The FDA approved Febuxostat for the treatment of hyperuricemia

In February 16, 2009, the United States FDA approved nearly 40 years first for the treatment of hyperuricemia in gout drug. The febuxostat is produced by the Takeda pharmaceuticals North America. Febuxostat by reducing blood levels of uric acid in the blood of patients with gout symptoms improve.

According to a statement of Takeda's drug: the structure of febuxostat (CAS NO: 144060-53-7)

 is quite different from the structure of xanthine oxidase inhibitors developed 40 years ago, it is a kind of new and efficient non purine selective inhibitor of xanthine oxidase. Xanthine oxidase is the key enzyme of promoting the formation of uric acid. The Febuxostat can lower blood levels of uric acid in hyperuricemic gout patients, the efficacy and safety of febuxostat have been demonstrated in clinical studies. What’s more, in moderate to severe renal insufficiency patients do not need to adjust the dosage.

The dose of febuxostat 1 times a day, every 40 mg or 80 mg, but it is not recommended patients with gout but no high hyperuricemia to use febuxostat.

The original manufacturer of Febuxostat is another Japanese company - Japan Teijin Pharmaceutical. The president of the Teijin pharmaceutical companies had a recent statement; we can understand the company’s global strategy of febuxostat. He said, before the FDA in febuxostat license, the product of Ipsen Company has also obtained the approval of EU. Ipsen is about Benfeibusuotan Kyorin pharmaceutical in the EU's permission, Takeda Kitami pharmaceuticals is the product in the United States licensing company. The company has been in the global strategic sense of milepost type. At the same time, he also pointed out that, in the Asian market, Kyorin pharmaceutical will take the independent development or the form of joint development.

Gout is a heterogeneous group of disorders, hereditary and (or) to obtain the excretion of uric acid by reducing and (or) purine metabolic disorder. Clinical features: hyperuricemia, and urate crystal deposition characteristic, caused by acute arthritis, gout, interstitial nephritis, serious show joint deformity and function of dirty love. It is often associated with uric acid calculi. Pseudogout is often confused with gout, because its symptoms are very similar, then, pseudogout is caused by metabolic disorder of calcium phosphate, instead of uric acid metabolism disorder caused by.

According to the United States National Arthritis and musculoskeletal and skin diseases research institute (NIAMS) data showed that, there are 6000000, 20 years of age or older people experience the gout life in the United States of America. The male patients usually aged 40-50 is more common, and women with premenopausal rare. Experienced in organ transplant patients are also prone to gout. NIAMS points out that the drugs can increase the risk of gout: (1) the diuretic furosemide; hydrochlorothiazide; metolazone; (2) such as aspirin, salicylic acid; (3) nicotinic acid; (4) Cyclosporine Neoral; (5) Levodopa.

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Side effects of Febuxostat

Febuxostat (INN; trade names Adenuric [Europe], Febutaz [India] and Takeda's Uloric [United States]) 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. The CAS NO of Febuxostat is 144060-53-7.

Febuxostat is used to treat gout. Gout is a type of arthritis in which uric acid, a naturally occurring substance in the body, builds up in the joints and causes sudden attacks of redness, swelling, pain, and heat in one or more joints. Febuxostat is in a class of medications called xanthine oxidase inhibitors. It works by decreasing the amount of uric acid that is made in the body. Febuxostat is used to prevent gout attacks, but not to treat them once they occur.

Nausea may occur. If this effect persists or worsens, tell your doctor or pharmacist promptly.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Febuxostat may rarely cause serious (possibly fatal) liver disease. It may also cause an increase in liver enzymes. Your doctor will order blood tests to measure these enzymes. Keep all medical/lab appointments. Tell your doctor immediately if you develop symptoms of liver disease, including persistent nausea, stomach/abdominal pain, dark urine, yellowing eyes/skin.

Tell your doctor immediately if any of these rare but very serious side effects occur: chest pain/pressure, sudden tiredness, weakness, jaw/left arm pain, weakness on one side of the body, slurred speech, sudden vision changes, confusion, pink/bloody urine, painful urination.

Febuxostat may cause a rash that could be a sign of a severe reaction. Therefore, tell your doctor immediately if you develop any rash.

A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

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The Clinical efficacy of Febuxostat

Febuxostat 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. Almost forgot, the CAS NO is 144060-53-7.

Febuxostat is used widely in Clinical, but the Clinical efficacy is not very clearly.

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): 760 patients with gout and a sUA >8.0 mg/dl were randomly assigned to receive either febuxostat 80 or 120mg or allopurinol 300mg once daily for 52 weeks.The primary endpoint was the proportion of patients to achieve a sUA concentration below 6.0 mg/dl at the last three monthly measurements. The primary endpoint was achieved in 53% of patients receiving 80 mg febuxostat, 62% of patients receiving 120mg and 21% of those receiving allopurinol (p <0.001 for each febuxostat group compared with allopurinol).

Allopurinol Placebo controlled Efficacy study of febuXostat (APEX): The APEX trial was a head-to-head phase III controlled clinical trial for gout, with a total of 1072 patients with sUA levels higher than 8.0 mg/dl. Patients were randomized to a once daily fixed dose of placebo; febuxostat 80mg,120mg, or 240 mg; or allopurinol 300mg or 100mg, depending on their baseline serum creatinine (≤1.5 mg/dl or ≥1.6 to <2.0 mg/dl, respectively). The primary endpoint for the trial was the proportion of subjects with sUA levels below 6.0 mg/dl at each of the last three visits. After 1 year of treatment, 82% of the patients in all febuxostat groups achieved sUA levels below 6.0 mg/dl, compared with 39% of the patients in both allopurinol groups. In groups with moderate renal impairment the primary endpoint was achieved by 44% receiving febuxostat 80mg, 45% receiving 120mg, and 60% receiving 240mg, compared with 0% in the allopurinol and placebo groups.

Febuxostat Comparative EXtension Long-Term study (EXCEL): The EXCEL trial was the other long-term trial that assessed the clinical efficacy and safety of febuxostat against allopurinol. In this study, 1086 patients were enrolled to receive fixed daily doses of febuxostat 80mg or 120 mg, or allopurinol 300 mg. Dose adjustments were allowed during the first 6 months to maintain sUA levels between 3.0 and 6.0 mg/dl. The primary endpoint, as in most of the trials, was maintenance of sUA below 6.0 mg/dl and other measures assessed were flares requiring treatment, tophus size and safety profile. After the first month of treatment, nearly 80% of patients receiving either febuxostat dose achieved sUA less than 6 mg/dl, compared with only 46% of subjects on allopurinol. After ULT reassignment, more than 80% of all remaining subjects maintained target levels of sUA at each visit. Maintenance of sUA below 6.0 mg/dl resulted in baseline tophus resolution in 46%, 36%, and 29% of subjects on febuxostat 80mg, 120mg and allopurinol, respectively. In addition, gout flares were significantly reduced, obviating the need for gout flare therapy. Overall adverse events did not show significant differences among groups.

Febuxostat Open Label of Urate-Lowering Efficacy and Safety(FOCUS):The FOCUS trial was a 5-year extension study that assessed reduction and maintenance of sUA levels below 6.0 mg/dl as the primary efficacy endpoint. A total of 116 patients were initially enrolled to receive a dose of 80mg febuxostat with dose adjustment to either 40 or 120mg between weeks 4 and 24. At 5 years, 50% of patients were discontinued prematurely from the study with no apparent relation to adverse events; among the remaining 50% of patients, 93% maintained a sUA level below 6.0 mg/dl at 5 years. There was a clear association with no gout flares in these patients and most patients also had tophus resolution.

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