The Introduction of Febuxostat

Febuxostat is a tablet, is the anti-gout drug. Febuxostat for the oxidized and reduced XOR showed a significant inhibition, and thus its role in reducing uric acid more powerful, durable, so can be used in the treatment of chronic gout hyperuricemia. Febuxostat (Febuxostat) was the first non-Huangpiao new generation of xanthine oxidase inhibitors, alcohol, which by inhibiting xanthine oxidase activity, prevent and reduce hypoxanthine and xanthine to uric acid synthesis to reduce the blood uric acid purpose; clinical trials showed that its tolerance is good, can effectively control the level of hematuria, high uric acid for the treatment of clinical disease (gout). The drug first by the Japanese Teijin in Japan in early 2004 listing, IPSEN company listing in Europe, FDA in February 2009 has been approved in the United States.
Feature
Gout occurs as a result the body produces too much uric acid renal clearance and reduced ability to accumulate uric acid, leading to urate crystal deposition in joints and various organs. Therefore, the treatment of gout usually resort: to promote uric acid excretion and inhibit uric acid production, and use appropriate measures to improve related symptoms. The generation of uric acid and purine metabolism, in the final step in purine metabolism, hypoxanthine in xanthine oxidoreductase (XOR) generated under the action of xanthine, uric acid generated further inhibit the enzyme activity can effectively reduce the uric acid formation. Febuxostat is currently the world's newly developed XOR inhibitors, through a highly selective effect on the oxidase, reduce uric acid synthesis, decreased uric acid concentrations, which effectively treat the disease ventilation. 30 years, allopurinol is the only clinically used drugs that inhibit the production of uric acid and gout as gold is widely used in clinical treatment, the treatment of gout in the anti-achieved good results.
Obvious Advantages:
(1) allopurinol only for the reduced inhibition of XOR, rather than Febuxostat for the oxidized and reduced XOR showed a significant inhibition, and thus its role in reducing uric acid more powerful and lasting;
(2) As for the purine analogues, allopurinol, the inevitable result of involving purine and pyridine metabolism of other enzyme activities. Therefore, allopurinol treatment, the need for repeated administration of large doses of drugs to maintain a high level. This also caused accumulation of the drug due to serious and even fatal adverse reactions. XOR instead of Febuxostat non-purine inhibitor, it has better security.
Clinical Evaluation
A multi-center, double-blind, randomized phase Ⅱ clinical study evaluated the safety and Febuxostat for gout treatment. A total of 136 male and 17 female gout patients were randomized to receive placebo or the product (40, 80 or 120mg / d), 4 weeks after the test found that the materials of each dose group of patients with serum uric acid concentrations than before treatment were significantly lower, by dose groups, respectively, from low to high average of 37%, 44% and 59%, while the placebo group decreased only 2% of patients; the vast majority of patients to adhere to the completion of the test, the product and the placebo group the incidence of adverse reactions similar to , and these adverse reactions are mild, self-limiting, common diarrhea, pain, back pain, headaches and joint pain. A parallel Ⅲ clinical trials comparing the product (80 and 120mg / d) and allopurinol (300mg / d) effect. 760 patients on the one-year study, compared with allopurinol in this product group has more patients to achieve the main trial endpoint - the last 3 months were measured sUA concentration of less than 60mg / L (All subjects were patients with gout, and before the trial sUA concentrations were 80mg / L or more); 52 weeks of treatment, the product did not significantly reduce the size of tophi (gout tophi is unique to the aggregation of uric acid salt crystals body), but early in the trial of high-dose group, the role of the more obvious; each treatment group, sUA concentration standard (<60mg / L) in patients less then sudden gout, tophi and its more pronounced reduction in area ; each treatment group and the incidence of adverse reactions similar adverse reactions, including liver dysfunction, diarrhea, headache, joint-related signs and symptoms and musculoskeletal / connective tissue symptoms.

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