Low concentrations of STI571 in the cerebrospinal fluid: a case report

Br J Haematol. 2002 Jun;117(3):623-5. doi: 10.1046/j.1365-2141.2002.03523.x.


We report a 53-year-old man with lymphoid blast crisis of Ph+ chronic myeloid leukaemia who was treated with STI571, a selective inhibitor of the enzymatic activity of BCR-ABL. He responded excellently to STI571 (600 mg/d), obtaining a complete cytogenetic remission after 3 months of therapy. Although remission in the bone marrow was sustained, the patient developed an isolated central nervous system relapse. Subsequent analyses of STI571 concentrations in the cerebrospinal fluid (CSF) revealed 2-log lower CSF levels of STI571 than corresponding plasma levels. These are the first data demonstrating a low penetration of orally administered STI571 into the CSF in humans.

Publication types

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

MeSH terms

  • Antineoplastic Agents / cerebrospinal fluid*
  • Antineoplastic Agents / therapeutic use
  • Benzamides
  • Blast Crisis / cerebrospinal fluid*
  • Blast Crisis / drug therapy
  • Enzyme Inhibitors / cerebrospinal fluid
  • Enzyme Inhibitors / therapeutic use
  • Follow-Up Studies
  • Humans
  • Imatinib Mesylate
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive / cerebrospinal fluid
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive / drug therapy
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive / pathology*
  • Male
  • Middle Aged
  • Piperazines / cerebrospinal fluid*
  • Piperazines / therapeutic use
  • Protein-Tyrosine Kinases / antagonists & inhibitors
  • Pyrimidines / cerebrospinal fluid*
  • Pyrimidines / therapeutic use


  • Antineoplastic Agents
  • Benzamides
  • Enzyme Inhibitors
  • Piperazines
  • Pyrimidines
  • Imatinib Mesylate
  • Protein-Tyrosine Kinases