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5-Fluorouracil

Deterministic view of the source YAML entity. Clinical authority remains with the cited source IDs and reviewer sign-off state.

IDDRUG-5-FLUOROURACIL
TypeDrug
Aliases
5-FU5-ФторурацилAdrucilCaracEfudexFluorouracil
Statusreviewed 2026-04-26 | pending_clinical_signoff
DiseasesDIS-ANAL-SCC DIS-CRC DIS-ESOPHAGEAL DIS-GASTRIC DIS-HNSCC DIS-PDAC
SourcesSRC-ESMO-COLON-2024 SRC-NCCN-COLON-2025

Drug Facts

ClassAntimetabolite (fluoropyrimidine, pyrimidine analog)
MechanismPyrimidine analog. Intracellularly converted to FdUMP, FdUTP, and FUTP. FdUMP forms a stable ternary complex with thymidylate synthase (TS) + reduced folate (leucovorin), depleting dTMP and blocking DNA synthesis. FUTP misincorporation into RNA disrupts pre-mRNA processing; FdUTP misincorporation into DNA produces strand breaks. Backbone of FOLFOX, FOLFIRI, FOLFIRINOX, FLOT, and capecitabine-bridged regimens. Bolus and continuous-infusion (CIV) schedules differ in toxicity profile (more myelosuppression with bolus, more mucositis/HFS with CIV).
Typical dosingFOLFOX (mFOLFOX6): 400 mg/m² IV bolus day 1 + 2400 mg/m² IV CIV over 46 h every 14 d. FOLFIRI: 400 mg/m² IV bolus day 1 + 2400 mg/m² IV CIV over 46 h q14d. FOLFIRINOX: 400 mg/m² IV bolus + 2400 mg/m² CIV over 46 h q14d. FLOT: 2600 mg/m² IV CIV over 24 h day 1 q14d. Bolus 5-FU/LV (Mayo Clinic, adjuvant legacy): 425 mg/m² IV bolus days 1-5 every 28 d. Continuous infusion (de Gramont): 400 mg/m² IV bolus + 600 mg/m² CIV over 22 h days 1-2 q14d. Head & neck CRT: 1000 mg/m² CIV days 1-4 with cisplatin.
Ukraine registeredTrue
NSZU reimbursedTrue
Ukraine last verified2026-04-27

Warnings

Notes

DPYD genotyping (variants *2A, *13, c.2846A>T, HapB3) recommended before first dose per CPIC guidelines and EMA 2020 recommendation (NCCN colon v2.2025, pretreatment section). Bolus-only schedules largely superseded by infusional + LV in modern adjuvant. Coronary spasm: hold drug, urgent ECG; switch to raltitrexed if confirmed. Uridine triacetate (Vistogard) is the antidote for severe overdose or early-onset toxicity (≤96 h post-exposure).

Used By

Regimens