In 2 phase 3 studies, treatment with opicapone (Neurocrine Biosciences, San Diego, CA) increased ON time without troublesome dyskinesia almost twice as much as placebo for participants with Parkinson’s disease (PD). The ON period was defined as the period during which motor symptoms are controlled by levodopa/carbidopa treatment. ON time duration was measured with the validated Hauser patient diary.
Opicapone (50 mg) is taken once daily with the first dose of levodopa and does not require titration. Neither troublesome gastrointestinal side effects nor clinically significant changes in liver enzyme elevation were seen in clinical trials. For patients with sialorrhea, opicapone has the advantage of not discoloring the saliva. It is hoped that these factors will all promote increased adherence to treatment.
Eiry Roberts, MD, chief medical officer of Neurocrine remarked, “In our 2 pivotal studies, we see that once-daily opicapone added to levodopa therapy results in significant increases in ON time without troublesome dyskinesia for people with PD and motor fluctuations. We are very excited about the opportunity to provide clinicians and patients with a new option for treating motor fluctuations of PD and remain on track with plans for submission of opicapone to the Food and Drug Administration (FDA) in the second quarter of 2019.”
In BIPARK-1 (NCT01568073), treatment with opicapone (50 mg) increased ON time by an average of 1.9 ± 0.2 hours compared with 0.9 ± 0.2 hours with placebo (P = .002). Similarly, in BIPARK-2 (NCT01227655), participants treated with 50 mg of opicapone had 1.7 ± 0.3 hours more time in the ON state vs 0.9 ± 0.3 more hours for those treated with placebo (P = .025). The mean change from baseline for all participants treated with opicapone was 2.0 ± 2.6 hours in BIPARK-1 (n = 494) and 1.8 ± 3.2 hours in BIPARK-2 (n = 339). More than 60% of participants treated with opicapone achieved at least 1 hour more time in the ON state.
Dyskinesia occurred in 17.4% of participants treated with opicapone vs 6.2% of those given placebo; however, few participants discontinued for this reason (1.9% in opicapone arms vs 0.4% in placebo arm). Serious dyskinesia occurred in only 0.3% of participants treated with opicapone.
Opicapone is a novel and highly selective peripheral catechol-O-methyltransferase (COMT) inhibitor in development in the US for the adjunctive treatment of Parkinson’s disease. Approved for adjunctive treatment of Parkinson’s disease in Europe, opicapone is marketed under the brand name Ongentys by BIAL – Portela & CA, SA Opicapone increases the length of time levodopa is available in the periphery for transport across the blood-brain barrier by inhibiting levodopa breakdown.