1. S-1: a promising new oral fluoropyrimidine derivative.
- Author
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Saif MW, Syrigos KN, and Katirtzoglou NA
- Subjects
- Administration, Oral, Animals, Antineoplastic Combined Chemotherapy Protocols administration & dosage, Antineoplastic Combined Chemotherapy Protocols metabolism, Antineoplastic Combined Chemotherapy Protocols therapeutic use, Clinical Trials as Topic, Drug Combinations, Drug Evaluation, Preclinical, Humans, Neoplasms drug therapy, Neoplasms pathology, Oxonic Acid administration & dosage, Oxonic Acid metabolism, Oxonic Acid therapeutic use, Tegafur administration & dosage, Tegafur metabolism, Tegafur therapeutic use, Antineoplastic Combined Chemotherapy Protocols pharmacology, Oxonic Acid pharmacology, Tegafur pharmacology
- Abstract
S-1 is an oral fluoropyrimidine that is designed to improve the antitumor activity of 5-fluorouracil (5-FU) concomitantly with an intent to reduce its toxicity. S-1 consists of tegafur, a prodrug of 5-FU combined with two 5-FU biochemical modulators:5-chloro-2,4-dihydroxypyridine (gimeracil or CDHP), a competitive inhibitor of dihydropyrimidine dehydrogenase and oteracil potassium which inhibits phosphorylation of 5-FU in the gastrointestinal tract decreasing serious gastrointestinal toxicities,including nausea, vomiting, stomatitis and diarrhea. Being an oral agent, S-1 offers convenience of administration and prevents complications of central venous access such as infection, thrombosis and bleeding. S-1 has shown efficacy in both gastrointestinal as well non-gastrointestinal malignancies. The authors review the current literature and provide their expert opinion on the incorporation of S-1 in the treatment of solid malignancies [corrected].
- Published
- 2009
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