Tegafur is an antineoplastic agent used in combination with other anticancer medications to treat advanced gastric and colorectal cancers. It is a pyrimidine analogue used in combination therapies as an active chemotherapeutic agent in conjunction with DB09257 and DB03209, or along with DB00544 as DB09327.
- Mechanism
- Curator reviewed · 5 references
The transformation of 2'-deoxyurindylate (dUMP) to 2'-deoxythymidylate (dTMP) is essential in driving the synthesis of DNA and purines in cells. Thymidylate synthase catalyzes the conversion of dUMP to dTMP, which is a precursor of thymidine triphosphate (TTP), one of the four deoxyribonucleotides required for DNA synthesis. After administration into the body, tegafur is converted into the active antineoplastic metabolite, fluorouracil (5-FU). In tumour cells, 5-FU undergoes phosphorylation to form the active anabolites, including 5-fluorodeoxyuridine monophosphate (FdUMP). FdUMP and reduced folate are bound to thymidylate synthase leading to formation of a ternary complex which inhibits DNA synthesis. In addition, 5-fluorouridine-triphosphate (FUTP) is incorporated into RNA causing disruption of RNA functions.
- Primary indication
- Indicated for the treatment of cancer usually in combination with other biochemically modulating drugs.Curator reviewed · 1 structured indication
- Formula / weight
- C8H9FN2O3 · 200.169 g/mol (avg)
- First approval
- European Union, 2016
- Code names
- MJF-12264
- Brand names
Resolves to
WFWLQNSHRPWKFK-UHFFFAOYSA-NSMILESFC1=CN(C2CCCO2)C(=O)NC1=OWhat you can answer from here — as of September 24, 2025
Which drugs share a target with Tegafur, and which of those have an active Phase 3 trial?
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