A Phase I Dose-Escalation Study of the Pharmacokinetics, Pharmacodynamics, and Safety of a Single Oral Dose of Tigulixostat

These findings demonstrate that tigulixostat exhibits approximately dose-proportional PK, with linear elimination and predictable exposure across the 25-300 mg range. A dose-dependent reduction in serum uric acid was observed up to 200 mg, with a plateau effect at 300 mg. The PK profile of GD-MET-1 indicated lower systemic exposure and less consistent dose proportionality compared with the parent compound, suggesting a supportive rather than dominant role in PD activity. The favorable safety and tolerability profile reinforces tigulixostat's potential as a novel therapeutic agent for the management of hyperuricemia.