E. Fuse et al., DISPOSITION OF DX-52-1, A NOVEL ANTICANCER AGENT, AFTER INTRAVENOUS ADMINISTRATION TO MICE AND DOGS, European journal of drug metabolism and pharmacokinetics, 22(1), 1997, pp. 53-63
DX-52-1 is a new derivative of a quinocarmycin analogue. The dispositi
on of [H-3]-DX-52-1 was investigated in mice and dogs after intravenou
s administration (4 and 0.15 mg/kg, respectively). The plasma concentr
ation of non-volatile radioactivity was 7.4 mu g eq./ml 3 min after ad
ministration to mice, then declined biphasically until 2 h. The distri
bution of non-volatile radioactivity into blood cells was 20% 3 min af
ter administration, being maintained until 30 min. The plasma concentr
ation of unchanged drug was almost equal to that of the radioactivity
3 min after administration and the unchanged drug ratio decreased rapi
dly. High radioactivity was found in the gall bladder, kidney, liver,
and lung 15 min after administration. No radioactivity was detected in
most tissues 24 h post-administration. The cumulative excretion of to
tal radioactivity into urine and feces after administration was 68 and
28% within 96 h, respectively. The plasma concentration of non-volati
le radioactivity was 0.65 mu g eq./ml 3 min after administration to do
gs. The distribution of non-volatile radioactivity into blood cells wa
s about 20% 3 min after administration and this level tended to increa
se with time. The cumulative excretion of total radioactivity into uri
ne and feces after administration was 62 and 24%, respectively.