TY - JOUR
T1 - Dasatinib for the treatment of Philadelphia chromosome-positive leukaemias
AU - Jabbour, Elias
AU - Cortes, Jorge
AU - Kantarjian, Hagop
N1 - Funding Information:
Dasatinib is a novel potent multi-targeted kinase inhibitor, Assistance with manuscript preparation was provided by which was recently approved for the treatment of adults with Gardiner-Caldwell US (funded by Bristol-Myers Squibb). Ph-positive CML or Ph-positive ALL who were resistant to or J Cortes and H Kantarjian received research grants from intolerant of imatinib. Other potential benefits of dasatinib in Novartis and Bristol-Myers Squibb.
Copyright:
Copyright 2008 Elsevier B.V., All rights reserved.
PY - 2007/5
Y1 - 2007/5
N2 - BCR-ABL, a constitutively active tyrosine kinase, causes chronic myeloid leukaemia (CML). Rational development of drugs targeting BCR-ABL has significantly improved the treatment of CML. Imatinib (a BCR-ABL tyrosine kinase inhibitor) produces haematological and cytogenetic remissions across all phases of CML and is the present standard of care. Imatinib resistance occurs in a significant proportion of patients and mechanisms of resistance include BCR-ABL mutations and activation of alternate oncogenic pathways. Dasatinib is a novel, potent, multi-targeted oral kinase inhibitor. Preclinical and clinical investigations demonstrate that dasatinib effectively overcomes imatinib resistance and has further improved the treatment of CML. Dasatinib was recently approved by the FDA for use in Philadelphia-positive leukaemias in patients who are resistant or intolerant to imatinib.
AB - BCR-ABL, a constitutively active tyrosine kinase, causes chronic myeloid leukaemia (CML). Rational development of drugs targeting BCR-ABL has significantly improved the treatment of CML. Imatinib (a BCR-ABL tyrosine kinase inhibitor) produces haematological and cytogenetic remissions across all phases of CML and is the present standard of care. Imatinib resistance occurs in a significant proportion of patients and mechanisms of resistance include BCR-ABL mutations and activation of alternate oncogenic pathways. Dasatinib is a novel, potent, multi-targeted oral kinase inhibitor. Preclinical and clinical investigations demonstrate that dasatinib effectively overcomes imatinib resistance and has further improved the treatment of CML. Dasatinib was recently approved by the FDA for use in Philadelphia-positive leukaemias in patients who are resistant or intolerant to imatinib.
KW - Chronic myeloid leukaemia
KW - Dasatinib
KW - Imatinib intolerance
KW - Imatinib resistance
KW - Philadelphia chromosome-positive acute lymphoblastic leukaemia
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U2 - 10.1517/13543784.16.5.679
DO - 10.1517/13543784.16.5.679
M3 - Review article
C2 - 17461740
AN - SCOPUS:34248204301
SN - 1354-3784
VL - 16
SP - 679
EP - 687
JO - Expert Opinion on Investigational Drugs
JF - Expert Opinion on Investigational Drugs
IS - 5
ER -