Drug intelligence / Profile preview

benzbromarone

Development stage
Phase 4
Lead developer
Sanofi
Modality
Small Molecules
Administration
Oral
01

Overview

Benzbromarone is a uricosuric agent and non-competitive inhibitor of xanthine oxidase used primarily for the treatment and prevention of gout, especially in patients who are intolerant to or do not respond to first-line therapies like allopurinol. It lowers plasma uric acid concentrations by blocking renal tubular reabsorption of uric acid, mainly through inhibition of the urate transporter 1 (URAT1) in the proximal renal tubule, and possibly by increasing intestinal elimination of uric acid. Benzbromarone is structurally related to amiodarone and has also been shown to be a potent inhibitor of cytochrome P450 enzymes CYP2C9 and CYP2C19. The drug was introduced in the 1970s, marketed widely outside the United States, but withdrawn by Sanofi-Synthélabo in 2003 due to reports of serious hepatotoxicity; it remains available from other manufacturers in some countries. Clinical trials have suggested it may be more effective than both allopurinol and probenecid for lowering serum uric acid levels[1][3][4][5][6].

Brand names
BenzbromaroneBenzbromaron ALBenzbromarone TevaBenaroneBenroneBemaronBeenroneBenzmaronBenzon
Other names
2-ethyl-3-(3,5-dibromo-4-hydroxybenzoyl)benzofuran3,5-dibromo-4-hydroxyphenyl-(2‑ethyl‑3‑benzofuranyl) ketonebenzbromaronabenzbromaronum
02

Targets

URAT1 (Uric Acid Transporter 1)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)XO (Xanthine Oxidoreductase)CYP2C19 (Cytochrome P450 2C19)

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