Objective: To assess the differences between two catechol-O-methyltransferase (COMT) inhibitors, opicapone (OPC) and entacapone (ENT).

Background: Opicapone and ENT are COMT inhibitors developed as adjunct therapies to levodopa (LD) to improve the bioavailability of LD, smoothen LD plasma levels and decrease peak-trough fluctuations.

Method: A review of all published OPC clinical studies that included an ENT arm was conducted, to compare the extent of COMT inhibition, clinical efficacy, and safety profiles of OPC and ENT in the management of motor fluctuations in Parkinson’s disease.

Results: A randomized, double-blind study in healthy subjects showed that OPC, when compared to ENT, provides prolonged and enhanced LD bioavailability associated with more pronounced, long-lasting, and sustained COMT inhibition. A phase 3 clinical trial, BIPARK I, established the noninferiority of OPC 50mg vs ENT 200mg. In addition, it demonstrated OPC’s effectiveness in reducing “Off” time with once-daily dosing, with greater magnitude of reduction in time in the “Off” state vs ENT (LS mean change of –116.8min vs –96.3min, respectively), offering potential advantages over the multiple daily doses required with ENT. In this study, a higher proportion of patients on OPC vs ENT showed minimally, much or very much improved Clinician (73% vs 50.9% respectively) and Patient (72.1% vs 52.5% respectively) Global Impression of Change scores. The open-label phase of the study showed that patients who switched from ENT to OPC, had an additional 39.3min reduction in “Off” time and an additional 45min increase in “Good On” time. Moreover, OPC has shown a favorable safety profile compared to ENT; while severe diarrhea and urine discoloration are associated with the treatment of ENT, no treatment-related diarrhea or urine discoloration has been observed with OPC. In real-world clinical practice, a recent HEOR study showed that after 6 months of treatment with both COMT inhibitors, treatment with OPC resulted in 18.5% fewer neurology outpatient visits compared to ENT, this effect was maintained until the last follow-up (18 months).

Conclusion: Opicapone’s sustained COMT inhibition, once-daily dosing convenience, favorable efficacy and safety profiles distinguish it from ENT, potentially offering improved patient outcomes, treatment adherence and reduced healthcare cost.

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MDS Abstracts - https://www.mdsabstracts.org/abstract/comparative-analysis-of-opicapone-and-entacapone-in-the-management-of-motor-fluctuations-in-patients-with-parkinsons-disease-from-clinical-trials-to-healthcare-resource-usage/