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

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Abstract
A new minor metabolite of 5‐fluorocytosine, 6‐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, α‐fluoro‐β‐alanine, was identified and quantitated in the urine of nine patients. In general, α‐fluoro‐β‐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.