Opicapone
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| Clinical data | |
|---|---|
| Trade names | Ongentys |
| Routes of administration |
By mouth (capsules) |
| ATC code | |
| Pharmacokinetic data | |
| Protein binding | > 99% |
| Metabolism | Reduction, sulphation, glucuronidation, methylation |
| Biological half-life | 0.7 to 3.2 hours |
| Excretion | Faeces (~67%) |
| Identifiers | |
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| Synonyms | 2,5-dichloro-3-(5-(3,4-dihydroxy-5-nitrophenyl)-1,2,4-oxadiazol-3-yl)-4,6-dimethylpyridine 1-oxide |
| CAS Number | |
| ChemSpider | |
| Chemical and physical data | |
| Formula | C15H10Cl2N4O6 |
| Molar mass | 413.17 g/mol |
| 3D model (Jmol) | |
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Opicapone (INN; brand name Ongentys) is a very long acting catechol-O-methyltransferase (COMT) inhibitor discovered, produced and commercialized by BIAL – Portela & Cª, S.A. (S. Mamede do Coronado, Portugal). It was designed to provide a peripherally selective high COMT inhibitory potency and to avoid cell toxicity Opicapone 50 mg is indicated as adjunctive oral therapy to preparations of levodopa + DOPA decarboxylase inhibitors (DDCIs) in adult patients with Parkinson’s disease (PD) and end-of-dose motor fluctuations who cannot be stabilized on those combinations, increasing the bioavailability of levodopa by 24% vs. entacapone and up to 55% vs. levodopa formulations alone. In two phase III multinational trials, BIPARK-I and BIPARK-II, opicapone was shown to be an effective and well tolerated adjunctive therapy to levodopa plus a DDCI and other PD therapy. During the 14- to 15-week double-blind phase of BIPARK-I, once daily adjunctive 50 mg opicapone provided significantly better improvements in motor fluctuations than placebo being non-inferior to entacapone. The beneficial improvements in motor fluctuations with opicapone were maintained in patients who continued adjunctive opicapone in both phase III trials during the 1-year extension open-label studies, with patients who switched from placebo or entacapone to 50 mg opicapone experiencing significant improvements in motor fluctuations during this period. All safety assessments during the 66–67 weeks full study period of these two phase III trials demonstrated a favourable profile of adverse effects with no new unexpected safety concerns, namely, no hepatotoxicity reported. Furthermore, opicapone doesn’t cause urine discolouration due to the low glucuronidation rate and very low plasma/urine concentrations of its metabolite BIA 9-1106, the only metabolite found in urine, being the absence of this adverse effect with opicapone one important advantage over entacapone for patient drug compliance.
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