Topiroxostat, a selective
xanthine oxidoreductase inhibitor, is used in Japan for the treatment of hyperuricemic patients with or without
gout. In terms of the effectiveness of
topiroxostat in lowering serum
urate levels, the dose-response relationship has been evaluated; however, it remains to be verified. A randomized, multi-center, double-blinded study of
topiroxostat was performed for Japanese hyperuricemic patients with or without
gout. During the 16-week study, 157 Japanese hyperuricemic patients with or without
gout were randomly assigned to receive a placebo,
topiroxostat at 120 or 160 mg/day, or
allopurinol at 200 mg/day. The primary endpoint of this study was to determine the lowering rate of serum
uric acid levels compared to those of baseline at the end of administration. A dose-response relationship (regarding decreases in the serum
urate levels) was confirmed for the placebo and
topiroxostat at 120 and at 160 mg/day. Moreover, at the end of administration, the lowering rate of serum
urate levels was determined to be -44.8% in the
topiroxostat 160-mg/day group. No significant difference in the incidence of adverse events was observed among all groups, including the
allopurinol group. The serum
urate-lowering effect of
topiroxostat was found to have a dose-response relationship in Japanese hyperuricemic patients with or without
gout.