Tegafur

Tegafur structure

Tegafur

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

• 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

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

• 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)
• Pancreatic

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

Mechanism of Action

Tegafur is a prodrug to fluorouracil which is a thymidylate synthase inhibitor.

Pharmacokinetics

Tegafur is metabolized into fluorouracil by CYP2A6.

Adverse Effects

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

Interactive Pathway Map

Click on genes, proteins and metabolites below to link to respective articles.

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

Fluorouracil (5-FU) Activity edit

See Also

• Tegafur/uracil
• Tegafur/gimeracil/oteracil

Conclusion

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.

See also

• Tegafur/uracil
• Tegafur/gimeracil/oteracil

Tegafur Resources
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