Galocitabine (Neofrutulon), a thymidylate synthase inhibitor, is used potentially for the treatment of cancer.

We performed 4-week toxicity studies of capecitabine (N(4)-pentyloxycarbonyl-5'-deoxy-5-fluorouridine), galocitabine (trimethoxybenzyl-5'-deoxy-5-fluorocytidine), 4 different fluoropyrimidine carbamate analogs. Four-week toxicity data for capecitabine in rats and mice were also obtained for comparison. Capecitabine, galocitabine, butyl, and isopentyl analogs showed similar toxicities in hematopoietic and intestinal organs at 1.0 mmol/kg. These compounds showed slight toxicity at 0.5 mmol/kg and no toxicity at 0.1 mmol/kg. [1]