Leukemia Research
Volume 36, Issue 3 , Pages 253-261, March 2012

What do kinase inhibition profiles tell us about tyrosine kinase inhibitors used for the treatment of CML?

  • Michael W. Deininger

      Affiliations

    • Huntsman Cancer Institute, University of Utah, Salt Lake City, UT, USA
    • Corresponding Author InformationCorresponding author at: University of Utah, Huntsman Cancer Institute, 2000 Circle of Hope, Room 4280, Salt Lake City, Utah 84112-5550, USA. Tel.: +1 801 581 6363; fax: +1 801 585 0900.
  • ,
  • Paul Manley

      Affiliations

    • Novartis Pharma AG, Basel, Switzerland

Received 14 July 2011; received in revised form 12 September 2011; accepted 19 September 2011. published online 13 October 2011.

Abstract 

Cancer treatment has long been based upon cytotoxic therapies that affect all rapidly dividing cells, and as such, is necessarily associated with significant toxicity. More recently, drugs targeted toward pathways critical for tumor cell survival have been developed. With limited off-target activity, such therapies are expected to be better tolerated than broad-acting cytotoxic chemotherapies. BCR-ABL inhibitors in chronic myeloid leukemia are reviewed as a model to investigate the concept of targeted cancer therapies and evaluate how the kinase inhibition profiles of these agents may contribute to their toxicity profiles.

Keywords: Kinase inhibition profiles, BCR-ABL inhibitors, Chronic myeloid leukemia, Tyrosine kinase inhibitors, Imatinib, Nilotinib, Dasatinib, Bosutinib

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PII: S0145-2126(11)00461-9

doi:10.1016/j.leukres.2011.09.018

Leukemia Research
Volume 36, Issue 3 , Pages 253-261, March 2012