Description
Selumetinib is an orally bioavailable noncompetitive inhibitor of MEK1/2; it primarily displays immunosuppressive and anticancer chemotherapeutic activities. In cellular and animal models of cancer, selumetinib downregulates MAPK activation and mTOR phosphorylation and upregulates caspases 3 and 7, resulting in caspase-mediated apoptosis and inhibition of tumor growth. In an animal model of graft versus host disease (GVHD), selumetinib inhibits alloreactivity through inhibition of naïve and less-differentiated T cells. Additionally, this compound decreased serum creatine phosphokinase and aspartate aminotransferase to inhibit skeletal muscle pathology and increase muscle function in an animal model of muscular dystrophy.