Spotlight on opicapone as an adjunct to levodopa in Parkinson's disease: design, development and potential place in therapy

Drug Des Devel Ther. 2017 Jan 9;11:143-151. doi: 10.2147/DDDT.S104227. eCollection 2017.


Parkinson's disease (PD) is a progressive, chronic, neurodegenerative disease characterized by rigidity, tremor, bradykinesia and postural instability secondary to dopaminergic deficit in the nigrostriatal system. Currently, disease-modifying therapies are not available, and levodopa (LD) treatment remains the gold standard for controlling motor and nonmotor symptoms of the disease. LD is extensively and rapidly metabolized by peripheral enzymes, namely, aromatic amino acid decarboxylase and catechol-O-methyltransferase (COMT). To increase the bioavailability of LD, COMT inhibitors are frequently used in clinical settings. Opicapone is a novel COMT inhibitor that has been recently approved by the European Medicines Agency as an adjunctive therapy to combinations of LD and aromatic amino acid decarboxylase inhibitor in adult PD patients with end-of-dose motor fluctuations. We aimed to review the biochemical properties of opicapone, summarize its preclinical and clinical trials and discuss its future potential role in the treatment of PD.

Keywords: COMT inhibitors; Parkinson’s disease; opicapone.

Publication types

  • Review

MeSH terms

  • Antiparkinson Agents / chemical synthesis
  • Antiparkinson Agents / chemistry
  • Antiparkinson Agents / therapeutic use*
  • Drug Design*
  • Drug Therapy, Combination
  • Humans
  • Levodopa / therapeutic use*
  • Oxadiazoles / therapeutic use*
  • Parkinson Disease / drug therapy*


  • Antiparkinson Agents
  • Oxadiazoles
  • Levodopa
  • opicapone