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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

The preclinical discovery and development of opicapone for the treatment of Parkinson's disease

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Author(s):
Ettcheto, Miren [1, 2, 3, 4] ; Busquets, Oriol [1, 2, 3, 4, 5] ; Sanchez-Lopez, Elena [6, 7, 4] ; Cano, Amanda [6, 7, 4] ; Manzine, Patricia R. [1, 8, 3, 4, 5] ; Verdaguer, Ester [1, 4, 9] ; Olloquequi, Jordi [3, 10] ; Auladell, Carme [1, 4, 9] ; Folch, Jaume [1, 2] ; Camins, Antoni [1, 3, 4, 5, 10]
Total Authors: 10
Affiliation:
[1] Biomed Res Networking Ctr Neurodegenerat Dis CIBE, Madrid - Spain
[2] Univ Rovira & Virgili, Fac Med & Life Sci, Dept Biochem & Biotechnol, Reus - Spain
[3] Univ Barcelona, Fac Pharm & Food Sci, Dept Pharmacol Toxicol & Therapeut Chem, Barcelona - Spain
[4] Univ Barcelona, Inst Neurosci, Barcelona - Spain
[5] Camins, Antoni, Univ Autonoma Chile, Fac Ciencias Salud, Inst Ciencias Biomed, Lab Cellular \& Mol Pathol, Talca, Chile.Ettcheto, Miren, Univ Barcelona, Fac Pharm & Food Sci, Dept Pharmacol Toxicol & Therapeut Chem, Barcelona - Spain
[6] Univ Barcelona, Fac Pharm & Food Sci, Dept Pharm Pharmaceut Technol & Phys Chem, Barcelona - Spain
[7] Univ Barcelona, Inst Nanosci & Nanotechnol IN2UB, Barcelona - Spain
[8] Fed Univ Sao Carlos UFSCar, Dept Gerontol, Sao Carlos - Brazil
[9] Univ Barcelona, Fac Biol, Dept Cellular Biol Physiol & Immunol, Barcelona - Spain
[10] Univ Autonoma Chile, Fac Ciencias Salud, Inst Ciencias Biomed, Lab Cellular & Mol Pathol, Talca - Chile
Total Affiliations: 10
Document type: Review article
Source: EXPERT OPINION ON DRUG DISCOVERY; v. 15, n. 9 MAY 2020.
Web of Science Citations: 0
Abstract

Introduction Opicapone (OPC) is a well-established catechol-O-methyltransferase (COMT) inhibitor that is approved for the treatment of Parkinson's disease (PD) associated with L-DOPA/L-amino acid decarboxylase inhibitor (DDI) therapy allowing for prolonged activity due to a more continuous supply of L-DOPA in the brain. Thus, OPC decreases fluctuation in L-DOPA plasma levels and favors more constant central dopaminergic receptor stimulation, thus improving PD symptomatology. Areas covered This review evaluates the preclinical development, pharmacology, pharmacokinetics and safety profile of OPC. Data was extracted from published preclinical and clinical studies published on PUBMED and SCOPUS (Search period: 2000-2019). Clinical and post-marketing data are also evaluated. Expert opinion OPC is a third generation COMT inhibitor with a novel structure. It has an efficacy and tolerability superior to its predecessors, tolcapone (TOL) and entacapone (ENT). It also provides a safe and simplified drug regimen that allows neurologists to individually adjust the existing daily administration of L-DOPA. OPC is indicated as an adjunctive therapy to L-DOPA/DDI in patients with PD and end-of-dose motor fluctuations who cannot be stabilized on those combinations. (AU)

FAPESP's process: 17/13224-5 - Study of the JNK1 pathway as a selective target for the treatment of cognitive metabolic disorder: ADAM10 protein analysis
Grantee:Patricia Regina Manzine Moralles
Support Opportunities: Scholarships abroad - Research Internship - Post-doctor
FAPESP's process: 15/26084-1 - Evaluation of platelet ADAM10 in non-Alzheimer's dementias
Grantee:Patricia Regina Manzine Moralles
Support Opportunities: Scholarships in Brazil - Post-Doctoral