Opicapone CAS# 923287-50-7 奥匹帕酮

Opicapone (BIA 9-1067) is a potent, long-acting, reversible inhibitor of catechol-O-methyltransferase (COMT) developed to enhance levodopa bioavailability in Parkinson’s disease. In preclinical studies, it inhibited rat liver COMT with an IC50 of ~3 nM and showed >1000-fold selectivity over other enzymes. In rodent and primate models, opicapone markedly reduced peripheral COMT activity (>90% inhibition) and prolonged plasma levodopa exposure and striatal dopamine levels. The compound exhibited high plasma protein binding and a slow dissociation rate from COMT, explaining its long duration of action. Pharmacokinetic and pharmacodynamic data supported once-daily dosing and clinical development alongside levodopa therapy.