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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 EU: Rx-only
Pharmacokinetic data
Bioavailability	77%
Protein binding	91%-93%
Elimination half-life	16 h
Identifiers
IUPAC name 5--2,4-dimethyl-N--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
3D model (JSmol)	Interactive image
SMILES Fc1ccc2c(c1)/C(C(=O)N2)=C/c4c(c(C(=O)NCCN3CCCC3)c(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 (INN), sold under the brand name Palladia, is a receptor tyrosine kinase inhibitor that is used in the treatment of canine mast cell tumor also called mastocytoma. It is the first medication developed specifically for the treatment of cancer in dogs. It is used as its phosphate salt, toceranib phosphate. It was developed by SUGEN as SU11654, a sister compound to sunitinib, which was later approved for human therapies. Toceranib is a tyrosine kinase inhibitor and works in two ways: by killing tumor cells and by cutting off the blood supply to the tumor.

The most common side effects include diarrhea, decrease or loss of appetite, lameness, weight loss, and blood in the stool.

Veterinary uses

Toceranib is indicated to treat canine cutaneous (skin-based) mast cell tumors, a type of cancer responsible for about one out of five cases of canine skin tumors. It is approved to treat the tumors with or without regional lymph node involvement.

References

1. "Palladia EPAR". European Medicines Agency. 1 October 2009. Retrieved 1 July 2024.
2. World Health Organization (2009). "International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 62". WHO Drug Information. 23 (2). hdl:10665/74420.
3. London CA, Malpas PB, Wood-Follis SL, Boucher JF, Rusk AW, Rosenberg MP, 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". Clinical Cancer Research. 15 (11): 3856–3865. doi:10.1158/1078-0432.CCR-08-1860. PMID 19470739.
4. ^ "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. This article incorporates text from this source, which is in the public domain.
5. "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.
6. "In Trials for New Cancer Drugs, Family Pets Are Benefiting, Too". The New York Times. 24 November 2006. Archived from the original on 27 February 2021. Retrieved 2 October 2021.

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