Febuxostat (Adenuric(®),
Uloric(®), Feburic(®)) is an orally-active, potent, non-
purine, selective
xanthine oxidase inhibitor. In the EU, it is indicated in adults for the treatment of chronic hyperuricaemia in conditions where
urate deposition has already occurred. Unlike
allopurinol, the prototypical
xanthine oxidase inhibitor that is the cornerstone
therapy for chronic
gout,
febuxostat does not require dosage adjustment in patients with mild or moderate renal impairment. In randomized, double-blind studies, 6-12 months' treatment with
febuxostat at dosages approved for use in the EU (80 and 120 mg/day) was significantly more effective in lowering serum
uric acid (sUA) levels in patients with hyperuricaemia and
gout than
allopurinol at dosages commonly prescribed in practice (100-300 mg/day);
febuxostat demonstrated greater
urate-lowering efficacy than
allopurinol in patients with renal impairment. In open-label extension studies, 3-5 years' treatment with
febuxostat maintained a target sUA level of <6.0 mg/dL in most patients; sustained reduction in sUA level was associated with near elimination of
gout flares and improved tophus status.
Febuxostat therapy was generally well tolerated during clinical development; frequently reported adverse events included liver function abnormalities, diarrhoea and
rash. Cardiovascular (CV) events were the most common serious adverse events; the comparative safety of
febuxostat and
allopurinol is being examined further in large, ongoing trials in patients with
gout who already have, or are at risk of developing, CV disease. In conclusion,
febuxostat is a well established antihyperuricaemic agent that provides an effective alternative to
allopurinol for the management of chronic
gout.