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首页> 外文期刊>International journal of clinical pharmacology and therapeutics >Pharmacokinetic study of S-1
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Pharmacokinetic study of S-1

机译：S-1的药代动力学研究

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Since the first synthesis of 5-FU in 1957 fluoropyrimidines have been widely used clinically in the treatment of solid tumors. Because of good anti-tumor efficacy of 5-FU as a single agent on gastrointestinal tract tumors, many attempts have been made to develop new and superior 5-FU derivatives. Recently, S-1, a new antitumor medication based on the biochemical modulation of 5-FU, (1 M Tegafur (ftorafur, FT), 0.4 M 5-chloro-2, 4-dihydroxypyridine (gimeracil, CDHP), and 1 M potassium oxonate (oteracil, Oxo)) was developed. FT, which is a prodrug of 5-FU, plays a role as an effector. Both CDHP and Oxo, which do not have antitumor activity themselves act as modulators. CDHP competitively inhibits dihydropyrimidine dehydro-genase (DPD, EC 1.3.1.2), which in vitro degrades 5-FU about 180 times more effectively than uracil, leading to prolonged concentrations of 5-FU in blood. Oxo competitively inhibits pyrimidine phosphoribosyl transferase (EC 2.4.2.10), which converts 5-FU to 5-fluorouridine 5'-monophosphate. Oxo is distributed primarily to the gastrointestinal tract after p.o. administration. This component of S-1 decreases the incorporation of 5-fluoro-uridine triphosphate into RNA in the gastrointestinal mucosa and reduces the incidence of diarrhea
机译：自1957年首次合成5-FU以来，氟嘧啶已在临床上广泛用于治疗实体瘤。由于5-FU作为单一药物对胃肠道肿瘤具有良好的抗肿瘤功效，因此人们进行了许多尝试来开发新的和优异的5-FU衍生物。最近，S-1是一种新的抗肿瘤药物，其基于5-FU的生化调节，（1 M替加氟（ftorafur，FT），0.4 M 5-chloro-2、4-二羟基吡啶（gimeracil，CDHP）和1 M研制了奥索酸钾（奥曲西汀，Oxo）。 FT是5-FU的前药，起着效应器的作用。不具有抗肿瘤活性的CDHP和Oxo本身均作为调节剂。 CDHP具有竞争性抑制二氢嘧啶脱氢酶（DPD，EC 1.3.1.2）的能力，该酶在体外降解5-FU的效率是尿嘧啶的180倍左右，从而延长了血液中5-FU的浓度。氧代竞争性抑制嘧啶磷酸核糖基转移酶（EC 2.4.2.10），后者可将5-FU转化为5-氟尿苷5'-单磷酸酯。氧自由基在大便后主要分布于胃肠道。行政。 S-1的这种成分减少了5-氟尿苷三磷酸在胃肠道粘膜中向RNA的掺入并降低了腹泻的发生率

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