Fluorouracil (5-FU)

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General information

Class/mechanism: Pyrimidine analog, antimetabolite, inhibitor of thymidylate synthase. Metabolized to 5-fluoro-2'-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP). FdUMP inhibits DNA synthesis by binding to thymidylate synthase and inhibiting production of thymidylate; FUTP interferes with RNA processing when it is mistakenly incorporated in place of uridine triphosphate (UTP).[1][2].
Route: IV
Extravasation: irritant

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.[1]

Patient safety

DPYD intermediate or poor metabolizers: Results in higher adverse reaction risk (severe, life-threatening, or fatal toxicities). No dosage has proven safe in poor metabolizers, and insufficient data are available to recommend a dosage in intermediate metabolizers. Withhold or discontinue in the presence of early-onset or unusually severe toxicity.[3]

EMA has recommended that patients should be tested for the lack of the enzyme dihydropyrimidine dehydrogenase (DPD) before starting cancer treatment with fluorouracil given by injection or infusion (drip) or with the related medicines, capecitabine and tegafur.

References

  1. Delaunoit T, Goldberg RM, Sargent DJ, Morton RF, Fuchs CS, Findlay BP, Thomas SP, Salim M, Schaefer PL, Stella PJ, Green E, Mailliard JA. Mortality associated with daily bolus 5-fluorouracil/leucovorin administered in combination with either irinotecan or oxaliplatin: results from Intergroup Trial N9741. Cancer. 2004 Nov 15;101(10):2170-6. link to original article PubMed

Diseases for which it is established (work in progress)

Diseases for which it is used

Diseases for which it was used

Patient drug information

History of changes in FDA indication

History of changes in EMA indication

  • 1977-12-16: EURD

History of changes in PMDA indication

  • 2013-12-20: New additional indication and a new dosage for the treatment of unresectable pancreatic cancer.
  • 2018-09-21: New indication and a new dosage for the treatment of small intestine cancer.
  • 2021-11-25: New indication and a new dosage for the treatment of esophageal cancer.

Also known as

  • Code name: Ro-2-9757
  • Generic names: 5 Fluorouracil, 5 FU, 5-FU, 5-fluoracilo, 5-fluorouracilo, 5-fluorouracyl, FU
  • Brand names:
Synonyms
Accusite Actino Hermal Adrucil Arumel Benton Biofur Carac Carebin
Carzonal Cinco-FU Cinkef-U Curacil Effcil Efudex Efurix Ezadex
Fauldfluor Fivocil Fivoflu Flacule Flonida Florac Fluhomer Fluolex
Fluoroplex Fluor-Uracil Fluoro-Uracile ICN Fluoro-Uracil ICN Fluorouracile Fluorouracilo Fluorourcil Fluoruracilo
Fluoxan Flurablastin Flurac Fluracedyl Fluracil Fluril Fluroblastin Fluroblastine
Ftoruracil Ftouracil Haemato-FU Ifacil Kang Ning Kecimeton Tatumi Killit Lunachol
Lunapon Natira U Neofluor O Fluor Oncofu Onkofluor Pentafu Pharmauracil
Phthoruracil Phtoruracil Ribofluor Rotianin Satelol Seco Uracil Tecflu Timadin
Triosules Uflahex Ulosagen Ulup Uraciflor Utoral Vaflu Vafu

References

  1. ↑ 1.0 1.1 Fluorouracil (5-FU) package insert (locally hosted backup)
  2. ↑ 5-FU pathway
  3. ↑ [1]
  4. ↑ Fluorouracil (5-FU) Package Insert
  5. ↑ Fluorouracil (5-FU) patient drug information (Chemocare)
  6. ↑ Fluorouracil (5-FU) patient drug information (UpToDate)
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