Masitinib is a protein tyrosine kinase inhibitor that selectively targets stem cell factor receptor c-kit in particular and also PDGFRalpha/beta and Lyn. It is more potent and selective for c-kit than imatinib (Gleevec). Masitinib has antineoplastic and anti-inflammatory activity. It inhibits the survival, migration and activity of mast cells, key components of the inflammation response. It is used to treat mast cell tumors in dogs and is in clinical trials for human use in rheumatoid arthritis, asthma, and as an adjuct therapy for Alzheimer′s disease.
The stem cell factor receptor, KIT, is a target for the treatment of cancer, mastocytosis, and inflammatory diseases. Here, we characterise the in vitro and in vivo profiles of masitinib (AB1010), a novel phenylaminothiazole-type tyrosine kinase inhibitor that targets KIT.
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