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Tegafur

Published: July 26, 2026Updated: August 20, 2026

Tegafur is an antineoplastic agent classified as a fluoropyrimidine analog that serves as a prodrug for 5-fluorouracil (5-FU). It is used in the treatment of various solid tumors, including cancers of the gastrointestinal tract. The drug works by being metabolized in the body to its active form, which inhibits DNA and RNA synthesis in rapidly dividing cancer cells.

Quick summary

Tegafur is a chemotherapy drug (fluoropyrimidine prodrug) used to treat various solid tumors by interfering with cancer cell DNA and RNA production.

Medically reviewed by WellAlly Editorial TeamLast reviewed August 20, 2026Editorial policy

Key facts at a glance

ATC
L01BC03
RxNorm
4582
Generic
Tegafur
Class
atc-l01
Brands
—
Availability
rx
Lactation
unknown
Routes
oral
Forms
capsule
Regions
US, EU, CN, JP
Monitoring
—

This page is for informational purposes only.

Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.

Tegafur is used to treat various solid malignancies, including colorectal cancer, gastric (stomach) cancer, and sometimes breast cancer. It may be used alone or in combination with other chemotherapy agents depending on the specific cancer type and treatment protocol.

As a prodrug, tegafur is converted in the body to 5-fluorouracil (5-FU), its active form. The drug inhibits thymidylate synthase, an enzyme essential for DNA synthesis, and also incorporates into RNA and DNA molecules, disrupting normal cellular function and causing cell death in rapidly dividing cancer cells.

Tegafur is a cytotoxic chemotherapy agent and should only be administered under the supervision of an oncologist. Common side effects may include bone marrow suppression, gastrointestinal disturbances, and potential toxicity to rapidly dividing normal cells. Patient monitoring for hematologic and hepatic function is typically required during treatment.

Official drug label

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This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.

Medical Disclaimer

This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.

If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.

Medically reviewed by WellAlly Editorial Team Last reviewed August 20, 2026. · Read our editorial policy