N1-(2-Tetrahydrofuryl)-5-fluorouracil (FT-207), a new antimetabolic anticancer agent synthesized in USSR, was studied on antimicrobial activity in vitro and distribution, excretion and metabolism in vivo.
The results obtained were as follows.
1) Antimicrobial activity
FT-207 showed fairly active against Micrococcus flavus ATCC 10240, Sarcina lutea PCI 1001, Staphylococcus epidermidis and Staphylococcus aureus 209 P, but in general the activity was inferior to that of 5-FU.
2) Distribution
By the intravenous administration of FT-207, 400mg/kg, in normal and AH-130 bearing rats, the concentration of FT-207 in serum and tissues maintained measurably until 16-24 hours.
On the other hand, the active substances (5-FU, etc.) from FT-207 detected at 1-4 hours and peaked at 4-16 hours in tissues.
3) Urinary excretion
FT-207 and its active substances were excreted in urine for a long time, and the recoveries of FT-207 for 48 hours in rats, mice and rabbits were 12-18%.
4) Metabolism
In normal and AH-130 bearing rats, the main active substance from FT-207 administrated intravenously was 5-FU.
