Toceranib

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Toceranib
Toceranib.svg
Ball-and-stick model of the toceranib molecule
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
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 (WHO)
PubChem CID: 8034466
ChemSpider 4486268
UNII 59L7Y0530C YesY
ChEMBL CHEMBL13608
Chemical data
Formula C22H25FN4O2
Molecular mass 396.46 g/mol
494.46 g/mol (phosphate)
  • 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.

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