Drug glossary Drug

Tegafur UFT, Ftorafur

A drug approved for colorectal cancer. It appears in 6 clinical trials.

Oral Thymidylate synthase DNA synthesis pathways
See its trials
United States FDA approved Since 2001
European Union EMA approved
Spain Hospital use Approved for colorectal cancer

What it is

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.

How it works

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

Common side effects

DiarrheaNauseaVomitingFatigueHand-foot syndromeStomatitisNeutropeniaAnemia

Not all are listed, and everyone experiences them differently. If you notice any, tell your care team.