Tegafur (UFT (when combined with uracil), Ftorafur)
Other Medications · Approved since 2001
Description
Tegafur is an oral fluoropyrimidine antimetabolite chemotherapy agent used in the treatment of colorectal cancer, particularly as adjuvant therapy following surgical resection. It is commonly formulated in combination with uracil (as UFT - uracil-tegafur) and administered with leucovorin to enhance efficacy. Tegafur serves as a prodrug that is converted to 5-fluorouracil (5-FU) in the body, providing sustained release of the active cytotoxic agent while potentially reducing some systemic toxicities associated with intravenous 5-FU administration.
Mechanism of Action
Tegafur is metabolized to 5-fluorouracil through cytochrome P450 enzymes, primarily in the liver and tumor tissues. The active metabolite 5-FU inhibits thymidylate synthase, blocking DNA synthesis and repair, while also incorporating into RNA to disrupt protein synthesis. The co-administered uracil competitively inhibits dihydropyrimidine dehydrogenase, the enzyme responsible for 5-FU degradation, thereby prolonging the half-life and enhancing the antitumor activity of the converted 5-FU.
Molecular Targets
Side Effects
Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.