Metabolex, Inc.

Home > Pipeline > Arhalofenate

Potential Novel Uricosuric Treatment for Patients with Gout

Arhalofenate (MBX-102) is a novel oral small molecule uricosuric agent that is potentially an attractive new therapy for the treatment of gout. Arhalofenate not only controls hyperuricemia, leading to reduced risk of flares and dissolution of tophi, but also addresses other aspects of metabolic syndrome.

Clinical Development

Arhalofenate has demonstrated robust uric acid lowering in normal subjects and patients with type 2 diabetes with once daily dosing. Arhalofenate was initially being developed for type 2 diabetes, and has completed eight Phase 1 and four Phase 2 studies. During this development program, Metabolex discovered that arhalofenate is an effective uricosuric agent with unique properties, and is repurposing the drug to treat gout. Arhalofenate’s excellent safety and tolerability have been demonstrated in more than 870 patients (>190 patient-years) treated with doses of up to 600 mg for 6 months.

Impressive Profile

Arhalofenate demonstrates robust, dose-dependent reductions in serum uric acid, in patients with mild-to-moderate renal insufficiency and in patients on concomitant aspirin therapy. The uricosuric effect is achieved without increasing urine acidity, thereby not increasing the risk of urolithiasis, and without any effect on kidney function. Additional benefits of arhalofenate include significant improvements in insulin sensitivity, as well as reductions in serum glucose, triglycerides, and markers of inflammation. This wide spectrum of beneficial effects makes arhalofenate an attractive new therapy for the treatment of gout that also addresses other aspects of metabolic syndrome commonly seen in patients with hyperuricemia and gout.