NCIt definition : An orally bioavailable, Bcr-Abl tyrosine kinase inhibitor, with potential antineoplastic
activity. Designed to overcome resistance of tumor cells to second generation Bcr-Abl
inhibitors, vamotinib targets and binds to the Bcr-Abl fusion oncoprotein, including
those fusion proteins with the 'gatekeeper' resistance mutation T315I, an amino acid
substitution at position 315 in Bcr-Abl from a threonine (T) to an isoleucine (I).
This inhibits Bcr-Abl-mediated proliferation of, and enhances apoptosis in, Philadelphia
chromosome-positive (Ph ) hematologic malignancies. The Bcr-Abl fusion protein is
an aberrantly activated tyrosine kinase produced by leukemia cells that contain the
Philadelphia chromosome.;