In vitro drug resistance to imatinib and mutation of ABL gene in childhood Philadelphia chromosome-positive (Ph+) acute lymphoblastic leukemia

Leuk Lymphoma. 2005 Feb;46(2):273-6. doi: 10.1080/10428190400011609.

Abstract

Imatinib, the ABL kinase inhibitor, is used not only for Philadelphia chromosome-positive (Ph + ) chronic myelogenous leukemia, but also for Ph + acute lymphoblastic leukemia (ALL), although resistance to the drug tends to develop in an early stage of the clinical course. We describe a childhood refractory Ph + ALL patient in whom progressive resistance to imatinib was correlated with the appearance of a mutation in the BCR-ABL kinase domain and in vitro drug resistance to imatinib as determined by the methyl-thiazol-tetrazolium (MTT) assay. A missense mutation of T to C (Y253H) of the ABL gene was identified in the resistant clone, suggesting that this mutation may play an etiological role in the rapid loss of drug sensitivity.

Publication types

  • Case Reports
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Benzamides
  • Cell Survival / drug effects
  • Child
  • Drug Resistance, Neoplasm / genetics*
  • Genes, abl / genetics*
  • Genes, abl / physiology
  • Humans
  • Imatinib Mesylate
  • Male
  • Mutation, Missense*
  • Philadelphia Chromosome
  • Piperazines / pharmacology
  • Piperazines / therapeutic use*
  • Precursor Cell Lymphoblastic Leukemia-Lymphoma / diagnosis
  • Precursor Cell Lymphoblastic Leukemia-Lymphoma / drug therapy*
  • Precursor Cell Lymphoblastic Leukemia-Lymphoma / genetics
  • Pyrimidines / pharmacology
  • Pyrimidines / therapeutic use*

Substances

  • Benzamides
  • Piperazines
  • Pyrimidines
  • Imatinib Mesylate