Effect of opicapone on levodopa pharmacokinetics, catechol‐O‐methyltransferase activity and motor fluctuations in patients with Parkinson's disease

Abstract

OPC is a promising new COMT inhibitor that significantly decreased COMT activity, increased systemic exposure to levodopa and improved motor response.

International Parkinson and movement disorder society evidence‐based medicine review: Update on treatments for the motor symptoms of Parkinson's disease

“…There were no new studies evaluating tolcapone, and the conclusion remains unchanged. Opicapone, a new COMT inhibitor, was evaluated in 2 high‐quality positive efficacy studies and 1 high‐quality pharmacokinetic study but with motor outcomes . The conclusion is thus “efficacious,” and the implication for clinical practice is “clinically useful” for treating motor fluctuations.…”

Effect of 3 Single‐Dose Regimens of Opicapone on Levodopa Pharmacokinetics, Catechol‐O‐Methyltransferase Activity and Motor Response in Patients With Parkinson Disease

“…15 Levodopa exposure increased up to 66%, maximum COMT inhibition (E max ) reached 80%, and improvement in various motor outcomes was observed, including a dose-dependent change in absolute OFF time. 18 All treatments tested were generally well tolerated. In conclusion, this exploratory (phase 2a) single-dose study in PD patients with motor fluctuations showed that OPC inhibited COMT activity, increased levodopa bioavailability, and was well tolerated when administered with standard-release 100/25 mg levodopa/carbidopa or levodopa/benserazide.…”

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

“…All active treatments increased LD bioavailability in a dose-dependent manner, caused sustained dose-dependent but not proportional COMT inhibition and consequently a significantly lower exposure to 3-OMD. Based on the participants’ diaries, all active treatments caused a dose-dependent decrease in the absolute OFF time (15.6 min and 145 min with 5 mg and 30 mg OPC, respectively) 38. Overall, 15 mg and 30 mg OPC reached statistical significance compared to PLC in improving ON time without dyskinesia.…”

“…Ferreira et al38 investigated the effects of 28-day long administration of 5 mg, 15 mg and 30 mg OPC on LD pharmacokinetics, COMT inhibition and motor fluctuations in PD patients. The population of the study was similar to that described in the previous trial.…”