Tegafur
Tegafur[edit | edit source]
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 | edit source]
- 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 | edit source]
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 | edit source]
Tegafur is a prodrug to fluorouracil which is a thymidylate synthase inhibitor.[1]
Pharmacokinetics[edit | edit source]
Tegafur is metabolized into fluorouracil by CYP2A6.[3][4]
Adverse Effects[edit | edit source]
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 | edit source]
Click on genes, proteins and metabolites below to link to respective articles.[§ 1]
See Also[edit | edit source]
Conclusion[edit | edit source]
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[edit | edit source]
References[edit | edit source]
- ↑ 1.0 1.1 1.2 1.3 1.4 1.5 1.6 Martindale: The Complete Drug Reference Full text, , Pharmaceutical Press, 14 November 2011,
- ↑ Ishikawa, T, Chemotherapy with enteric-coated tegafur/uracil for advanced hepatocellular carcinoma., World Journal of Gastroenterology : WJG, Vol. 14(Issue: 18), pp. 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, Vol. 15(Issue: 1), pp. 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, Vol. 16(Issue: 10), pp. 1451-1457, DOI: 10.1634/theoncologist.2011-0224, PMID: 21963999, PMC: 3228070, Full text,
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