Difference in histologic effects on the liver with regard to the route of administration of fluorinated pyrimidines in gastric cancer patients

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Radioautography (ARG) using ^3H-Tegafur (^3H-FT) and ^3H-UFT in tumorbearing mice reealed incorporation of these drugs into tumor cells as well as liver parenchymal cells. Oral administration of FT (>10g) or UFT (>7.2g) in gastric cancer patients resulted in regressive changes in the gastric carcinomas (GC) as well as fatty change and focal necrosis in the liver. The histologic effects of i.v. 5-fluorouracil (FU,>2.5g) on both GC and liver were less marked than those of oral FU (>1.2g). ARG experiments showed that 0.1<micrn>g/g actinomycin D (AD) increased the uptake of ^3H-FU and ^3H-FT into murine tumor cells. A combination of i.v. AD (>0.5mg) and i.v. FU (>1.5g) in gastric cancer patients had treater histologic effects on GC, but the same grade of effects on the livr as i.v. FU only.