Dasatinib for the treatment of Philadelphia chromosome-positive leukaemias.

Abstract	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.
Authors	Elias Jabbour, Jorge Cortes, Hagop Kantarjian
Journal	Expert opinion on investigational drugs (Expert Opin Investig Drugs) Vol. 16 Issue 5 Pg. 679-87 (May 2007) ISSN: 1744-7658 [Electronic] England
PMID	17461740 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)
Chemical References	Antineoplastic Agents Benzamides Piperazines Protein Kinase Inhibitors Pyrimidines Thiazoles Imatinib Mesylate Protein-Tyrosine Kinases Fusion Proteins, bcr-abl Dasatinib
Topics	Administration, Oral Animals Antineoplastic Agents (administration & dosage, therapeutic use) Benzamides Dasatinib Drug Resistance, Neoplasm Fusion Proteins, bcr-abl Humans Imatinib Mesylate Leukemia, Myelogenous, Chronic, BCR-ABL Positive (drug therapy, metabolism) Piperazines (therapeutic use) Protein Kinase Inhibitors (administration & dosage, therapeutic use) Protein-Tyrosine Kinases (antagonists & inhibitors, metabolism) Pyrimidines (administration & dosage, therapeutic use) Thiazoles (administration & dosage, therapeutic use) Treatment Outcome

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