STI571: an inhibitor of the BCR-ABL tyrosine kinase for the treatment of chronic myelogenous leukaemia

Lancet Oncol. 2000 Dec:1:207-11. doi: 10.1016/s1470-2045(00)00149-2.

Abstract

The deregulated tyrosine kinase activity of the BCR-ABL fusion protein has been established as the causative molecular event in chronic myelogenous leukaemia. Thus, the BCR-ABL tyrosine kinase is an ideal target for pharmacological inhibition. STI571 (formerly CGP57148B), is an ABL-specific inhibitor of tyrosine kinase that, in preclinical studies, selectively killed BCR-ABL-containing cells in vitro and in vivo. Clinical studies have shown the potential of this specifically targeted therapy, and STI571 is emerging as an important new therapeutic agent for chronic myelogenous leukaemia.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use
  • Benzamides
  • Clinical Trials, Phase I as Topic
  • Disease Models, Animal
  • Enzyme Inhibitors / pharmacology*
  • Enzyme Inhibitors / therapeutic use
  • Fusion Proteins, bcr-abl / drug effects*
  • Fusion Proteins, bcr-abl / metabolism
  • Humans
  • Imatinib Mesylate
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive / diagnosis
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive / drug therapy*
  • Piperazines / pharmacology*
  • Piperazines / therapeutic use
  • Protein-Tyrosine Kinases / antagonists & inhibitors*
  • Pyrimidines / pharmacology*
  • Pyrimidines / therapeutic use
  • Sensitivity and Specificity

Substances

  • Antineoplastic Agents
  • Benzamides
  • Enzyme Inhibitors
  • Piperazines
  • Pyrimidines
  • Imatinib Mesylate
  • Protein-Tyrosine Kinases
  • Fusion Proteins, bcr-abl