NCIt definition : An orally bioavailable, selective, active-form inhibitor of tyrosine kinase BCR-ABL
fusion oncoprotein, with potential antineoplastic activity. Upon oral administration,
BCR-ABL inhibitor ELVN-001 specifically targets and binds to the ATP-binding site
in the kinase domain of activated BCR-ABL1, thereby inhibiting the activity of both
wild-type BCR-ABL and certain mutation forms, including the T315I mutation. This binding
results in the inhibition of BCR-ABL-mediated proliferation and enhanced apoptosis
of Philadelphia chromosome-positive (Ph ) hematological malignancies. The BCR-ABL
fusion protein tyrosine kinase is an abnormal enzyme produced by leukemia cells that
contain the Philadelphia chromosome. The T315I mutation, the most common BCR-ABL mutation,
shows resistance to nearly all commonly used tyrosine kinase inhibitors (TKIs).;