Target spectrum of the BCR-ABL inhibitors imatinib, nilotinib and dasatinib

Leuk Lymphoma. 2008 Apr;49(4):615-9. doi: 10.1080/10428190801896103.

Abstract

Following the initial success of imatinib as frontline therapy for chronic myeloid leukemia (CML), several second-generation therapeutics have been developed with increased potency and the ability to inhibit the majority of imatinib-resistant mutations. Here, we review the current knowledge about the target specificity of the two new inhibitors nilotinib and dasatinib in comparison to imatinib, including the recent large-scale chemical proteomics screens.

Publication types

  • Review

MeSH terms

  • Benzamides
  • Dasatinib
  • Drug Delivery Systems / methods*
  • Fusion Proteins, bcr-abl / antagonists & inhibitors*
  • Humans
  • Imatinib Mesylate
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive / drug therapy
  • Piperazines
  • Protein Kinase Inhibitors / therapeutic use*
  • Pyrimidines
  • Thiazoles

Substances

  • 4-methyl-N-(3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl)-3-((4-pyridin-3-ylpyrimidin-2-yl)amino)benzamide
  • Benzamides
  • Piperazines
  • Protein Kinase Inhibitors
  • Pyrimidines
  • Thiazoles
  • Imatinib Mesylate
  • Fusion Proteins, bcr-abl
  • Dasatinib