Tegafur[edit]

Tegafur is a chemotherapeutic agent and a prodrug to 5-FU, used in the treatment of various cancers. It is metabolized into 5-FU by CYP2A6, exerting its anticancer effects.

Overview[edit]

Classification: Chemotherapeutic agent, Fluorouracil prodrug
Specialty: Oncology
Mechanism of Action: Converted to 5-fluorouracil, inhibits thymidylate synthase
Administration: Oral
Metabolism: Primarily in the liver to 5-FU by CYP2A6

Medical Uses[edit]

As a prodrug to 5-FU, Tegafur is used in the treatment of the following cancers:^[1]

Stomach (when combined with gimeracil and oteracil)
Breast (with uracil)
Gallbladder
Lung (specifically adenocarcinoma, typically with uracil)
Colorectal (usually when combined with gimeracil and oteracil)
Head and neck
Liver (with uracil)^[2]
Pancreatic

It is often given in combination with drugs that alter its bioavailability and toxicity such as gimeracil, oteracil, or uracil.^[1] These agents achieve this by inhibiting the enzyme dihydropyrimidine dehydrogenase (uracil/gimeracil) or orotate phosphoribosyltransferase (oteracil).^[1]

Mechanism of Action[edit]

Tegafur is a prodrug to fluorouracil which is a thymidylate synthase inhibitor.^[1]

Pharmacokinetics[edit]

Tegafur is metabolized into fluorouracil by CYP2A6.^[3]^[4]

Adverse Effects[edit]

The major side effects of tegafur are similar to fluorouracil and include myelosuppression, central neurotoxicity, and gastrointestinal toxicity (especially diarrhea).^[1] Gastrointestinal toxicity is the dose-limiting side effect of tegafur.^[1] Central neurotoxicity is more common with tegafur than with fluorouracil.^[1]

Interactive Pathway Map[edit]

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

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|{{{bSize}}}px|alt=Fluorouracil (5-FU) Activity edit]]

Fluorouracil (5-FU) Activity edit

↑ ^1.0 ^1.1 ^1.2 ^1.3 ^1.4 ^1.5 ^1.6 Martindale: The Complete Drug Reference(link). Pharmaceutical Press.14 November 2011.
↑ Ishikawa, T."Chemotherapy with enteric-coated tegafur/uracil for advanced hepatocellular carcinoma.".World Journal of Gastroenterology : WJG.14 May 2008;14(18)
2797-2801.doi:10.3748/wjg.14.2797.PMID:18473401.PMC:2710718.Full text.
↑ Nakayama, T."Therapeutic usefulness of postoperative adjuvant chemotherapy with Tegafur-Uracil (UFT) in patients with breast cancer: focus on the results of clinical studies in Japan.".The Oncologist.January 2010;15(1)
26-36.doi:10.1634/theoncologist.2009-0255.PMID:20080863.PMC:3227888.Full text.
↑ Matt, P."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).".The Oncologist.October 2011;16(10)
1451-1457.doi:10.1634/theoncologist.2011-0224.PMID:21963999.PMC:3228070.Full text.

Conclusion[edit]

Tegafur is a crucial chemotherapeutic agent used in the treatment of various cancers. Its effectiveness often relies on combination with other drugs that modulate its bioavailability and toxicity. Understanding its pharmacokinetics, mechanisms of action, and potential adverse effects is essential for healthcare professionals in oncology to optimize patient care and improve treatment outcomes.

References[edit]

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[MD-1] 1.0 ^1.1 ^1.2 ^1.3 ^1.4 ^1.5 ^1.6 Martindale: The Complete Drug Reference(link). Pharmaceutical Press.14 November 2011.

[2] Ishikawa, T."Chemotherapy with enteric-coated tegafur/uracil for advanced hepatocellular carcinoma.".World Journal of Gastroenterology : WJG.14 May 2008;14(18)
2797-2801.doi:10.3748/wjg.14.2797.PMID:18473401.PMC:2710718.Full text.

[3] Nakayama, T."Therapeutic usefulness of postoperative adjuvant chemotherapy with Tegafur-Uracil (UFT) in patients with breast cancer: focus on the results of clinical studies in Japan.".The Oncologist.January 2010;15(1)
26-36.doi:10.1634/theoncologist.2009-0255.PMID:20080863.PMC:3227888.Full text.

[4] Matt, P."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).".The Oncologist.October 2011;16(10)
1451-1457.doi:10.1634/theoncologist.2011-0224.PMID:21963999.PMC:3228070.Full text.

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[§ 1]

Tegafur