Imatinib mesylate has limited activity against the central nervous system involvement of Philadelphia chromosome-positive acute lymphoblastic leukaemia due to poor penetration into cerebrospinal fluid

Br J Haematol. 2002 Oct;119(1):106-8. doi: 10.1046/j.1365-2141.2002.03881.x.


A 32-year-old woman with relapsed Philadelphia chromosome-positive acute lymphoblastic leukaemia was treated with imatinib mesylate (formerly STI571), a selective inhibitor of BCR/ABL tyrosine kinase. Although the initial marrow response was good and stably maintained, she subsequently relapsed with extensive infiltration of leukaemic cells into the central nervous system (CNS). After controlling her CNS disease with additional intrathecal chemotherapy, we measured the concentration of imatinib in cerebrospinal fluid (CSF) and blood simultaneously. The concentration of imatinib in CSF was about 92-fold lower than that in blood. These results suggest that imatinib poorly penetrates the blood-brain barrier and has limited activity against CNS leukaemia.

Publication types

  • Case Reports

MeSH terms

  • Adult
  • Antineoplastic Agents / blood
  • Antineoplastic Agents / cerebrospinal fluid
  • Antineoplastic Agents / therapeutic use*
  • Benzamides
  • Blood-Brain Barrier
  • Central Nervous System Neoplasms / blood
  • Central Nervous System Neoplasms / cerebrospinal fluid
  • Central Nervous System Neoplasms / drug therapy*
  • Enzyme Inhibitors / blood
  • Enzyme Inhibitors / cerebrospinal fluid
  • Enzyme Inhibitors / therapeutic use*
  • Female
  • Humans
  • Imatinib Mesylate
  • Piperazines / blood
  • Piperazines / cerebrospinal fluid
  • Piperazines / therapeutic use*
  • Precursor Cell Lymphoblastic Leukemia-Lymphoma / blood
  • Precursor Cell Lymphoblastic Leukemia-Lymphoma / cerebrospinal fluid
  • Precursor Cell Lymphoblastic Leukemia-Lymphoma / drug therapy*
  • Pyrimidines / blood
  • Pyrimidines / cerebrospinal fluid
  • Pyrimidines / therapeutic use*


  • Antineoplastic Agents
  • Benzamides
  • Enzyme Inhibitors
  • Piperazines
  • Pyrimidines
  • Imatinib Mesylate