Pharmacokinetics and pharmacodynamics of febuxostat (TMX-67), a non-purine selective inhibitor of xanthine oxidase/xanthine dehydrogenase (NPSIXO) in patients with gout and/or hyperuricemia

Nucleosides Nucleotides Nucleic Acids. 2004 Oct;23(8-9):1119-22. doi: 10.1081/NCN-200027381.


The diurnal change of sUA and the effect of febuxostat on this change were investigated in 10 patients with gout and/or hyperuricemia. The diurnal sUA change after the last dose during the 4-week treatment phase (20 mg, QD) was almost the same as the pre-treatment value. Considering the dose, the AUC(obs) and Cmax of unchanged drug in patients with gout and/or hyperuricemia were estimated to be similar to those of healthy male adults. The results show that a 6-week treatment with febuxostat is safe and well-tolerated in the target patient population for this drug.

Publication types

  • Clinical Trial
  • Clinical Trial, Phase II

MeSH terms

  • Area Under Curve
  • Enzyme Inhibitors / pharmacokinetics*
  • Enzyme Inhibitors / therapeutic use*
  • Febuxostat
  • Gout / drug therapy*
  • Humans
  • Hyperuricemia / drug therapy*
  • Male
  • Oxygen / metabolism
  • Thiazoles / pharmacokinetics*
  • Thiazoles / therapeutic use*
  • Time Factors
  • Xanthine Dehydrogenase / antagonists & inhibitors
  • Xanthine Oxidase / antagonists & inhibitors


  • Enzyme Inhibitors
  • Thiazoles
  • Febuxostat
  • Xanthine Dehydrogenase
  • Xanthine Oxidase
  • Oxygen