[5-Fluorouracil level and pyrimidine nucleoside phosphorylase activity in cancer patients after oral administration of doxifluridine (5'-DFUR)].
For the purpose to evaluate the distribution of 5'-DFUR in the cancerous tissues and non-cancerous tissues of 64 cancer patients (21 gastric, 25 colo-rectal and 18 breast cancers), pyrimidine nucleoside phosphorylase (PyNPase) activity and 5-FU level were determined by bioassay and GC-MS method. 5-FU levels in the plasma were also measured in all patients. Four hundred mg of 5'-DFUR was orally administrated three times a day for 3 to 7 days and just 3 hours before surgical operations. PyNPase activity and 5-FU level were significantly higher in the cancerous tissues than non-cancerous ones. 5-FU levels in the plasma were significantly lower than those in both cancerous and non-cancerous tissues. In conclusion, 5'-DFUR is expected to be an useful anticancer drug because of the selective accumulation of converted 5-FU in cancerous tissues.
Maeda
H
H
Dept. of Surgery II, Nagasaki Univ. School of Medicine, Japan.
Miyamoto
T
T
Mochinaga
N
N
Tsunoda
T
T
D000230:Adenocarcinoma / Q000188:drug therapy / Q000378:metabolism*; D000284:Administration, Oral; D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D001943:Breast Neoplasms / Q000188:drug therapy / Q000378:metabolism*; D003110:Colonic Neoplasms / Q000188:drug therapy / Q000378:metabolism*; D004789:Enzyme Activation / Q000187:drug effects; D005260:Female; D005467:Floxuridine / Q000008:administration & dosage* / Q000493:pharmacokinetics; D005472:Fluorouracil / Q000032:analysis*; D006801:Humans; D008297:Male; D008875:Middle Aged; D010430:Pentosyltransferases / Q000378:metabolism*; D057845:Pyrimidine Phosphorylases; D013274:Stomach Neoplasms / Q000188:drug therapy / Q000378:metabolism*
D005467:Floxuridine; D010430:Pentosyltransferases; D057845:Pyrimidine Phosphorylases; D005472:Fluorouracil; C025034:doxifluridine