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Fluorouracil (5-FU)

EMD Serono Research & Development Institute, Inc. · Phase 3 active Small molecule

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

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 nameFluorouracil (5-FU)
Also known as5-FU, Adrucil, (5-FU), 5-Fluorouracil, Efudex
SponsorEMD Serono Research & Development Institute, Inc.
Drug classAntimetabolite
TargetThymidylate synthase
ModalitySmall molecule
Therapeutic areaOncology
PhasePhase 3

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. These dual mechanisms make it effective against rapidly dividing cancer cells.

Approved indications

Common side effects

Key clinical trials

Primary sources

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