Toceranib

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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 ℞-only (US)
Routes Oral
Pharmacokinetic data
Bioavailability 77%
Protein binding 91%-93%
Half-life 16 h
Identifiers
CAS number 256068-94-5
ATCvet code QL01XE91
PubChem CID 8034466
ChemSpider 4486268
UNII 59L7Y0530C YesY
Chemical data
Formula C22H25FN4O2 
Mol. mass 396.46 g/mol
494.46 g/mol (phosphate)

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

Targeted therapy / extracellular chemotherapeutic agents/antineoplastic agents (L01)
CI monoclonal antibodies ("-mab")
Others for solid tumors
Tyrosine-kinase inhibitors ("-nib")

EML4-ALK (Crizotinib)

RET inhibitors: Vandetanib (Also VEGFR and EGFR).

c-MET inhibitor: Cabozantinib (Also VEGFR2).
Other

M: NEO

tsoc, mrkr

tumr, epon, para

drug (L1i/1e/V03)


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