Masitinib

4-[(4-Methylpiperazin-1-yl)methyl]-N-(4-methyl-3-{[4-(pyridin-3-yl)-1,3-thiazol-2-yl]amino}phenyl)benzamid (IUPAC)

QL01XE90

Protein -tyrosine kinase inhibitor

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Masitinib is a tyrosine kinase inhibitor that is approved in veterinary medicine for the treatment of mast cell tumors in dogs. After the approval in November 2008 masitinib is under the trade name Masivet since mid-2009 in Europe available. In the U.S., the veterinary medicinal product under the trade name Kinavet since 2011 on the market. Holder is AB Science from Paris. The drug is orally effective.

In human medicine, masitinib is in development for the treatment of various cancers (multiple myeloma, metastatic pancreatic cancer, mast cell tumors, malignant melanoma ) and for the treatment of dementia in Alzheimer 's disease. Masitinib is classified as an orphan drug for the treatment of treatment of pancreatic cancer in the EU.

Mechanism of action

Masitinib inhibits in vitro selectively mutated form of c-kit tyrosine kinase. Such permanently activated by mutation c - kit tyrosine kinase plays a role in several forms of cancer. The selective effect of masitinib other receptor tyrosine kinases of class III are not affected.

Masitinib also inhibits the platelet-derived growth factor receptor ( PDGFR ) and fibroblast growth factor receptor ( FGFR3 ).

Chemical and pharmaceutical information

Is used medicinally masitinib as the salt of methanesulfonic acid ( Masitinibmesilat ), which is very good, at alkaline pH in aqueous solutions at acidic pH, however, insoluble.