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Title: In vitro partition of irinotecan (CPT-11) in human volunteer blood: the influence of concentration, gender and smoking
Authors: Dumez, Herlinde ×
Guetens, Gunther
De Boeck, Geert
Highley, Martin S
de Bruijn, Ernst
Van Oosterom, Allan
Maes, Robert A A #
Issue Date: Sep-2005
Series Title: Anti-cancer drugs vol:16 issue:8 pages:893-5
Abstract: We have performed in vitro incubations of blood from male and female volunteers, smokers and non-smokers, with irinotecan at a gradient of different concentrations in order to investigate changes of partition between red blood cells (RBCs), total plasma and the free fraction. Since irinotecan (CPT-11) is not metabolized in vitro, there is no data available on its active metabolite SN-38. After extraction and sample pre-treatment, a validated high-performance liquid chromatography method followed by fluorescence detection was used to determine the concentration of the drug in the different blood constituents. The partition ratio [the concentration in the erythrocytes divided by the concentration in plasma (E/P)] was calculated. The partition ratio of CPT-11 varied from 0.7 to 2.8, reflecting its relatively high affinity for the erythrocyte, probably because of its only moderate plasma protein binding (65%). The partition ratios increased significantly with higher whole-blood concentrations, favoring uptake in the erythrocytes when plasma protein binding is saturated. No gender difference was detected, but we found relatively more CPT-11 in the erythrocytes of non-smokers compared to smokers. The incorporation of drugs into the RBC pool may be important for transportation to tumor tissue and efficacy. Smoking can have a significant influence on drug partition in the blood.
ISSN: 0959-4973
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Experimental Oncology
Department of Oncology - miscellaneous
× corresponding author
# (joint) last author

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