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5Fluorouracil

University of Nebraska · FDA-approved active Small molecule

5-Fluorouracil is a pyrimidine analog that inhibits thymidylate synthase and gets incorporated into RNA and DNA, disrupting nucleotide synthesis and causing cancer cell death.

5-Fluorouracil is a pyrimidine analog that inhibits thymidylate synthase and gets incorporated into RNA and DNA, disrupting nucleotide synthesis and causing cancer cell death. Used for Colorectal cancer, Breast cancer, Gastric cancer.

At a glance

Generic name5Fluorouracil
Also known asAdrucil, 5-FU, Efudix, 5Fu, Adrucil®
SponsorUniversity of Nebraska
Drug classAntimetabolite
TargetThymidylate synthase
ModalitySmall molecule
Therapeutic areaOncology
PhaseFDA-approved

Mechanism of action

5-FU is converted intracellularly to active metabolites that inhibit thymidylate synthase, blocking dTMP synthesis and DNA replication. It also incorporates into RNA, disrupting protein synthesis. This dual mechanism makes it effective against rapidly dividing cancer cells.

Approved indications

Common side effects

Key clinical trials

Primary sources

Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.

SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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