FT-207の作用機序に関する研究

抄録

FT-207 was activated to 5-FU by microsomal drug-metabolizing enzyme in the liver, and 5-FU was converted to F-β-alanine etc. in the microsomal supernatants or to FuR etc. in the nucleus.
After administration of FT-207, 5-FU activated in the liver was released into the blood and then transferred to the tumor tissues.
On the other hand, in experiment of the rat treated with CCl₄ in vivo and of the activation of FT-207 by several tissues in vivo, it was observed that FT-207 was activated in the lung, the kidney and spontaneously besides the liver.
After administration of ³H-FT-207, the radioactivities were incorporated as FUMP into the RNA fraction of tumor cells.
Based on these results, we postulated that FT-207 was activated to 5-FU mainly in the liver, partially in the lung, the kidney enzymatically and in whole bodies spontaneously, was transferred to the tumor tissues and remarkably inhibited the RNA and DNA synthesis.