NCIt definition : A second-generation tyrosine kinase inhibitor of Bcr-Abl fusion protein and the platelet-derived
growth factor receptor (PDGFR), with potential antineoplastic activity. Upon administration,
radotinib specifically inhibits the Bcr-Abl fusion protein, an abnormal enzyme expressed
in Philadelphia chromosome positive chronic myeloid leukemia (CML) cells. In addition,
this agent also inhibits PDGFR thereby blocking PDGFR-mediated signal transduction
pathways. The inhibitory effect of radotinib on these specific tyrosine kinases may
decrease cellular proliferation and inhibit angiogenesis. PDGFR, upregulated in many
tumor cell types, is a receptor tyrosine kinase essential to cell migration and the
development of the microvasculature.;