|
IC50
a (μmol/L)
|
Relative ratio of IC50
b
|
Plasma concentrationc (μmol/L)
|
Concentrationd (μmol/L)
|
---|
Topiroxostat
|
0.069
|
1
|
0.152
|
0.152
|
N-Oxide
|
13
|
1/188
|
0.0952
|
0.0005
|
N
1-Glucuronide
|
>100
|
1/1449
|
2.77
|
0.002
|
N
2-Glucuronide
|
>100
|
1/1449
|
0.686
|
0.0005
|
-
aHalf maximal (50 %) xanthine oxidoreductase (XOR)-inhibitory concentration
-
bThe relative ratio of IC50 between topiroxostat and its metabolites
-
cPre-hemodialysis plasma concentrations of topiroxostat and its metabolites at week 52
-
dEstimated plasma concentrations based on the relative ratio of IC50 between topiroxostat and its metabolites