Objective: To clarify the decision-making process for opicapone’s bedtime regímen.

Background: OPC, a new once-daily COMT inhibitor, was shown to be effective in the treatment of motor fluctuations in Parkinson’s disease patients.

Methods: Review of opicapone, levodopa, carbidopa and benserazide pharmacokinetic data. Five phase 1 studies were selected on the basis of concomitant, alone or 1-hour apart administration between oral single-doses of opicapone (25, 50 and 100mg) and immediate- (IR) or controlled-release (CR) levodopa/carbidopa (LC, 100/25) or levodopa/benserazide (LB, 100/25).

Results: In studies conducted with concomitant administration between opicapone and IR/CR LB, an increase in rate (as assessed by C_max) and extent (as assessed by AUC) to levodopa and benserazide occurred at all doses of opicapone. The increase was statistically significant for IR formulation. Levodopa C_max decreased when doses of opicapone increased. In studies conducted with concomitant administration between opicapone and IR/CR LC, a statistically significant increase in C_max and AUC to levodopa, but not to carbidopa, occurred at all doses of opicapone. Levodopa C_max decreased (more pronounced with CR formulation) when doses of opicapone increased. Finally, similar levodopa and carbidopa C_max was observed when opicapone (50mg) was administered 1-hour apart from IR LC. In all studies, C_max and AUC to opicapone increased in a dose-proportional manner but an important variability was observed between different levodopa formulations and the use of carbidopa or benserazide.

Conclusions: The pharmacokinetic data suggest a certain degree of interaction at absorption phase that was minimized by separating both administrations for at least 1-hour. Opicapone was developed as an add-on to levodopa and, taking into consideration that Parkinson’s disease patients may well necessitate several daily doses of levodopa, a bedtime regimen for opicapone was proposed to better allow the physician to individually tailor the levodopa daily regimen without any concern of a potential absorption interaction.

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MDS Abstracts - https://www.mdsabstracts.org/abstract/decision-making-process-for-opicapones-bedtime-regimen/