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https://www.readbyqxmd.com/read/28916530/elucidation-of-the-impact-of-p-glycoprotein-and-breast-cancer-resistance-protein-on-the-brain-distribution-of-catechol-o-methyltransferase-inhibitors
#1
Joana Bicker, Ana Fortuna, Gilberto Alves, Patricio Soares-da-Silva, Amilcar Falcao
P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) are clinically important efflux transporters that act cooperatively at the blood-brain barrier, limiting the entry of several drugs into the CNS and affecting their pharmacokinetics, therapeutic efficacy and safety. In the present study, the interactions of catechol-O-methyltransferase (COMT) inhibitors (BIA 9-1059, BIA 9-1079, entacapone, nebicapone, opicapone and tolcapone) with P-gp and BCRP were investigated in order to determine the contribution of these transporters in their access to the brain...
September 15, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28734868/a-single-and-multiple-dose-study-to-investigate-the-pharmacokinetics-and-pharmacodynamics-of-opicapone-a-novel-comt-inhibitor-in-rat
#2
Daniela Gonçalves, Gilberto Alves, Ana Fortuna, Maria João Bonifácio, Patrício Soares-da-Silva, Amílcar Falcão
Opicapone is a novel catechol-O-methyltransferase (COMT) inhibitor that emerged to fulfil the need of a safer and more efficacious COMT inhibitor. The present study was carried out in order to assess and compare the pharmacokinetics and pharmacodynamics (COMT inhibition) of opicapone after single and multiple oral administrations (30 mg/kg) to Wistar rats. For this purpose, at predefined time points up to 72 h post-dosing, blood, liver and kidneys were collected and, then, the concentrations of opicapone and its active metabolite (BIA 9-1079) were determined in plasma and in liver and kidney tissues, as well as the erythrocyte, liver and kidney COMT activity...
July 19, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28580819/opicapone-for-the-management-of-end-of-dose-motor-fluctuations-in-patients-with-parkinson-s-disease-treated-with-l-dopa
#3
Andrew J Lees, Joaquim Ferreira, Olivier Rascol, Heinz Reichmann, Fabrizio Stocchi, Eduardo Tolosa, Werner Poewe
Opicapone is a third generation, highly potent and effective catechol O‑methyltransferase (COMT) inhibitor that optimizes the pharmacokinetics and bioavailability of L-DOPA therapy. Areas covered: In this review, the authors describe the preclinical and clinical development of opicapone. In PD patients with motor fluctuations, once daily opicapone administration was well-tolerated and consistently reduced OFF-time and increased ON-time without increasing the frequency of troublesome dyskinesia, and these benefits were maintained over at least a year of continued open-label therapy...
July 2017: Expert Review of Neurotherapeutics
https://www.readbyqxmd.com/read/28531266/concerns-regarding-opicapone-as-adjunct-to-levodopa-therapy-reply
#4
Andrew J Lees, José-Francisco Rocha, Patricio Soares-da-Silva
No abstract text is available yet for this article.
July 1, 2017: JAMA Neurology
https://www.readbyqxmd.com/read/28531250/concerns-regarding-opicapone-as-adjunct-to-levodopa-therapy
#5
Yu Zhang, Xiaoming Huang
No abstract text is available yet for this article.
July 1, 2017: JAMA Neurology
https://www.readbyqxmd.com/read/28322896/pharmacokinetics-of-opicapone-a-third-generation-comt-inhibitor-after-single-and-multiple-oral-administration-a-comparative-study-in-the-rat
#6
COMPARATIVE STUDY
Daniela Gonçalves, Gilberto Alves, Ana Fortuna, Patrício Soares-da-Silva, Amílcar Falcão
Opicapone is a novel potent, reversible and purely peripheral catechol-O-methyltransferase inhibitor that has been developed to be used as an adjunct to levodopa/aromatic L-amino acid decarboxylase inhibitor therapy for Parkinson's disease. Thus, this study aimed to compare the plasma pharmacokinetics of opicapone and its active metabolite (BIA 9-1079) after the administration of single and multiple oral doses to rats. Wistar rats (n=8 per group) were orally treated with single (30, 60 or 90mg/kg) or multiple (30mg/kg once-daily for seven consecutive days) oral doses of opicapone...
May 15, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28123288/spotlight-on-opicapone-as-an-adjunct-to-levodopa-in-parkinson-s-disease-design-development-and-potential-place-in-therapy
#7
REVIEW
Ádám Annus, László Vécsei
Parkinson's disease (PD) is a progressive, chronic, neurodegenerative disease characterized by rigidity, tremor, bradykinesia and postural instability secondary to dopaminergic deficit in the nigrostriatal system. Currently, disease-modifying therapies are not available, and levodopa (LD) treatment remains the gold standard for controlling motor and nonmotor symptoms of the disease. LD is extensively and rapidly metabolized by peripheral enzymes, namely, aromatic amino acid decarboxylase and catechol-O-methyltransferase (COMT)...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28027332/opicapone-as-adjunct-to-levodopa-therapy-in-patients-with-parkinson-disease-and-motor-fluctuations-a-randomized-clinical-trial
#8
RANDOMIZED CONTROLLED TRIAL
Andrew J Lees, Joaquim Ferreira, Olivier Rascol, Werner Poewe, José-Francisco Rocha, Michelle McCrory, Patricio Soares-da-Silva
Importance: Catechol O-methyltransferase (COMT) inhibitors are an established treatment for end-of-dose motor fluctuations associated with levodopa therapy in patients with Parkinson disease (PD). Current COMT inhibitors carry a high risk for toxic effects to hepatic cells or show moderate improvement. Opicapone was designed to be effective without the adverse effects. Objective: To evaluate the efficacy and safety of 25- and 50-mg/d dosages of opicapone compared with placebo as adjunct to levodopa therapy in patients with PD experiencing end-of-dose motor fluctuations...
February 1, 2017: JAMA Neurology
https://www.readbyqxmd.com/read/28027328/opicapone-a-novel-adjunct-for-an-old-standard
#9
Allison Boyle, Jessika Suescun, Mya C Schiess
No abstract text is available yet for this article.
February 1, 2017: JAMA Neurology
https://www.readbyqxmd.com/read/27763682/effect-of-opicapone-multiple-dose-regimens-on-levodopa-pharmacokinetics
#10
José-Francisco Rocha, Éric Sicard, Nicolas Fauchoux, Amílcar Falcão, Ana Santos, Ana I Loureiro, Roberto Pinto, Maria João Bonifácio, Teresa Nunes, Luís Almeida, Patrício Soares-da-Silva
AIMS: To compare the levodopa/carbidopa (LC) and levodopa/benserazide (LB) pharmacokinetic profiles following repeated doses of opicapone (OPC) administered apart from levodopa. METHODS: Two randomized, double blind, sex-balanced, placebo-controlled studies in four groups of 12 or 18 healthy subjects each. In each group, enrolled subjects received a once-daily morning (5, 15 and 30 mg) or evening (5, 15 and 50 mg) administration of OPC or placebo for up to 28 days...
March 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27599671/clinical-pharmacology-review-of-opicapone-for-the-treatment-of-parkinson-s-disease
#11
Margherita Fabbri, Mario M Rosa, Joaquim J Ferreira
Two catechol-O-methyl transferase inhibitors are currently used as add-on therapy to levodopa for the amelioration of end-of-dose motor fluctuations in Parkinson's disease patients: entacapone, which has moderate efficacy and requires multiple dosing, and tolcapone, which has a poor safety profile. Opicapone (OPC) is a novel, long-acting, peripherally selective, once daily, third-generation catechol-O-methyl transferase inhibitor. Two Phase III clinical trials demonstrated OPC efficacy in reducing OFF-time by an average of about 60 min daily compared with placebo, without increasing ON-time with troublesome dyskinesias, with a good drug safety profile...
October 2016: Neurodegenerative Disease Management
https://www.readbyqxmd.com/read/27590245/erratum-to-opicapone-a-review-in-parkinson-s-disease
#12
Lesley J Scott
No abstract text is available yet for this article.
October 2016: Drugs
https://www.readbyqxmd.com/read/27498199/opicapone-a-review-in-parkinson-s-disease
#13
REVIEW
Lesley J Scott
Oral opicapone (Ongentys(®)), a potent, third-generation, long-acting, peripheral catechol-O-methyltransferase (COMT) inhibitor, is approved as adjunctive treatment to levodopa (L-Dopa)/dopa-decarboxylase inhibitor (DDCI) therapy in adults with Parkinson's disease (PD) and end-of-dose motor fluctuations who cannot be stabilized on those combinations. In 14- to 15-week, double-blind, multinational trials and in 1-year, open-label extension studies in this patient population, opicapone was an effective and generally well tolerated adjunctive therapy to L-Dopa plus a DDCI and other PD therapy...
September 2016: Drugs
https://www.readbyqxmd.com/read/27163503/effect-of-3-single-dose-regimens-of-opicapone-on-levodopa-pharmacokinetics-catechol-o-methyltransferase-activity-and-motor-response-in-patients-with-parkinson-disease
#14
José-Francisco Rocha, Joaquim J Ferreira, Amílcar Falcão, Ana Santos, Roberto Pinto, Teresa Nunes, Luis Almeida, Patrício Soares-da-Silva
This study determined the effects of single doses of opicapone (OPC), a novel third-generation catechol-O-methyltransferase (COMT) inhibitor, on levodopa and 3-O-methyl-levodopa (3-OMD) pharmacokinetics (PK), COMT activity and motor fluctuations in patients with Parkinson disease (PD). Subjects received, in a double-blind manner, 25, 50, and 100 mg OPC or placebo (PLC) in 4 separate treatment periods. The washout period between doses was at least 10 days. During each period, the OPC/PLC capsules were to be coadministered with the morning dose of 100/25 mg levodopa/carbidopa (LC) or levodopa/benserazide (LB) on day 3...
May 2016: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/27138028/opicapone-pharmacokinetics-and-pharmacodynamics-comparison-between-healthy-japanese-and-matched-white-subjects
#15
Amílcar Falcão, José Francisco Rocha, Ana Santos, Teresa Nunes, Patrício Soares-da-Silva
Opicapone (OPC) is a novel third-generation catechol-O-methyltransferase (COMT) inhibitor. This randomized, double-blind, parallel, placebo-controlled and multiple ascending dose study in 3 sequential groups of up to 38 (19 Japanese plus 19 white subjects) aimed to compare the pharmacokinetics (PK) and pharmacodynamics (PD; COMT activity) of opicapone between healthy Japanese and matched white subjects. Enrolled subjects received a once-daily morning administration of OPC (5, 25, or 50 mg) or placebo for 10 days, with plasma and urine concentrations of opicapone and its metabolites measured up to 144 hours postdose, including S-COMT activity...
March 2016: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/27137718/evaluation-of-opicapone-on-cardiac-repolarization-in-a-thorough-qt-qtc-study
#16
Roberto Pinto, Philippe l'Hostis, Alain Patat, Marie-Claude Homery, Amílcar Falcão, Teresa Nunes, José-Francisco Rocha, Patrício Soares-da-Silva
Opicapone, a novel third-generation catechol-O-methyltransferase inhibitor for use as adjunctive therapy in levodopa-treated Parkinson's disease patients, was investigated on cardiac repolarization in healthy adult volunteers. This was a single-center, randomized, double-blind, placebo-controlled, open-label active-controlled, 4-period crossover study conducted in 64 subjects. In each period, subjects received a single oral dose of 50 mg opicapone, 800 mg opicapone, placebo, or 400 mg moxifloxacin and 24-hour 12-lead Holter monitoring was performed on day -1 (baseline) and after each single dose...
November 2015: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/26725545/opicapone-for-motor-fluctuations-in-parkinson-s-disease
#17
David Devos, Caroline Moreau
No abstract text is available yet for this article.
February 2016: Lancet Neurology
https://www.readbyqxmd.com/read/26725544/opicapone-as-an-adjunct-to-levodopa-in-patients-with-parkinson-s-disease-and-end-of-dose-motor-fluctuations-a-randomised-double-blind-controlled-trial
#18
RANDOMIZED CONTROLLED TRIAL
Joaquim J Ferreira, Andrew Lees, José-Francisco Rocha, Werner Poewe, Olivier Rascol, Patrício Soares-da-Silva
BACKGROUND: Opicapone is a novel, once-daily, potent third-generation catechol-O-methyltransferase inhibitor. We aimed to assess the safety and efficacy of opicapone as an adjunct to levodopa compared with placebo or entacapone in patients with Parkinson's disease and motor fluctuations. METHODS: We did a randomised, double-blind, placebo-controlled and active-controlled trial of opicapone as an adjunct to levodopa in patients with Parkinson's disease with end-of-dose motor fluctuations...
February 2016: Lancet Neurology
https://www.readbyqxmd.com/read/26293004/new-treatments-for-levodopa-induced-motor-complications
#19
REVIEW
Olivier Rascol, Santiago Perez-Lloret, Joaquim J Ferreira
Levodopa (l-dopa)-induced motor complications, including motor fluctuations and dyskinesia, affect almost all patients with Parkinson's disease (PD) at some point during the disease course, with relevant implications in global health status. Various dopaminergic and nondopaminergic pharmacological approaches as well as more invasive strategies including devices and functional surgery are available to manage such complications. In spite of undisputable improvements during the last decades, many patients remain significantly disabled, and a fully satisfying management of l-dopa-induced motor complications is still an important unmet need of PD therapy...
September 15, 2015: Movement Disorders: Official Journal of the Movement Disorder Society
https://www.readbyqxmd.com/read/26147707/development-of-a-liquid-chromatography-assay-for-the-determination-of-opicapone-and-bia-9-1079-in-rat-matrices
#20
Daniela Gonçalves, Gilberto Alves, Ana Fortuna, Patrício Soares-da-Silva, Amílcar Falcão
Opicapone is a novel potent, reversible and purely peripheral third generation catechol-O-methyltransferase inhibitor, currently under clinical trials as an adjunct to levodopa therapy for Parkinson's disease. To support additional nonclinical pharmacokinetic studies, a novel high-performance liquid chromatographic method coupled to a diode array detector (HPLC-DAD) to quantify opicapone and its active metabolite (BIA 9-1079) in rat plasma and tissues (liver and kidney) is herein reported. The analytes were extracted from rat samples through a deproteinization followed by liquid-liquid extraction...
March 2016: Biomedical Chromatography: BMC
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