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Table 4 Xanthine oxidoreductase-inhibitory activities of topiroxostat and its metabolites in patients at week 52

From: Effects, safety, and plasma levels of topiroxostat and its metabolites in patients receiving hemodialysis

 

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

  1. aHalf maximal (50 %) xanthine oxidoreductase (XOR)-inhibitory concentration
  2. bThe relative ratio of IC50 between topiroxostat and its metabolites
  3. cPre-hemodialysis plasma concentrations of topiroxostat and its metabolites at week 52
  4. dEstimated plasma concentrations based on the relative ratio of IC50 between topiroxostat and its metabolites