Dasatinib for the treatment of Philadelphia chromosome-positive leukaemias

Elias Jabbour, Jorge Cortes, Hagop Kantarjian

Research output: Contribution to journalReview article

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.

Original languageEnglish (US)
Pages (from-to)679-687
Number of pages9
JournalExpert Opinion on Investigational Drugs
Volume16
Issue number5
DOIs
StatePublished - May 1 2007
Externally publishedYes

Fingerprint

Philadelphia Chromosome
Leukemia
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
Protein-Tyrosine Kinases
Leukemia, Myeloid, Chronic Phase
Therapeutics
Drug Delivery Systems
Standard of Care
Cytogenetics
Phosphotransferases
Mutation
Imatinib Mesylate
Dasatinib

Keywords

  • Chronic myeloid leukaemia
  • Dasatinib
  • Imatinib intolerance
  • Imatinib resistance
  • Philadelphia chromosome-positive acute lymphoblastic leukaemia

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

Cite this

Dasatinib for the treatment of Philadelphia chromosome-positive leukaemias. / Jabbour, Elias; Cortes, Jorge; Kantarjian, Hagop.

In: Expert Opinion on Investigational Drugs, Vol. 16, No. 5, 01.05.2007, p. 679-687.

Research output: Contribution to journalReview article

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