Chronic inflammatory disorders are linked to a deregulation of the immune system, leading to organ infiltration of many inflammatory cells (e.g. mast cell, macrophage, lymphocyte, granulocytes, dendritic cells). It has been widely demonstrated that kinases such as c-Kit, Lyn and PDGFR, all key targets of masitinib, are strongly implicated in the activation of inflammatory cells and fibrous tissue remodeling.
It has been shown that mast cells play a key role in the organization and activation of the inflammatory cascade, not only by participating directly in the tissue destruction but also by recruiting and activating other immune cells such as macrophages and lymphocytes. The kinases of c-Kit, Lyn and Fyn are critical kinases for mast cell function. Therefore, therapeutic agents able to inhibit these kinases can modulate the activity of mast cells, subsequently leading to a reduction in tissue inflammation and consequently clinical benefits. In-vitro and animal studies have now largely demonstrated that masitinib is a potent inhibitor of these kinases, which makes masitinib a promising drug candidate in diseases where chronic inflammation plays a central role.