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BCR-ABL tyrosine kinase inhibitors inhibit the enzyme BCR-ABL tyrosine kinase, which is important in the pathogenesis of chronic myelogenous leukemia (CML).

Chronic myelogenous leukemia occurs due a single genetic abnormality, known as the Philadelphia chromosome. During the translocation when the Philadelphia chromosome is created, a fusion gene called BCR-ABL gene is formed. The BCR-ABL gene encodes for the BCR-ABL tyrosine kinase. The BCR-ABL positive cells in chronic myelogenous leukemia have increased proliferation and resistance to cell death.

BCR-ABL tyrosine kinase inhibitors are used to treat chronic myelogenous leukemia.