Pharmacokinetic-pharmacodynamic interaction between nebicapone and controlled-release levodopa/benserazide: a single-center, Phase I, double-blind, randomized, placebo-controlled, four-way crossover study in healthy subjects

Clinical Therapeutics
Teresa NunesPatrício Soares-da-Silva

Abstract

Nebicapone is a reversible catechol-O-methyltransferase (COMT) inhibitor. Coadministration of a COMT inhibitor with levodopa and a dopa-decarboxylase inhibitor (carbidopa or benserazide) increases levodopa exposure and its therapeutic effect. The primary objective of this study was to investigate the effect of nebicapone (50, 100, and 200 mg), compared with placebo, on levodopa pharmacokinetics when coadministered with a single dose of controlled-release levodopa 100 mg/benserazide 25 mg. The secondary objectives were to investigate the effect of nebicapone on the erythrocyte-soluble COMT (S-COMT) activity and on the plasma levels of the levodopa 3-O-methylated metabolite (3-O-methyldopa [3-OMD]). Nebicapone's tolerability was also assessed. This was a single-center, Phase I, doubleblind, randomized, placebo-controlled, 4-way crossover study conducted in healthy adult volunteers. Each of the 4 single-dose treatment periods was separated by a washout period of > or = 5 days. During the different treatment periods, subjects received a single dose of controlled-release levodopa 100 mg/benserazide 25 mg concomitantly with nebicapone 50, 100, and 200 mg or placebo. Plasma concentrations of nebicapone, levodopa, and 3-OMD were determ...Continue Reading

References

Feb 1, 1996·British Journal of Pharmacology·M A Vieira-Coelho, P Soares-da-Silva
Jan 14, 2004·Neurology·David J Brooks
Apr 20, 2004·Clinical Neuropharmacology·Luis AlmeidaPatrício Soares-da-Silva
Apr 12, 2005·Movement Disorders : Official Journal of the Movement Disorder Society·Katherine L Widnell, Cynthia Comella
Jun 23, 2006·Drug Metabolism and Disposition : the Biological Fate of Chemicals·A I LoureiroP Soares-Da-Silva
Sep 27, 2007·CNS Drug Reviews·Maria João BonifácioPatrício Soares-da-Silva

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Citations

Aug 3, 2013·Molecular Neurobiology·Hongjuan SunJing Wu
Mar 17, 2010·Current Medical Research and Opinion·Luis AlmeidaPatricio Soares-da-Silva
Jun 10, 2015·American Journal of Cardiovascular Drugs : Drugs, Devices, and Other Interventions·Walid Saliba
Jul 27, 2010·CNS Neuroscience & Therapeutics·Joaquim J FerreiraUNKNOWN BIA-3202-202 Study Investigators

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