The fluoropyrimidine antimetabolites were employed in a wide range of neoplastic diseases. In particular, 5-fluorouracil in association with other chemotherapeutic agents, or biochemical modulators was successfully used in the treatment of colorectal, gastric, breast, head and neck cancers. With this type of chemotherapy, a response rate < or = 20% was obtained in gastrointestinal tumors, without a statistically significant impact on the overall survival. UFT is a combination of tegafur an uracil, which has the important advantage of an improved oral bioavailability, if we compare it with 5-fluorouracil. Uracil, avoiding the fluoropyrimidine degradation inside the tumor cells, increases the permanence of the metabolically active fluoropyrimidine into the target cell, so having an improvement in the therapeutic activity. A very large spectrum of cancers were treated with this molecule. In particular, a response rate in the range of 20-40% was observed in the treatment of patients with metastatic colorectal cancer. Phase III trials are ongoing to evaluate the advantage on 5-FU of this new fluoropyrimidine in terms of clinical efficacy, and quality of life, considering the possibility to administer it orally.