Febuxostat 99% Purity Antigout API Xanthine Oxidase Inhibitor CAS 144060-53-7 Pharmaceutical Grade EP USP Standard for Gout Treatment

Product Overview

Febuxostat is a potent, non-purine, selective xanthine oxidase inhibitor used for the chronic management of hyperuricemia in patients with gout. It works by inhibiting xanthine oxidase, the enzyme responsible for the production of uric acid, thereby reducing serum uric acid levels. Unlike allopurinol, a purine analog that inhibits multiple enzymes in the purine synthesis pathway, febuxostat is highly selective for xanthine oxidase, resulting in a more targeted mechanism of action and potentially fewer side effects.

Chemically, febuxostat is 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-1,3-thiazole-5-carboxylic acid with the molecular formula C₁₆H₁₆N₂O₃S and a molecular weight of 316.37 g/mol. It is a white crystalline powder with low aqueous solubility but good oral bioavailability of approximately 84%.

Mechanism of Action

Febuxostat exerts its urate-lowering effect through selective xanthine oxidase inhibition:

• Xanthine Oxidase Inhibition: Highly selective, non-purine inhibitor that binds to both the oxidized and reduced forms of xanthine oxidase

• Uric Acid Reduction: Blocks the conversion of hypoxanthine to xanthine and xanthine to uric acid, the final steps in uric acid biosynthesis

• Dose-dependent Effect: Serum uric acid lowering is dose-dependent over the therapeutic range

• No Effect on Purine/Pyrimidine Synthesis: Does not inhibit other enzymes involved in purine and pyrimidine metabolism, unlike allopurinol

Febuxostat achieves rapid uric acid lowering, with maximal effects typically observed within 2-4 weeks of initiating therapy. It is effective in patients with mild to moderate renal impairment and does not require dose adjustment in these populations.

Clinical Indications & Market Position

Febuxostat is indicated for:

• Chronic Gout Management: Long-term treatment of hyperuricemia in patients with gout who have failed or are intolerant to allopurinol

• Tophaceous Gout: Particularly useful in patients with tophi due to its potent urate-lowering efficacy

• Treatment-naïve Patients: First-line option for chronic gout management in many guidelines

The global gout treatment market continues to grow due to increasing prevalence of hyperuricemia and gout worldwide, driven by aging populations, changing diets, and rising rates of metabolic syndrome. Febuxostat, as the first new oral urate-lowering therapy in decades, holds a significant position in this market.

Quality Specifications

Our febuxostat API meets strict pharmacopoeial standards:

• Complies with EP and USP monograph requirements

• Purity: ≥99.0% by HPLC

• Related substances: Total impurities ≤0.5%, single impurity ≤0.1%

• Residual solvents: Meet ICH Q3C guidelines

• Heavy metals: ≤10 ppm

• Loss on drying: ≤0.5%

• Residue on ignition: ≤0.1%

• Melting point: 205-208°C

• Particle size: Customizable

• Each batch released with full Certificate of Analysis (COA)

• GMP manufacturing with complete regulatory documentation

Packaging & Storage

• Packaging options: 25kg fiber drums with double PE liners, 5kg aluminum tins, 1kg aluminum foil bags

• Custom packaging: Available upon request for special requirements

• Storage conditions: Store in tightly sealed containers in a cool, dry place, protected from light

• Shelf life: 36 months under proper storage conditions

• Supply capacity: Tons per month, ensuring reliable supply for both large and small customers

• Regulatory support: DMF, CEP, and other regulatory filings available to support customer registrations