Febuxostat CAS NO 144060-53-7 Inquire about Febuxostat

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What is Febuxostat?

Febuxostat (INN; trade names Adenuric [EU], Febutaz [India] and Uloric [US]) is a urate lowering drug, an inhibitor of xanthine oxidase that is indicated for use in the treatment of hyperuricemia and chronic gout.

Febuxostat received marketing approval by the European Medicines Agency on April 21, 2008 and was approved by the U.S. Food and Drug Administration on February 16, 2009.

A study comparing febuxostat to allopurinol found that more individuals treated with febuxostat had decreased levels of uric acid, but there was no difference in the amount of initial gout flares or the surface area of gout tophi.

A committee of the British National Institute for Health and Clinical Excellence concluded that although febuxostat had been shown to be more effective than fixed-dose (300 mg) allopurinol in lowering serum uric acid concentration, it had not been shown to be clinically more efficacious or cost effective compared with allopurinol when taken to control uric acid levels (up to 900 mg). However, the committee recommended febuxostat for people who are intolerant of allopurinol.

Mechanism of action

Febuxostat is a non-purine selective inhibitor of xanthine oxidase. It works by non-competitively blocking the molybdenum pterin center which is the active site on xanthine oxidase. Xanthine oxidase is needed to successively oxidize both hypoxanthine and xanthine to uric acid. Hence, febuxostat inhibits xanthine oxidase, therefore reducing production of uric acid. Febuxostat inhibits both, oxidized as well as reduced form of xanthine oxidase because of which febuxostat cannot be easily displaced from the molybdenum pterin site.

Clinical efficacy

Many long and short-term clinical trials have proved the efficacy of Febuxostat in the treatment of gout and lowering uric acid levels. In these studies Febuxostat was found to be superior to Allopurinol in reducing the serum uric acid levels. Some notable landmark clinical trials are FACT, APEX, EXCEL, FOCUS and CONFIRMS.

Febuxostat versus Allopurinol Controlled Trial (FACT): Serum urate levels were reduced below 6.0 mg/dL at the last three monthly observations in a significantly greater proportion of patients with gout and hyperuricaemia receiving febuxostat 80 or 120 mg once daily than in those receiving allopurinol 300 mg once daily in a 52-week, randomized, double-blind trial.

Allopurinol Placebo controlled Efficacy study of febuXostat (APEX): Febuxostat 80, 120 or 240 mg once daily showed significantly greater urate-lowering efficacy than allopurinol 100 or 300 mg once daily in a 28-week, randomized, double-blind, placebo-controlled trial in patients with gout and hyperuricaemia.

Side effects

The adverse effects associated with febuxostat therapy include nausea, diarrhea, arthralgia, headache, increased hepatic serum enzyme levels and rash.

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Information on this page is provided for general information purposes. You should not make a clinical treatment decision based on information contained in this page without consulting other references including the package insert of the drug, textbooks and where relevant, expert opinion. We cannot be held responsible for any errors you make in administering drugs mentioned on this page, nor for use of any erroneous information contained on this page.