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tegafur + folinic acid
- Development stage
- Unknown
- 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 + folinic acid is an oral combination chemotherapy regimen primarily used for the treatment of advanced or metastatic colorectal cancer. Tegafur is a prodrug that is converted in the body to fluorouracil (5-FU), a pyrimidine analogue that inhibits DNA synthesis by blocking thymidylate synthase. Folinic acid (also known as leucovorin or calcium folinate) enhances the cytotoxic effect of 5-FU by stabilizing its binding to thymidylate synthase, thereby increasing inhibition of DNA synthesis in tumor cells. This combination allows for effective oral administration and has demonstrated efficacy with acceptable toxicity profiles in clinical studies[2][3][6][7]. Folinic acid itself does not have direct anticancer activity but potentiates the effect of fluoropyrimidine drugs like tegafur.
- Brand names
- Uftoral
- Other names
- calcium folinateleucovorin5-formyl tetrahydrofolic acid
02
Targets
DHFR (Dihydrofolate reductase)TS (Thymidylate synthase)
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