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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