EXCRETION OF 1-HEXYLCARBAMOYL-5-FLUOROURACIL IN URINE OF MICE

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Excretion and metabolites in urine and feces of mice after oral administration of 1-hexylcarbamoyl-5-fluorouracil-6-^<14>C (^<14>C-HCFU) or 5-fluorouracil-6-^<14>C (^<14>C-FU) were examined. After oral administration, about 90% of ^<14>C-HCFU was excreted in urine within 48 h but not in feces. Major radioactive compounds in urine were 1-(3-carboxypropylcarbamoyl)-5-fluorouracil (CPRFU), FU, 5,6-dihydro-5-fluorouracil (DHFU) and α-fluoro-β-alanine (FBAL). Excretion ratio of these metabolites within 48 h was 13.5,32.5,20.2 and 23.9%, respectively, CPRFU and FU were rapidly excreted in urine after ^<14>C-HCFU administration followed by DHFU and FBAL. Excretion of the latter two degradation products of FU was slower. On the other hand, major metabolites in urine after ^<14>C-FU administration were DHFU and FBAL, but intact FU was slightly excreted. Excretion ratio of FU, DHFU and FBAL within 48 h was 4.8,58.1 and 28.2%, respectively.
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