Gan To Kagaku Ryoho. 1986 Jun;13(6):2193-8.
590-S (PH-FU) has a chemical structure of 1-(3-oxo-1, 3-dihydro-1-isobenzofranyl)-5-fluorouracil, which belongs to the fluorinated pyrimidine group. Preclinical studies of the drug revealed better a therapeutic index compared with that of Tegafur. The preclinical pharmacokinetic studies revealed a steep increase and rapid decrease of 590-S and activated 5-FU in the blood compared with those of other fluorinated pyrimidines. We performed pharmacokinetic studies on patients using oral administration of 590-S. The results indicated a steep increase and rapid decrease of 590-S and 5-FU in blood concentrations. Both substances were excreted in extremely small amounts into the urine and bile. In contrast to the blood concentrations, 590-S and 5-FU remained in the tissues for an extended period. The above results indicated that orally administered 590-S showed interesting pharmacokinetic characteristics which warrant further clinical studies.
590-S（PH-FU）的化学结构为1-(3-氧代-1,3-二氢-1-异苯并呋喃基)-5-氟尿嘧啶，属于氟化嘧啶类。该药物的临床前研究显示，其治疗指数优于替加氟。临床前药代动力学研究表明，与其他氟化嘧啶相比，590-S和活化的5-氟尿嘧啶在血液中的浓度急剧上升和快速下降。我们对口服590-S的患者进行了药代动力学研究。结果表明，590-S和5-氟尿嘧啶的血药浓度急剧上升和快速下降。两种物质经尿液和胆汁排泄的量极少。与血药浓度不同，590-S和5-氟尿嘧啶在组织中停留的时间较长。上述结果表明，口服590-S显示出有趣的药代动力学特征，值得进一步开展临床研究。
