title: Opicapone for the treatment of Parkinson's disease.
abstract: Parkinson's disease (PD) is a progressive neurodegenerative disease. The currently available treatment options only have a symptomatic effect. With disease progression almost all antiparkinsonian pharmacological classes are tried, but the gold standard of pharmacological management is still L-dopa. Various strategies can be used to raise the dopaminergic tone. Catechol-O-methyltransferase (COMT) inhibitors attain this goal by decreasing L-dopa peripheral metabolism. Areas covered: Opicapone (Ongentys®) is a new COMT inhibitor developed to fulfill the need for more potent, safer and longer acting COMT inhibitors. This review puts into context opicapone's indications, its chemical and preclinical data, the pharmacodynamics and pharmacokinetic characteristics, and the efficacy and safety results delivered by clinical trials. Expert opinion: Opicapone is an efficacious COMT inhibitor. Its proprieties make it adequate for a once-a-day oral dose regimen. It has proved to reduce the off-time and to increase the on-time without troublesome dyskinesias in PD patients with motor fluctuations. The reported adverse events suggest an overall safe and well-tolerated profile. The most common adverse events were dyskinesia, and there were no issues of concern for hepatotoxicity, severe diarrhoea or chromaturia. Further evidence is still needed to conclude how it compares with other drugs for the treatment of motor fluctuations.
authors.affiliation: a Laboratory of Clinical Pharmacology and Therapeutics, Faculty of Medicine , University of Lisbon , Lisboa , Portugal.|b Clinical Pharmacology Unit, Instituto de Medicina Molecular, Faculty of Medicine , University of Lisbon , Lisbon , Portugal.|c Huntington's Disease Centre, Institute of Neurology , University College London , London , UK.
authors.forename: Filipe B
authors.initials: FB
authors.lastname: Rodrigues
authors.affiliation: a Laboratory of Clinical Pharmacology and Therapeutics, Faculty of Medicine , University of Lisbon , Lisboa , Portugal.|b Clinical Pharmacology Unit, Instituto de Medicina Molecular, Faculty of Medicine , University of Lisbon , Lisbon , Portugal.|d CNS - Campus Neurológico Sénior , Torres Vedras , Portugal.
authors.forename: Joaquim J
authors.initials: JJ
authors.lastname: Ferreira
mesh_terms: D000978:Antiparkinson Agents / Q000627:therapeutic use*; D002394:Catechol O-Methyltransferase / Q000187:drug effects; D065098:Catechol O-Methyltransferase Inhibitors / Q000627:therapeutic use; D018450:Disease Progression; D004298:Dopamine / Q000378:metabolism; D006801:Humans; D010069:Oxadiazoles / Q000627:therapeutic use*; D010300:Parkinson Disease / Q000188:drug therapy*
chemical_list: D000978:Antiparkinson Agents; D065098:Catechol O-Methyltransferase Inhibitors; D010069:Oxadiazoles; D002394:Catechol O-Methyltransferase; D004298:Dopamine; C549349:opicapone
keywords: COMT inhibitor; Opicapone; Parkinson’s disease; motor fluctuations