NCIt definition : The monohydrate form of bosutinib, a synthetic quinolone derivative and dual kinase
inhibitor that targets both Abl and Src kinases with potential antineoplastic activity.
Unlike imatinib, bosutinib inhibits the autophosphorylation of both Abl and Src kinases,
resulting in inhibition of cell growth and apoptosis. Because of the dual mechanism
of action, this agent may have activity in resistant CML disease, other myeloid malignancies
and solid tumors. Abl kinase is upregulated in the presence of the abnormal Bcr-abl
fusion protein which is commonly associated with chronic myeloid leukemia (CML). Overexpression
of specific Src kinases is also associated with the imatinib-resistant CML phenotype.;