Trial reportBritish journal of clinical pharmacology2013
Opicapone: a short lived and very long acting novel catechol-O-methyltransferase inhibitor following multiple dose administration in healthy subjects.
Trial report in British journal of clinical pharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 37 papers, 2 of them syntheses that pooled it.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
37 citing papers in PubMed, 2 syntheses or guidelines pooled it.
- Adverse event profiles of adjuvant treatment with opicapone in Parkinson's disease: A systematic review and meta-analysis.Frontiers in pharmacology · 2022Pooled it
- Systematic Review on Parkinson's Disease Medications, Emphasizing on Three Recently Approved Drugs to Control Parkinson's Symptoms.International journal of environmental research and public health · 2021Pooled it
- Long-term safety and efficacy of opicapone in Japanese Parkinson's patients with motor fluctuations.Journal of neural transmission (Vienna, Austria : 1996) · 2021Trial
- Pharmacokinetic Comparison of Capsule and Tablet Formulations of Opicapone in Healthy Japanese Subjects: Phase 1 Study.Clinical pharmacology in drug development · 2021Trial
- Effect of opicapone multiple-dose regimens on levodopa pharmacokinetics.British journal of clinical pharmacology · 2017Trial
- Effect of opicapone and entacapone upon levodopa pharmacokinetics during three daily levodopa administrations.European journal of clinical pharmacology · 2014Trial
- Opicapone Pharmacokinetics and Effects on Catechol- O -Methyltransferase Activity and Levodopa Pharmacokinetics in Patients With Parkinson Disease Receiving Carbidopa/Levodopa.Clinical neuropharmacologyTrial
- The safety and tolerability of opicapone in elderly Parkinson's disease patients: a real-world, multicenter, retrospective study.Journal of neural transmission (Vienna, Austria : 1996) · 2026Article
- German Delphi consensus: COMT inhibitors in the management of wearing-off fluctuations in Parkinson's disease.Journal of neural transmission (Vienna, Austria : 1996) · 2026Article
- Opicapone in Parkinson's disease: a real-world, multicenter, retrospective study to identify patient characteristics for sustained treatment benefit.Journal of neural transmission (Vienna, Austria : 1996) · 2026Article
- The Treatment of Older Patients with Parkinson's Disease.Deutsches Arzteblatt international · 2025Review
- Levodopa treatment: impacts and mechanisms throughout Parkinson's disease progression.Journal of neural transmission (Vienna, Austria : 1996) · 2025Review
- A phase I study to evaluate the effect of high-dose carbidopa on levodopa pharmacokinetics.Frontiers in pharmacology · 2025Article
- Review
- Know your molecule: pharmacological characterization of drug candidates to enhance efficacy and reduce late-stage attrition.Nature reviews. Drug discovery · 2024Review
- Objective assessment of the effects of opicapone in Parkinson's disease through kinematic analysis.Neurological sciences : official journal of the Italian Neurological Society and of the Italian Society of Clinical Neurophysiology · 2024Article
- Clinical benefit of MAO-B and COMT inhibition in Parkinson's disease: practical considerations.Journal of neural transmission (Vienna, Austria : 1996) · 2023Review
- Absorption, metabolism and excretion of opicapone in human healthy volunteers.British journal of clinical pharmacology · 2022Article
- [Relevance of COMT inhibitors in the treatment of motor fluctuations].Der Nervenarzt · 2022Review
- COMT Inhibitors in the Management of Parkinson's Disease.CNS drugs · 2022Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
10 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimsThe aim of this study was to assess the tolerability, pharmacokinetics and inhibitory effect on erythrocyte soluble catechol-O-methyltransferase (S-COMT) activity following repeated doses of opicapone.
methodsThis randomized, placebo-controlled, double-blind study enrolled healthy male subjects who received either once daily placebo or opicapone 5, 10, 20 or 30 mg for 8 days.
resultsOpicapone was well tolerated. Its systemic exposure increased in an approximately dose-proportional manner with an apparent terminal half-life of 1.0 to 1.4 h. Sulphation was the main metabolic pathway. Opicapone metabolites recovered in urine accounted for less than 3% of the amount of opicapone administered suggesting that bile is likely the main route of excretion. Maximum S-COMT inhibition (Emax ) ranged from 69.9% to 98.0% following the last dose of opicapone. The opicapone-induced S-COMT inhibition showed a half-life in excess of 100 h, which was dose-independent and much longer than plasma drug exposure. Such a half-life translates into a putative underlying rate constant that is comparable with the estimated dissociation rate constant of the COMT-opicapone complex.
conclusionDespite its short elimination half-life, opicapone markedly and sustainably inhibited erythrocyte S-COMT activity making it suitable for a once daily regimen.
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Registered trials
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