1] 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. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)

[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

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