Clinical pharmacology review of opicapone for the treatment of Parkinson's disease.
Two catechol-O-methyl transferase inhibitors are currently used as add-on therapy to levodopa for the amelioration of end-of-dose motor fluctuations in Parkinson's disease patients: entacapone, which has moderate efficacy and requires multiple dosing, and tolcapone, which has a poor safety profile. Opicapone (OPC) is a novel, long-acting, peripherally selective, once daily, third-generation catechol-O-methyl transferase inhibitor. Two Phase III clinical trials demonstrated OPC efficacy in reducing OFF-time by an average of about 60 min daily compared with placebo, without increasing ON-time with troublesome dyskinesias, with a good drug safety profile. In June 2016, the European Commission granted a marketing authorization valid throughout the European Union for OPC, indicated as adjunctive of levodopa decarboxylase inhibitors in adult patients with Parkinson's disease and end-of-dose motor fluctuations.
Clinical Pharmacology Unit, Instituto de Medicina Molecular, Faculty of Medicine, University of Lisbon, Lisbon, Portugal.
Margherita
M
Fabbri
Clinical Pharmacology Unit, Instituto de Medicina Molecular, Faculty of Medicine, University of Lisbon, Lisbon, Portugal.|Laboratory of Clinical Pharmacology & Therapeutics, Faculty of Medicine, University of Lisbon, Lisbon, Portugal.
Mario M
MM
Rosa
Clinical Pharmacology Unit, Instituto de Medicina Molecular, Faculty of Medicine, University of Lisbon, Lisbon, Portugal.|Laboratory of Clinical Pharmacology & Therapeutics, Faculty of Medicine, University of Lisbon, Lisbon, Portugal.|CNS - Campus Neurológico Sénior, Torres Vedras, Portugal.
Joaquim J
JJ
Ferreira
D000978:Antiparkinson Agents / Q000627:therapeutic use*; D065098:Catechol O-Methyltransferase Inhibitors / Q000627:therapeutic use*; D004359:Drug Therapy, Combination; D006801:Humans; D007980:Levodopa / Q000627:therapeutic use; D010069:Oxadiazoles / Q000627:therapeutic use*; D010300:Parkinson Disease / Q000188:drug therapy*; D010601:Pharmacology, Clinical
D000978:Antiparkinson Agents; D065098:Catechol O-Methyltransferase Inhibitors; D010069:Oxadiazoles; D007980:Levodopa; C549349:opicapone
COMT inhibitor; Parkinson's disease; advanced stage; motor fluctuations; opicapone