|Company Name:||Accendatech Co., LTD. Gold|
|Febuxostat Chemical Properties|
|Febuxostat Usage And Synthesis|
|product description ||Febuxostat developed by Teijin is a new generation of xanthine oxidase inhibitor, for the treatment of high uric acid disease (gout) on clinical , the structure is completely different from xanthine oxidase inhibitor drug developed 40 years ago, it is a new and efficient non-purine selective inhibitor of xanthine oxidase. Xanthine oxidase is a key enzyme in the promotion of uric acid. Febuxostat reduces blood uric acid level in gout patients with hyperuricemia , clinical studies show that the product is safe and effective, this product is metabolized by the liver, it does not depend on renal excretion, so for moderate - severe liver and kidney dysfunction patients it is not necessary to reduce the dose. Dose is once 1 day, 40 mg or 80 mg once ,it is not recommended for the treatment of gout patients without hyperuricemia. |
In February 2009, the US Food and Drug Administration (FDA) approved febuxostat for long-term treatment of gout patients with hyperuricemia.
|Anti-gout drug||Gout is a heterogeneous group of diseases, hereditary or acquired due to uric acid excretion decreasing and purine metabolism. Because the body produces too much uric acid and renal clearance capacity decreases, uric acid accumulates in the body, leading to urate crystals deposited in the joints and organs. Therefore, it means the treatment of gout usually taken to be: promote uric acid excretion, and suppression of uric acid, and adopt appropriate measures to improve related symptoms. |
Uric acid formation is associated with purine metabolism, in the final step of purine metabolism, hypoxanthine becomes xanthine through the role of xanthine oxidoreductase (XOR) ,then further generate uric acid ,inhibiting activity of the enzyme can effectively reduce uric acid production. Febuxostat is currently the world's latest generation of non-purine selective inhibitor of xanthine oxidase, which acts highly selectively on the oxidase, then reduces uric acid synthesis, reduces uric acid levels, thus effectively treats ventilation diseases.
30 years, Allopurinol is the only clinically used drugs to inhibit production of uric acid and is used as gold drugs widely in clinical treatment of gout, and achieves good results in the anti-gout treatment. Compared with allopurinol, febuxostat has obvious advantages:
(1) allopurinol only inhibit reduced XOR while febuxostat shows a significant inhibitory effect on oxidized and reduced XOR , so its role of reducing the uric acid is more powerful, long-lasting;
(2) Because allopurinol is a purine analog,it is inevitable affecting other purine and pyridine metabolic activity . Therefore, allopurinol treatment should be repeated large doses of the drugs to maintain a high level. This also leads to serious or even fatal adverse reactions due to the accumulation of the drug-induced. However, Febuxostat as non-purine XOR inhibitors, has better security.
The above information is edited by the Chemicalbook of Tian Ye.
|Drugs increasing the risk of gout||Diuretics: furosemide , hydrochlorothiazide ), metolazone |
Salicylic acid: such as aspirin (aspirin)
|Intermediate||4-hydroxy thiobenzamide CAS No.:25984-63-8 Appearance: light green to white powder. |
2- (4-hydroxyphenyl) -4-methyl-thiazole-5-carboxylic acid ethyl ester CAS: 161797-99-5 Appearance: yellow powder.
2- (3-aldehyde-4-hydroxyphenyl) -4-methyl-thiazole-5-carboxylic acid ethyl ester CAS No.:161798-01-2 Appearance: light yellow to yellow powder.
2- [3-aldehyde-4-isobutyloxyphenyl] -4-methyl-thiazole-5-carboxylic acid ethyl ester CAS No.:161798-03-4 Appearance: Light yellow to white powder.
2- [3-cyano-4-isobutoxy-phenyl] -4-methyl-thiazole-5-carboxylic acid ethyl ester CAS No.:160844-75-7 Appearance: white to white powder.
|Uses||Treatment of high uric acid disease (gout)
|Chemical Properties||Crystalline Solid|
|Usage||Xanthine oxidase/xanthine dehydrogenase inhibitor. Used for treatment of hyperuricemia and chronic gout. 40-120 mg/day febuxostat was proven effective in lowering serum urate levels when administered
to manage hyperuricemia in patients with gout.|
|Usage||Febuxostat is primarily indicated in conditions like Gout, Hyperuricemia|
|Febuxostat Preparation Products And Raw materials|