arhalofenate

Arhalofenate is a small molecule uricosuric drug developed primarily for the treatment of gout. It lowers serum uric acid by inhibiting its reabsorption in the proximal tubules of the kidney, acting as an inhibitor of Solute carrier family 22 member 12 (URAT1), Solute carrier family 22 member 11 (OAT4), and Solute carrier family 22 member 13 (OAT10). In addition to its uricosuric effect, arhalofenate exhibits anti-inflammatory properties by suppressing proinflammatory cytokines such as interleukin-1β (IL-1β) and reducing neutrophil influx at sites of inflammation. Mechanistically, it also acts as a selective partial agonist of Peroxisome proliferator activated receptor gamma (PPARγ), which was initially explored for type 2 diabetes mellitus but later discontinued for this indication. Arhalofenate has completed Phase 2 clinical trials for gout and is ready to advance to Phase 3; development for type 2 diabetes was terminated after Phase 3 studies. Developers: CymaBay Therapeutics Manufacturers: Gilead Sciences

Other names

(–)-halofenate