title: Low concentrations of STI571 in the cerebrospinal fluid: a case report.
abstract: 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.
authors.affiliation: Abteilung für Hämatologie & Onkologie, Universitätsklinik Innsbruck, Anichstrasse 35, A-6020 Innsbruck, Austria. andreas.petzer@uibk.ac.at
authors.forename: Andreas L
authors.initials: AL
authors.lastname: Petzer
authors.forename: Eberhard
authors.initials: E
authors.lastname: Gunsilius
authors.forename: Michael
authors.initials: M
authors.lastname: Hayes
authors.forename: Guenther
authors.initials: G
authors.lastname: Stockhammer
authors.forename: Hans C H
authors.initials: HC
authors.lastname: Duba
authors.forename: Folker
authors.initials: F
authors.lastname: Schneller
authors.forename: Kurt
authors.initials: K
authors.lastname: Grünewald
authors.forename: Werner
authors.initials: W
authors.lastname: Poewe
authors.forename: Guenther
authors.initials: G
authors.lastname: Gastl
mesh_terms: D000970:Antineoplastic Agents / Q000134:cerebrospinal fluid* / Q000627:therapeutic use; D001549:Benzamides; D001752:Blast Crisis / Q000134:cerebrospinal fluid* / Q000188:drug therapy; D004791:Enzyme Inhibitors / Q000134:cerebrospinal fluid / Q000627:therapeutic use; D005500:Follow-Up Studies; D006801:Humans; D000068877:Imatinib Mesylate; D015464:Leukemia, Myelogenous, Chronic, BCR-ABL Positive / Q000134:cerebrospinal fluid / Q000188:drug therapy / Q000473:pathology*; D008297:Male; D008875:Middle Aged; D010879:Piperazines / Q000134:cerebrospinal fluid* / Q000627:therapeutic use; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors; D011743:Pyrimidines / Q000134:cerebrospinal fluid* / Q000627:therapeutic use
chemical_list: D000970:Antineoplastic Agents; D001549:Benzamides; D004791:Enzyme Inhibitors; D010879:Piperazines; D011743:Pyrimidines; D000068877:Imatinib Mesylate; D011505:Protein-Tyrosine Kinases