Febuxostat is a novel, nonpurine, selective xanthine oxidase inhibitor and is a potential alternative to allopurinol for patients with hyperuricemia and gout. Unlike allopurinol, which undergoes renal elimination, febuxostat is metabolized via hepatic conjugation and oxidation. Phase III studies have shown that febuxostat, at a once-daily dose of 80, 120 or 240 mg (safety dose), is more effective than allopurinol (300 mg) in reducing and maintaining serum urate concentrations lower than 6 mg/dl. Reductions in gout flares and tophus areas with febuxostat treatment are similar to those occurring with allopurinol therapy. Patients with moderate renal impairment can achieve significant serum urate reductions, without dose adjustments. Therefore, febuxostat represents a viable treatment choice, with documented efficacy and safety in hyperuricemia and gout.