Febuxostat Case Study

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Febuxostat is a novel, orally administered, non-purine analogue & selective inhibitor of oxidized and reduced forms of xanthine oxidase, approved in February 2009 by the Us FDA for the cure, management and long term treatment of chronic hyperurecemia and gout even in patients with intolerance/hypersenstivity to allopurinol .If given at a daily dose of 80 mg or 120mg it is reported more effective than allupurinol . Febuxostat does not require any dosage adjustments in patients with mild to moderate renal impairment . In the reported clinical trials, it is found to be well tolerated and superior to conventional drugs for treatment of gout. The purpose of this review is to summarize and compile all the available information covering its chemistry and pharmacology including pharmacokinetic profile.…show more content…
Structure of Febuxostat 2.Chemistry: Febuxostat chemically known as 2-(3-cyano-4-isobutoxyphenyl)-4-methylthiazole-5-carboxylic acid [figure.1]. It is a non-purine analogue and a thiazole derivative possessing carboxylic group.Its molecular formula is C_16 H_16 N_2 O_3S with molecular weight 316.375g/mol. It is available as white, crystalline powder, freely soluble in dimethyl formamide, dimethyl sulfoxide, sparingly soluble in ethanol, methanol and acetonitrile and insoluble in water. Its melting point ranges from 205-208 degrees.it is advised to protect from light and stored at 15 to 25ᵒC. 2.1 Structural activity relationship The structural activity relationship around febuxostat was investigated by scientists at Tejin pharmaceuticals . Febuxostat contains a thiazole ring with a methyl group at the 4-position and a benzene ring with a CN group at the 3-position. These two rings can rotate freely a.Analysis of the structure–activity relationship of various drug candidates suggested that a purine structure is not necessary for xanthine oxidase inhibitory activity and a five-membered heterocycle with a phenyl ring is suitable for xanthine oxidase inhibitor

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