OBJECTIVE: To review the pharmacology and clinical data for febuxostat in the treatment of gout and hyperuricemia.

DATA SOURCES: Articles on febuxostat published in English between 1966 and November 2006 were identified through a MEDLINE search using the key words febuxostat, TEI-6720, TMX-67, gout, and hyperuricemia. Additional articles were identified through search of the publications’ reference lists. Abstracts from the 2005 proceedings of the American College of Rheumatology, American College of Clinical Pharmacology, and American Society for Clinical Pharmacology and Therapeutics were also searched for febuxostat studies.

STUDY SELECTION AND DATA EXTRACTION: All published febuxostat trials in humans were selected for this review. Clinical, pharmacokinetic, and pharmacodynamic data were evaluated.

DATA SYNTHESIS: Febuxostat is a non-purine, selective inhibitor of xanthine oxidase that has demonstrated efficacy in lowering serum uric acid levels in patients with hyperuricemia associated with gout. Compared with allopurinol 300 mg/day, febuxostat 80 or 120 mg/day was more effective in lowering serum uric acid levels to less than 6 mg/dL. Febuxostat appears to be safe, with the majority of treatment-related adverse events reported being transient and mild-to-moderate in severity. However, abnormal elevation of liver enzyme levels has been reported with its use. There have been no documented major drug interactions with febuxostat.

CONCLUSIONS: Febuxostat is a novel, non-purine xanthine oxidase inhibitor undergoing review by the FDA. It represents a potential advancement in the treatment of hyperuricemia associated with gout.

J Pharm Technol 2006;22:342-48.

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