Pharmacokinetics of arundic acid, an astrocyte modulating agent, in acute ischemic stroke.

Arundic acid is an astrocyte modulating agent that improves neurological outcome in experimental acute stroke models. The pharmacokinetics of arundic acid in patients with acute ischemic stroke was investigated in a randomized, double-blind study. Six groups of 8 to 9 patients each received 2, 4, 6, 8, 10, or 12 mg/kg/h of arundic acid for a daily 1-hour infusion until completion of 7 doses. Maximum plasma concentrations of arundic acid increased with increasing dose; however, the systemic exposure was less than dose proportional at higher doses. The mean terminal half-life was approximately 2 to 3 hours. There was no excessive accumulation in plasma. Although systemic exposure in elderly patients was 30% greater than that in younger patients, the plasma concentration returned to nearly or below the limit of quantification prior to next administration. The pharmacokinetics of arundic acid in acute stroke patients assessed in this study were similar to that in healthy adults.