TY - JOUR
T1 - Mechanisms of primary and secondary resistance to imatinib in chronic myeloid leukemia
AU - Quintás-Cardama, Alfonso
AU - Kantarjian, Hagop M.
AU - Cortes, Jorge E.
PY - 2009/4
Y1 - 2009/4
N2 - Background: Although the vast majority of patients with chronic myeloid leukemia (CML) respond to the tyrosine kinase inhibitor (TKI) imatinib mesylate, resistance might occur de novo or during treatment. Methods: The authors reviewed the known mechanisms of primary and secondary resistance to imatinib and other TKIs used in the management of CML. Results: Mutations within the kinase domain of BCR-ABLI account for 30% to 40% of cases of imatinib resistance. Other mechanisms include BCR-ABLI amplification, overexpression of the SRC family of kinases, and pharmacokinetic and pharmacodynamic factors. Conclusions: Although not all resistance mechanisms have been identified and understood, several agents based on the known mechanisms have already been designed and developed and are beginning clinical trials.
AB - Background: Although the vast majority of patients with chronic myeloid leukemia (CML) respond to the tyrosine kinase inhibitor (TKI) imatinib mesylate, resistance might occur de novo or during treatment. Methods: The authors reviewed the known mechanisms of primary and secondary resistance to imatinib and other TKIs used in the management of CML. Results: Mutations within the kinase domain of BCR-ABLI account for 30% to 40% of cases of imatinib resistance. Other mechanisms include BCR-ABLI amplification, overexpression of the SRC family of kinases, and pharmacokinetic and pharmacodynamic factors. Conclusions: Although not all resistance mechanisms have been identified and understood, several agents based on the known mechanisms have already been designed and developed and are beginning clinical trials.
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U2 - 10.1177/107327480901600204
DO - 10.1177/107327480901600204
M3 - Review article
C2 - 19337198
AN - SCOPUS:65249185560
SN - 1073-2748
VL - 16
SP - 122
EP - 131
JO - Cancer Control
JF - Cancer Control
IS - 2
ER -