Nilotinib’s target

Nilotinib (Nilotinib) is a transduction inhibitor that targets BCR-ABL, c-kit and PDGF and is used as a potential treatment for various leukemias, including chronic myelogenous leukemia (CML). Chronic myelogenous leukemia (CML) is caused by the BCR-ABL oncogene. Nilotinib inhibits the tyrosine kinase activity of BCR-ABL protein. Compared with imatinib, nilotinib fits the ATP-binding site of the BCR-ABL protein with higher affinity, overcoming resistance caused by mutations. In vitro, nilotinib inhibits BCR-ABL-mediated proliferation of murine leukemia cell lines and human cell lines derived from Ph+ CML patients. Under assay conditions, nilotinib was able to overcome imatinib resistance caused by BCR-ABL kinase mutations in 32 of 33 tested mutations.