[FT-207 and 5-FU concentrations in brain tumor tissues, plasma and CSF after administration of FT-207 suppository].

FT-207 suppository was administered to 19 patients with brain tumors. FT-207 and 5-FU concentrations in tumor tissues and plasma were measured using chemical assay method. After operation, FT-207 and 5-FU concentrations in plasma and CSF were measured serially for 24 hours in some patients following administration of FT-207 suppository. Following results were obtained. 1) The level of 5-FU concentration in tumor tissues was higher than that of in plasma while the level of FT-207 concentration in tumor tissues was lower than that of in plasma. 2) The level of 5-FU concentration in CSF had been kept highly very longer time, compared with that of in plasma. On the other hand the level of FT-207 concentration in plasma and CSF decreased rapidly. 3) About 0,05 mcg/ml of 5-FU in CSF would be maintained for 24 hours in patients following administration of FT-207 suppository (1 g, daily) for 3 days or more.

[Cerebrospinal fluid distributions of systemically administered fluorinated pyrimidines].

Transfer of systemically administered fluorinated pyrimidines (Tegafur, TAC-278, HCFU and FD-1) to cerebrospinal fluid was studied in 7 patients primary brain tumors. Seven patients had had irradiation and also had V-P shunt operation for hydrocephalus 5-FU concentration in CSF was extremely high in FD-1 and TAC-278 administration, but not in Tegafur and HCFU administration. In addition, Tegafur and HCFU did not reveal any cumulative effects of 5-FU in CSF by continuous prolonged systemic administration. The facts suggest strongly the usefullness of the agents in the treatment of intracranial neoplasms, which have high CSF concentrations. However, intermediate metabolites of 5-FU in CSF are different from those in systemic pathway, and FD-1 and TAC-278 produce CNS toxicities. Therefore, further extensive studies are necessary to utilize these agents for the treatment of intracranial neoplasms.