Drug intelligence / Profile preview

arhalofenate + allopurinol

Development stage
Unknown
Lead developer
Gilead Sciences
Modality
Small Molecules
Administration
Oral
01

Overview

**arhalofenate + allopurinol** is an investigational combination regimen for treating gout, consisting of two small molecule drugs: arhalofenate, a uricosuric agent with antiflare properties, and allopurinol, a xanthine oxidase inhibitor. Arhalofenate lowers serum urate by inhibiting urate transporter 1 in the renal proximal tubules, reducing urate reabsorption, and also inhibits neutrophil migration and suppresses proinflammatory cytokine release, preventing gout flares. Allopurinol reduces uric acid synthesis through inhibition of xanthine oxidase, contributing substantial serum urate lowering. Combining these agents leverages dual mechanisms: arhalofenate’s antiflare, anti-inflammatory effects and uricosuric action, plus allopurinol’s powerful urate-lowering effect[1][2][3][4].

02

Targets

OAT10 (Solute carrier family 22 member 13)URAT1 (Uric Acid Transporter 1)OAT4 (Solute carrier family 22 member 11)XO (Xanthine Oxidoreductase)PPARG (Peroxisome proliferator-activated receptor gamma)

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