Masitinib

Masitinib
Clinical data
Trade names	Masivet, Kinavet
AHFS/Drugs.com	International Drug Names
ATC code	L01XE22 (WHO) ;
Identifiers
	IUPAC name 4-[(4-Methylpiperazin-1-yl)methyl]-N-(4-methyl-3-{[4-(pyridin-3-yl)-1,3-thiazol-2-yl]amino}phenyl)benzamide;
CAS Number	790299-79-5;
PubChem CID	10074640;
ChemSpider	8250179;
KEGG	D10229;
ChEMBL	ChEMBL1908391;
PDB ligand	G65 (PDBe, RCSB PDB);
Chemical and physical data
Formula	C28H30N6OS
Molar mass	498.64 g/mol g·mol−1
3D model (JSmol)	Interactive image;
	SMILES O=C(c1ccc(cc1)CN2CCN(C)CC2)Nc3cc(c(cc3)C)Nc4nc(cs4)c5cccnc5;
	InChI InChI=InChI=1S/C28H30N6OSc1-20-5-10-24(16-25(20)31-28-32-26(19-36-28)23-4-3-11-29-17-23)30-27(35)22-8-6-21(7-9-22)18-34-14-12-33(2)13-15-34h3-11,16-17,19H,12-15,18H2,1-2H3,(H,30,35)(H,31,32); Key:WJEOLQLKVOPQFV-UHFFFAOYSA-N;

Masitinib is a tyrosine-kinase inhibitor used in the treatment of mast cell tumours in animals, specifically dogs.[1][2] Since its introduction in November 2008 it has been distributed under the commercial name Masivet. It has been available in Europe since the second part of 2009. Masitinib has been studied for several human conditions including melanoma, multiple myeloma, gastrointestinal cancer, pancreatic cancer, Alzheimer disease, multiple sclerosis, rheumatoid arthritis, mastocytosis, and amyotrophic lateral sclerosis.[3][4]

Mechanism of action

Masitinib inhibits the receptor tyrosine kinase c-Kit which is displayed by various types of tumour.[2] It also inhibits the platelet derived growth factor receptor (PDGFR), lymphocyte-specific protein tyrosine kinase (Lck), focal adhesion kinase (FAK) and fibroblast growth factor receptor 3 (FGFR3).[5]

References

Hahn, K.A.; Oglivie, G.; Rusk, T.; Devauchelle, P.; Leblanc, A.; Legendre, A.; Powers, B.; Leventhal, P.S.; Kinet, J.-P.; Palmerini, F.; Dubreuil, P.; Moussy, A.; Hermine, O. (2008). "Masitinib is Safe and Effective for the Treatment of Canine Mast Cell Tumors". Journal of Veterinary Internal Medicine. 22 (6): 1301–1309. doi:10.1111/j.1939-1676.2008.0190.x. ISSN 0891-6640. PMID 18823406.
Information about Masivet at the European pharmacy agency website
http://www.ema.europa.eu/ema/index.jsp?curl=pages/medicines/human/orphans/2016/10/human_orphan_001821.jsp
Folch, J; Petrov, D; Ettcheto, M; Pedrós, I; Abad, S; Beas-Zarate, C; Lazarowski, A; Marin, M; Olloquequi, J; Auladell, C; Camins, A (June 2015). "Masitinib for the treatment of mild to moderate Alzheimer's disease". Expert Review of Neurotherapeutics. 15 (6): 587–96. doi:10.1586/14737175.2015.1045419. PMID 25961655.
Gil da Costa, RM (July 2015). "C-kit as a prognostic and therapeutic marker in canine cutaneous mast cell tumours: From laboratory to clinic". Veterinary Journal (London, England : 1997). 205 (1): 5–10. doi:10.1016/j.tvjl.2015.05.002. PMID 26021891.

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[HahnOglivie2008-1] Hahn, K.A.; Oglivie, G.; Rusk, T.; Devauchelle, P.; Leblanc, A.; Legendre, A.; Powers, B.; Leventhal, P.S.; Kinet, J.-P.; Palmerini, F.; Dubreuil, P.; Moussy, A.; Hermine, O. (2008). "Masitinib is Safe and Effective for the Treatment of Canine Mast Cell Tumors". Journal of Veterinary Internal Medicine. 22 (6): 1301–1309. doi:10.1111/j.1939-1676.2008.0190.x. ISSN 0891-6640. PMID 18823406.

[epar-2] Information about Masivet at the European pharmacy agency website

[3] ttp://www.ema.europa.eu/ema/index.jsp?curl=pages/medicines/human/orphans/2016/10/human_orphan_001821.jsp

[4] Folch, J; Petrov, D; Ettcheto, M; Pedrós, I; Abad, S; Beas-Zarate, C; Lazarowski, A; Marin, M; Olloquequi, J; Auladell, C; Camins, A (June 2015). "Masitinib for the treatment of mild to moderate Alzheimer's disease". Expert Review of Neurotherapeutics. 15 (6): 587–96. doi:10.1586/14737175.2015.1045419. PMID 25961655.

[5] Gil da Costa, RM (July 2015). "C-kit as a prognostic and therapeutic marker in canine cutaneous mast cell tumours: From laboratory to clinic". Veterinary Journal (London, England : 1997). 205 (1): 5–10. doi:10.1016/j.tvjl.2015.05.002. PMID 26021891.