Abstract Learning Objectives After completing this course, the reader will be able to: Explain
the IC50 of a tyrosine kinase inhibitor and the kind of information this parameter provides …

Resistance against tyrosine kinase inhibitors (TKIs) represents a relevant clinical problem in
treatment of chronic myelogenous leukemia (CML). On the basis of their activity against the …

Preclinical studies of BCR-ABL mutation sensitivity to nilotinib or dasatinib suggested that
the majority would be sensitive. Correspondingly, the initial clinical trials demonstrated …

A comment on this article appears in" Comparative In vitro cellular data alone are insufficient
to predict clinical responses and guide the choice of BCR-ABL inhibitor for treating imatinib …

Discovery of imatinib mesylate (IM) as the targeted BCR-ABL protein tyrosine kinase
inhibitor (TKI) has resulted in its use as the frontline therapy for chronic myeloid leukemia …

Chronic myelogenous leukaemia (CML) and Philadelphia chromosome positive (Ph+) acute
lymphoblastic leukaemia (ALL) are caused by the BCR-ABL oncogene. Imatinib inhibits the …

Background Additional chromosomal aberrations in Philadelphia chromosome-positive
chronic myeloid leukemia are non-random and strongly associated with disease …

Imatinib is a small-molecule inhibitor of BCR-ABL tyrosine kinase activity, with proven
efficacy and tolerability. Despite imatinib's activity, the development of resistance, whether …

Purpose In patients with chronic myelogenous leukemia (CML), point mutations in the BCR-
ABL1 kinase domain are the most common cause of treatment failure with a tyrosine kinase …

Over the last decade, the treatment of chronic myeloid leukemia has progressed
tremendously. The first-generation tyrosine kinase inhibitor imatinib is now flanked by two …