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Passage of 5'‐dFUrd and its metabolites 5‐FU and 5‐FUH 2 to CSF in a clinical Phase 1 study
Author(s) -
Heier M. S.,
Heintz R.,
Fosså S. D.
Publication year - 1986
Publication title -
acta neurologica scandinavica
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.967
H-Index - 95
eISSN - 1600-0404
pISSN - 0001-6314
DOI - 10.1111/j.1600-0404.1986.tb07862.x
Subject(s) - plasma concentration , pharmacology , chemistry , toxicity , medicine , chromatography
— Lumbar puncture was performed on eight patients in a clinical Phase 1 study of doxifluridine (5′‐dFUrd). 5′‐dFUrd, 5'FU, and 5‐FUH 2 were shown to cross the bloodbrain barrier to CSF. The maximal concentrations of 5′‐dFUrd and 5‐FUH 2 were about 1–3% of the maximal concentrations in plasma, and were reached within 1–4 h after the end of iv infusion of 5′‐dFUrd. 5‐FUH 2 showed a marked increase in CSF between 3 and 4 h to about 40–60% of the maximal plasma concentration in 5 of the patients, indicating a possible further increase after 4 h. The relationship between the concentrations of 5′‐dFUrd and its metabolites in the CSF, and CNS toxicity is discussed.