Drug intelligence / Profile preview

lesinurad + febuxostat

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

Lesinurad + febuxostat is an oral fixed-dose combination therapy used for the treatment of gout, specifically in patients whose serum uric acid (UA) levels are inadequately controlled with febuxostat alone. Lesinurad is a selective uric acid reabsorption inhibitor which blocks URAT1 (and OAT4), promoting increased renal excretion of uric acid, while febuxostat is a xanthine oxidase inhibitor that suppresses the production of uric acid. The combination thus provides a dual mechanism: lowering urate levels both by decreasing production and enhancing excretion. Lesinurad is mainly indicated for use alongside a xanthine oxidase inhibitor in patients not at target urate levels, and clinical trials have shown that this combination yields superior serum urate lowering and reduction in tophus size compared with febuxostat alone in patients with tophaceous gout.

02

Targets

URAT1 (Uric Acid Transporter 1)OAT4 (Solute carrier family 22 member 11)XO (Xanthine Oxidoreductase)

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