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Potential Novel Anti-inflammatory Uricosuric Treatment for Patients with Gout

Arhalofenate is an anti-inflammatory uricosuric drug that reduces the risk of gout flares while also lowering sUA. It is the only drug that not only does not increase the risk of flares when lowering sUA, but it actually decreases their incidence, duration and severity. This exceptional profile is expected to lead to significant advantages in treating the gout patient, including reducing painful events and health care utilization, improving patient satisfaction and compliance, the latter leading to greater long-term achievement of treatment goals, including halting the progression of joint destruction.

Clinical Development

Across three Phase 2 studies, arhalofenate demonstrated a pattern in reductions in flare incidence, duration and severity, and in lowering of sUA. This novel dual action is a result of the drug's ability to lower IL-1β production in response to MSU crystals while at the same time being able to block uric acid uptake by transporters localized to the proximal renal tubule.

Arhalofenate was previously studied for diabetes and throughout its development has had a safe clinical profile. It has completed 15 studies with nearly 1000 subjects exposed, including four phase 2 studies with durations of 3 to 6 months (~175 patient-years). It has successfully completed all of its required non-clinical toxicology, including the 2-year carcinogenicity studies.

Impressive Profile

Arhalofenate decreases painful gout flares while lowering sUA. It demonstrates robust, dose-dependent reductions in serum uric acid, in patients with mild-to-moderate renal insufficiency and in patients on concomitant aspirin therapy. Additional benefits of arhalofenate include 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.