Novel drug safely lowers serum uric acid in hyperuricaemic patients

Treatment with HP501, a novel renal urate transporter 1 inhibitor, effectively reduces serum uric acid (SUA) in healthy volunteers and patients with hyperuricaemia, with no serious adverse effects, according to the results of study.

A team of investigators conducted a placebo-controlled, double-blind, randomized, three-part, phase I/IIa study to assess the safety, efficacy, and pharmacokinetics of HP501. The trial consisted of a single ascending dose (SAD) part with 32 participants, a multiple ascending dose part with 48 participants, and a drug-drug interaction part with 20 participants.

In addition, the investigators assessed the effects of food in healthy volunteers who received HP501 45 mg in the fed state in the SAD part.

Sixty-eight healthy volunteers and 32 hyperuricaemic patients participated in this study, and treatment with HP501 appeared to be well tolerated in both arms.

In hyperuricaemic patients dosed with HP501 45 mg over 10 days, two had elevated aspartate aminotransferase (<2 times upper limit of normal) and three had increased alanine transaminase (<2.5 times upper limit of normal). No dose-limited adverse events occurred.

The concentrations of SUA across HP501 doses (from 5 to 60 mg) decreased by a maximum of nearly 50 percent. The novel drug also showed predictable pharmacokinetics across different dose levels in both healthy volunteers and patients with hyperuricaemia.

Of note, HP501 and febuxostat delivered synergistic SUA-lowering effects with no evident pharmacokinetics interaction.

“HP501 was effective at reducing SUA in healthy volunteers and hyperuricaemic patients with a tolerable safety profile, warranting further development,” the investigators said.