Absorption and Excretion of a New Oral Antitumor Drug, 1-Hexylcarbamoyl-5-Fluorouracil (HCFU), in Cancer Patients

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Abstract
Absorption and excretion of a new antitumor drug, 1-hexylcarbamoyl-5-fluorouracil (HCFU), in cancer patients were investigated during the term of its Phase I study. HCFU was administered per os to the patients at a dose of 5 to 21 n (n = 1 mg/kg/day). Serum and urine concentrations of 5-fluorouracil (5-FU) and of HCFU and its intermediates which consisted of 1-(5-hydroxyhexylcar-bamoyl)-5-FU (HHCFU), 1-(5-oxohexylcarbamoyl)-5-FU (OHCFU), 1-carboxypentylcarbamoyl-5-FU (CPEFU) and l-carboxypropylcarbamoyl-5-FU (CPRFU) were measured by a bioassay method using an indicator bacterium. Their maximum serum levels were found 2 to 4 hr after administration, and the drugs continued to be present in the serum for 9 hr. The concentrations were dose related, and serum 5-FU levels reached more than 0.1 μg/ml at doses of more than 5 n and remained at that level for 2 to 4 hr. Approximately 15% of the administered HCFU was excreted in the urine as 5-FU, HCFU and its intermediates, and about half of these products was 5-FU.

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