Takayama Nobuyuki, Sato Norihide, O'Brien Stephen G, Ikeda Yasuo, Okamoto Shin-Ichiro
Division of Haematology, Department of Internal Medicine, Keio University School of Medicine, Tokyo, Japan.
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.
一名32岁复发的费城染色体阳性急性淋巴细胞白血病女性患者接受了甲磺酸伊马替尼（原STI571）治疗，该药是一种BCR/ABL酪氨酸激酶的选择性抑制剂。尽管最初骨髓反应良好且得以稳定维持，但她随后复发，白血病细胞广泛浸润中枢神经系统（CNS）。在用额外的鞘内化疗控制其CNS疾病后，我们同时测量了脑脊液（CSF）和血液中伊马替尼的浓度。CSF中伊马替尼的浓度比血液中的低约92倍。这些结果表明，伊马替尼难以穿透血脑屏障，对CNS白血病的活性有限。
