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Title: Tegafur  
Author: World Heritage Encyclopedia
Language: English
Subject: Tegafur/gimeracil/oteracil, Capecitabine, Chemotherapy, Cell-cycle nonspecific antineoplastic agents, Hazardous drugs
Publisher: World Heritage Encyclopedia


Systematic (IUPAC) name
Clinical data
Pregnancy cat.
Legal status
Routes Oral
Pharmacokinetic data
Half-life 3.9-11 hours
CAS number  YesY
ATC code L01
ChemSpider  YesY
Synonyms 5-fluoro-1-(oxolan-2-yl)pyrimidine-2,4-dione
Chemical data
Formula C8H9FN2O3 
Mol. mass 200.16 g/mol

Tegafur (INN, BAN, USAN) is a chemotherapeutic fluorouracil prodrug used in the treatment of cancers. It is a component of the combination drug tegafur/uracil. When metabolised, it becomes 5-fluorouracil.[1]

Medical uses

As a prodrug to 5-FU it is used in the treatment of the following cancers:[2]

It is often given in combination with drugs that alter its bioavailability and toxicity such as gimeracil, oteracil or uracil.[2] These agents achieve this by inhibiting the enzyme dihydropyrimidine dehydrogenase (uracil/gimeracil) or orotate phosphoribosyltransferase (oteracil).[2]

Adverse effects

The major side effects of tegafur are similar to fluorouracil and include myelosuppression, central neurotoxicity and gastrointestinal toxicity (especially diarrhoea).[2] Gastrointestinal toxicity is the dose-limiting side effect of tegafur.[2] Central neurotoxicity is more common with tegafur than with fluorouracil.[2]

Mechanism of action

It is a prodrug to fluorouracil which is a thymidylate synthase inhibitor.[2]


It is metabolised into fluorouracil by CYP2A6.[4][5]

Interactive pathway map

Click on genes, proteins and metabolites below to link to respective articles. [§ 1]

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Fluorouracil (5-FU) Activity edit
  1. ^ The interactive pathway map can be edited at WikiPathways: "FluoropyrimidineActivity_WP1601". 

See also


  1. ^ El Sayed, YM; Sadée, W (1983). "Metabolic activation of R,S-1-(tetrahydro-2-furanyl)-5-fluorouracil (ftorafur) to 5-fluorouracil by soluble enzymes". Cancer Research 43 (9): 4039–44.  
  2. ^ a b c d e f g Sweetman, S, ed. (14 November 2011). "Martindale: The Complete Drug Reference". Pharmaceutical Press. Retrieved 12 February 2014. 
  3. ^ Ishikawa, T (14 May 2008). "Chemotherapy with enteric-coated tegafur/uracil for advanced hepatocellular carcinoma." (PDF). World Journal of Gastroenterology : WJG 14 (18): 2797–2801.  
  4. ^ Nakayama, T; Noguchi, S (January 2010). "Therapeutic usefulness of postoperative adjuvant chemotherapy with Tegafur-Uracil (UFT) in patients with breast cancer: focus on the results of clinical studies in Japan." (PDF). The Oncologist 15 (1): 26–36.  
  5. ^ Matt, P; van Zwieten-Boot, B; Calvo Rojas, G; Ter Hofstede, H; Garcia-Carbonero, R; Camarero, J; Abadie, E; Pignatti, F (October 2011). "The European Medicines Agency review of Tegafur/Gimeracil/Oteracil (Teysuno™) for the treatment of advanced gastric cancer when given in combination with cisplatin: summary of the Scientific Assessment of the Committee for medicinal products for human use (CHMP)." (PDF). The Oncologist 16 (10): 1451–1457.  

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