Fluorouracil (5-FU)

==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). Fluorouracil (5-FU) package insert (locally hosted backup)5-FU pathway.
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 or the prescribing information. 
==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.
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===
#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 EuroPMC
==Diseases for which it is established (work in progress)==
*Hepatocellular carcinoma
*Nasopharyngeal carcinoma
==Diseases for which it is used==
*Anal cancer
*Bladder cancer
*Breast cancer
**Breast cancer, HER2-positive
**Breast cancer, triple negative
*Carcinoma of unknown primary
*Cervical cancer
*Cholangiocarcinoma
*Colorectal cancer
**Colon cancer
**Rectal cancer
*Esophageal cancer
**Esophageal adenocarcinoma
**Esophageal squamous cell carcinoma
*Gallbladder cancer
*Gastric cancer
*Head and neck cancer
*Hepatoblastoma
*Neuroendocrine tumor
*Pancreatic cancer
*Pancreatic NET
*Penile cancer
*Small bowel adenocarcinoma
==Diseases for which it was used==
*Diffuse large B-cell lymphoma
*Ovarian cancer
*Prostate cancer
==Patient drug information==
*Fluorouracil (5-FU) Package InsertFluorouracil (5-FU) Package Insert
*Fluorouracil (5-FU) patient drug information (Chemocare)Fluorouracil (5-FU) patient drug information (Chemocare)
*Fluorouracil (5-FU) patient drug information (UpToDate)Fluorouracil (5-FU) patient drug information (UpToDate)
==History of changes in FDA indication==
*1962-04-25: Initial FDA approval
*Uncertain date: Approved for the treatment of patients with adenocarcinoma of the colon and rectum; adenocarcinoma of the breast; gastric adenocarcinoma; and pancreatic adenocarcinoma. (No supporting studies are cited)
==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 	Synonyms 	Synonyms 	Synonyms 	Synonyms 	Synonyms 	Synonyms 	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==
Category:Drugs
Category:Intravenous medications
Category:Topical medications
Category:Irritant
Category:Fluoropyrimidines
Category:Anal cancer medications
Category:Bladder cancer medications
Category:Breast cancer medications
Category:Carcinoma of unknown primary medications 
Category:Cervical cancer medications
Category:Cholangiocarcinoma medications
Category:Colon cancer medications
Category:Colorectal cancer medications
Category:Esophageal adenocarcinoma medications
Category:Esophageal cancer medications
Category:Esophageal squamous cell carcinoma medications
Category:Gallbladder cancer medications
Category:Gastric cancer medications
Category:Head and neck cancer medications
Category:Hepatoblastoma medications
Category:Hepatocellular carcinoma medications
Category:Nasopharyngeal carcinoma medications
Category:Neuroendocrine tumor medications
Category:Pancreatic cancer medications 
Category:Pancreatic NET medications
Category:Penile cancer medications 
Category:Rectal cancer medications
Category:Small bowel adenocarcinoma medications
Category:Diffuse large B-cell lymphoma medications (historic)
Category:Ovarian cancer medications (historic)
Category:Prostate cancer medications (historic)
Category:FDA approved in 1962
Category:EMA approved in 1977
Category:WHO Essential Cancer Medicine