A PRODRUG FORM OF 5-FLUOROURACIL AND A METHOD OF TREATMENT OF CANCER

摘要

A prodrug form of 5-fluorouracil selected from the group consisting of optionally substituted 1-alkoxycarbonyl, 3-acyl, 1-acyloxyalkyl and 3-acyloxyalkyl derivatives of 5-fluorouracil having a) a partition coefficient between octanol and aqueous buffer (pH 7.4) greater than 0.5, b) a solubility in water at pH 7.4 greater than 0.05 M (at 20 DEG C), c) a susceptibility to undergo rapid enzymatic cleavage in vivo to regenerate 5-fluorouracil in quantitative amounts with the simultaneous release of a non-toxic pro-moiety, and d) a stability in aqueous solution to such an extent that no significant degradation occurs before the occurrence of absorption across the rectal biomembrane, has an improved bioavailability upon rectal administration. The compounds are highly useful in the treatment of cancer and can be used orally as well as rectally.