Drug intelligence / Profile preview

tegafur + uracil

Development stage
Phase 4
Lead developer
Taiho Pharmaceutical
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Tegafur + uracil is an oral chemotherapy combination used primarily for the treatment of colorectal (bowel) cancer. It consists of two components in a 1:4 molar ratio: tegafur, a prodrug that is converted in the liver to 5-fluorouracil (5-FU), and uracil, which inhibits dihydropyrimidine dehydrogenase (DPD), the enzyme responsible for degrading 5-FU. This inhibition increases and prolongs systemic exposure to active 5-FU, enhancing its cytotoxic effects on tumor cells. The active metabolites of 5-FU inhibit thymidylate synthase, disrupting DNA synthesis, and are incorporated into RNA, interfering with RNA function—both leading to tumor cell death. Tegafur + uracil was developed by Taiho Pharmaceutical as an alternative to intravenous fluorouracil therapy with improved oral bioavailability and reduced gastrointestinal toxicity[1][2][3][4][6].

Brand names
Uftoral
Other names
tegafur/uraciltegafur-uracil
02

Targets

DPYD (Dihydropyrimidine dehydrogenase)TS (Thymidylate synthase)

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