Previous Dosage of Allopurinol Is a Strong Determinant of Febuxostat Efficacy

Biol Pharm Bull. 2017;40(5):681-686. doi: 10.1248/bpb.b16-00972.


Febuxostat has currently played pivotal role in the treatment of hyperuricemia, but there is little comprehensive information for the determinants of individual difference in efficacy of febuxostat. Therefore, the present study, a retrospective investigation, was carried out to analyze the effects of patient characteristics on the efficacy of febuxostat. A total of 225 patients who were continuously prescribed the same dose of febuxostat for 8-12 weeks from the initial therapy were enrolled in the present study. The data, including patient information and laboratory data, were collected from electronic medical records. Serum urate lowering effects of febuxostat were evaluated by calculating the change in serum urate level at baseline and at 8-12 weeks after starting febuxostat. The multiple regression analysis showed the change in serum urate level was significantly lower in male patients and in those with a lower baseline serum urate level, higher previous dose of allopurinol, lower dose of febuxostat and lower body surface area-unadjusted estimated glomerular filtration rate. Concomitantly administered drugs did not show a significantly influence on the efficacy of febuxostat. In conclusion, it should be noted that the serum urate lowering efficacy of febuxostat may decrease in patients with a higher previous dose of allopurinol, renal impairment or male patients. The basic findings of the present study are believed to contribute to the proper use of febuxostat.

Keywords: allopurinol; febuxostat; gender; renal impairment; urate; uric acid.

MeSH terms

  • Adult
  • Aged
  • Aged, 80 and over
  • Allopurinol / administration & dosage*
  • Allopurinol / therapeutic use
  • Febuxostat / therapeutic use*
  • Glomerular Filtration Rate
  • Gout / drug therapy
  • Gout Suppressants / administration & dosage*
  • Gout Suppressants / therapeutic use
  • Humans
  • Hyperuricemia / drug therapy*
  • Hyperuricemia / physiopathology
  • Male
  • Middle Aged
  • Retrospective Studies
  • Treatment Outcome
  • Uric Acid / blood


  • Gout Suppressants
  • Febuxostat
  • Uric Acid
  • Allopurinol