Toceranib

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-[(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;

Last updated May 02, 2025

Toceranib (INN ^[2]), 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.^[3] It is the first medication developed specifically for the treatment of cancer in dogs.^[4]^[5] It is used as its phosphate salt, toceranib phosphate. It was developed by SUGEN as SU11654,^[6] 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.^[4]

The most common side effects include diarrhea, decrease or loss of appetite, lameness, weight loss, and blood in the stool.^[4]

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.^[4] It is approved to treat the tumors with or without regional lymph node involvement.^[4]

References

↑ "Palladia EPAR". European Medicines Agency. 1 October 2009. Retrieved 1 July 2024.
↑ World Health Organization (2009). "International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 62". WHO Drug Information. 23 (2). hdl: 10665/74420 .
↑ 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.
1 2 3 4 5 "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 .
↑ "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. Archived from the original on 27 February 2021. Retrieved 2 October 2021.

This page is based on this Wikipedia article
Text is available under the CC BY-SA 4.0 license; additional terms may apply.
Images, videos and audio are available under their respective licenses.

[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 .

[pmid17227978-3] 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.

[FDA_PR_20090603-4] 1 2 3 4 5 "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.

[1]

[2]

[3]

[4]

[5]

[6]