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Identification of minor metabolites of 5-fluorocytosine in man by chemical ionization gas chromatography mass spectrometry.

A new minor metabolite of 5-fluorocytosine, 5-hydroxy-5-fluorocytosine, was found in the urinary gravel excreted by a patient being treated with this drug. A metabolite of 5-fluorocytosine in animals, alpha-fluoro-beta-alanine, was identified and quantitated in the urine of nine patients. In general, alpha-fluoro-beta-alanine represented 0.05--0.25% of the daily dose of 5-fluorocytosine, both for orally and intravenously administered drug. Minor metabolites have been implicated in the occasional toxicity observed in patients receiving 5-fluorocytosine.