制癌剤の基礎的検討-1-TAC-278について

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In this study, we performed pharmacokinetic studies on TAC-278, a new type of fluorinated pyrimidine group. TAC-278 has a higher antitumor effect compared with that of FT-207 on MOPC-104E, L1210, Sarcoma 180 and Lewis Lung carcinoma. TAC-278 was administrated orally in a dose of 20 mg/kg to mongrel dogs. In the gastric mucosal layer, after oral administration, the concentration of TAC-278 was higher than that of TAC-478 or 5-FU. On the other hand, in the hepatic vein, the concentration of TAC-478 was higher than that of TAC-278 or 5-FU. It is considered that TAC-278 may be metabolized in the liver. A higher concentration of 5-FU in the plasma was revealed in comparison to other types in the fluorinated pyrimidine group. Although TAC-278 has a higher 5-FU level in plasma than other types of flouorinated pyrimidine, its clinical effect was not greater than that of 5-FU or FT-207 in phase I and II clinical trials. This discrepancy remains unsolved and requires further research on metabolism of F-dUMP or F. RNA in tumor.
学校法人昭和大学・昭和医学会の論文