Objective: To characterize the effect of food on the pharmacokinetics (PK) and pharmacodynamics (PD) of opicapone (OPC) after single and repeated doses.

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: Two open-label studies were conducted: Study-1 was a 50mg OPC single-dose, 2-period, 2-sequence, crossover fast versus fed (high-fat and high-caloric meal) study in 12 healthy subjects; Study-2 was a 12-day fasting once-daily 50mg OPC single-arm study in 28 healthy subjects, for which on day 10 OPC was administered in the evening with a moderate meal.

Results: In Study-1, following a 50mg OPC single-dose, the OPC rate and extent of absorption were significantly lower in the fed state compared to the fasted state (fed:fasted ratios of 31.73% for C_max and 47.11% for AUC_t). The t_max was also significantly increased by the presence of food. In Study-2, following once-daily 50mg OPC, the OPC rate and extent of absorption were significantly lower in the fed state (day 10) compared to the fasted state (day 9, fed:fasted ratios of 38.21% for C_max and 68.70% for AUC_t). The t_max was also significantly increased by the presence of food. However, despite AUEC being slightly higher (with upper limit of the 90%CI just outside the pre-specified acceptance interval of 80-125%), following a moderate meal (day 10), E_max and the threshold of efficacy, i.e., every 24 hour effect (E_min) of COMT were not affected in a relevant way.

Conclusions: Opicapone was safe and well tolerated and at steady-state, can be administered concomitantly with a moderate meal without affecting its COMT inhibition.

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MDS Abstracts - https://www.mdsabstracts.org/abstract/effect-of-food-on-opicapone-pharmacokinetics-and-pharmacodynamics/