Saif Muhammad Wasif, Syrigos Kostas N, Katirtzoglou Nikos A
Yale University School of Medicine, Division of Medical Oncology, 333 Cedar Street, FMP 116 New Haven, CT 06520, USA.
Expert Opin Investig Drugs. 2009 Mar;18(3):335-48. doi: 10.1517/13543780902729412.
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].
S-1是一种口服氟嘧啶，旨在提高5-氟尿嘧啶（5-FU）的抗肿瘤活性，同时降低其毒性。S-1由替加氟组成，替加氟是5-FU的前体药物，与两种5-FU生化调节剂联合使用：5-氯-2,4-二羟基吡啶（吉美嘧啶或CDHP），一种二氢嘧啶脱氢酶的竞争性抑制剂，以及奥替拉西钾，它抑制5-FU在胃肠道的磷酸化，减少严重的胃肠道毒性，包括恶心、呕吐、口腔炎和腹泻。作为一种口服药物，S-1给药方便，可避免中心静脉置管的并发症，如感染、血栓形成和出血。S-1在胃肠道和非胃肠道恶性肿瘤中均显示出疗效。作者回顾了当前的文献，并就S-1在实体恶性肿瘤治疗中的应用提供了专家意见[已修正]。
