Toceranib Knowpia

Toceranib
Clinical data
Trade names	Palladia
AHFS/Drugs.com	Veterinary Use
License data	US DailyMed: Toceranib;
Routes of; administration	By mouth
Drug class	Antineoplastic agent
ATCvet code	QL01EX90 (WHO) ;
Legal status
Legal status	CA: ℞-only; 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; as salt: 874819-74-6;
PubChem CID	5329106; as salt: 16034840;
ChemSpider	4486268; as salt: 13163443;
UNII	59L7Y0530C; as salt: 24F9PF7J3R;
KEGG	D08503; as salt: D08544;
ChEMBL	ChEMBL13608; as salt: ChEMBL2103833;
PDB ligand	BWC (PDBe, RCSB PDB);
CompTox Dashboard (EPA)	DTXSID50189076 ;
Chemical and physical data
Formula	C22H25FN4O2
Molar mass	396.466 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES Fc1ccc2c(c1)/C(C(=O)N2)=C/c4c(c(C(=O)NCCN3CCCC3)c([nH]4)C)C;
	InChI InChI=1S/C22H25FN4O2/c1-13-19(12-17-16-11-15(23)5-6-18(16)26-21(17)28)25-14(2)20(13)22(29)24-7-10-27-8-3-4-9-27/h5-6,11-12,25H,3-4,7-10H2,1-2H3,(H,24,29)(H,26,28)/b17-12-; Key:SRSGVKWWVXWSJT-ATVHPVEESA-N;

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 (FDA).^[3]^[4] It is sold under the brand name Palladia as its phosphate salt, toceranib phosphate (INN) by Pfizer. It was developed by SUGEN as SU11654,^[5] 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 edit

^ 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.
^ CBS News FDA Approves First-Ever Dog Cancer Drug
^ "FDA: First Drug to Treat Cancer in Dogs Approved". U.S. Food and Drug Administration (FDA) (Press release). 3 June 2009. Archived from the original on 22 July 2010. Retrieved 2 October 2021.
^ "Palladia New Animal Drug Application" (PDF). U.S. Food and Drug Administration (FDA). 22 May 2009. Archived from the original (PDF) on 16 November 2010. Retrieved 2 October 2021.
^ "In Trials for New Cancer Drugs, Family Pets Are Benefiting, Too". The New York Times. 24 November 2006. Retrieved 2 October 2021.

External links edit

"Toceranib". Drug Information Portal. U.S. National Library of Medicine.

[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.

[2] CBS News FDA Approves First-Ever Dog Cancer Drug

[3] "FDA: First Drug to Treat Cancer in Dogs Approved". U.S. Food and Drug Administration (FDA) (Press release). 3 June 2009. Archived from the original on 22 July 2010. Retrieved 2 October 2021.

[4] "Palladia New Animal Drug Application" (PDF). U.S. Food and Drug Administration (FDA). 22 May 2009. Archived from the original (PDF) on 16 November 2010. Retrieved 2 October 2021.

[5] "In Trials for New Cancer Drugs, Family Pets Are Benefiting, Too". The New York Times. 24 November 2006. Retrieved 2 October 2021.

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Summary

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