Nilotinib: A novel Bcr-Abl tyrosine kinase inhibitor for the treatment of leukemias

Elias Jabbour, Samih El Ahdab, Jorge Cortes, Hagop Kantarjian

Research output: Contribution to journalArticle

Abstract

The successful introduction of the tyrosine kinase inhibitors has initiated a new era in the management of chronic myeloid leukemia (CML). Imatinib mesilate therapy has significantly improved the prognosis of CML. A minority of patients in chronic-phase CML - and more patients in advanced phases - are resistant to imatinib, or develop resistance during treatment. This is attributed, in 40 - 50% of cases, to the development of mutations in the Bcr-Abl tyrosine kinase domain that impair imatinib binding. Nilotinib (Tasigna®) is a novel potent selective oral kinase inhibitor. Preclinical and clinical investigations demonstrate nilotinib effectively overcomes imatinib resistance, and has induced high rates of hematologic and cytogenetic responses in CML post imatinib failure.

Original languageEnglish (US)
Pages (from-to)1127-1136
Number of pages10
JournalExpert Opinion on Investigational Drugs
Volume17
Issue number7
DOIs
StatePublished - Jul 1 2008
Externally publishedYes

Fingerprint

bcr-abl Fusion Proteins
Leukemia
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
Leukemia, Myeloid, Chronic Phase
Therapeutics
Mesylates
Cytogenetics
Protein-Tyrosine Kinases
Phosphotransferases
4-methyl-N-(3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl)-3-((4-pyridin-3-ylpyrimidin-2-yl)amino)benzamide
Imatinib Mesylate
Mutation

Keywords

  • ALL
  • CML
  • Imatinib
  • Intolerance
  • Nilotinib
  • Ph-positive
  • Resistance

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

Cite this

Nilotinib : A novel Bcr-Abl tyrosine kinase inhibitor for the treatment of leukemias. / Jabbour, Elias; El Ahdab, Samih; Cortes, Jorge; Kantarjian, Hagop.

In: Expert Opinion on Investigational Drugs, Vol. 17, No. 7, 01.07.2008, p. 1127-1136.

Research output: Contribution to journalArticle

Jabbour, Elias ; El Ahdab, Samih ; Cortes, Jorge ; Kantarjian, Hagop. / Nilotinib : A novel Bcr-Abl tyrosine kinase inhibitor for the treatment of leukemias. In: Expert Opinion on Investigational Drugs. 2008 ; Vol. 17, No. 7. pp. 1127-1136.
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