Literature DB >> 20809869

Varespladib methyl in cardiovascular disease.

Robert S Rosenson1, Heather Fraser, Joaquim Trias, Colin Hislop.   

Abstract

IMPORTANCE OF THE FIELD: The high risk of recurrent cardiovascular events amongst patients with cardiovascular disease receiving evidence-based therapies has prompted investigations into complimentary treatments that may reduce residual risk. Analyses of clinical trials in statin-treated patients demonstrate that elevated lipid levels and an activated systemic inflammatory state are associated with a higher risk of recurrent cardiovascular events. AREAS COVERED IN THIS REVIEW: This article reviews evidence supporting the causal role for secretory phospholipase A(2) (sPLA(2)) in experimental atherosclerosis, the involvement of various sPLA(2) isozymes as mediators of pro-atherogenic lipoprotein remodeling and participants in vascular and systemic inflammatory responses, and the evidence that sPLA(2) inhibition reduces atherosclerosis in experimental models and biomarkers associated with cardiovascular events in coronary heart disease (CHD) patients. WHAT THE READER WILL GAIN: The experimental basis for sPLA(2) inhibition with varespladib methyl as a potential candidate for lowering recurrent cardiovascular events particularly in acute coronary syndrome patients is discussed. TAKE HOME MESSAGE: Varespladib methyl therapy reduces atherogenic lipoprotein concentrations and systemic inflammatory markers in CHD patients. The future role of varespladib methyl in CHD patients awaits the results of ongoing clinical trials.

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Year:  2010        PMID: 20809869     DOI: 10.1517/13543784.2010.517193

Source DB:  PubMed          Journal:  Expert Opin Investig Drugs        ISSN: 1354-3784            Impact factor:   6.206


  3 in total

1.  Novel genetic approach to investigate the role of plasma secretory phospholipase A2 (sPLA2)-V isoenzyme in coronary heart disease: modified Mendelian randomization analysis using PLA2G5 expression levels.

Authors:  Michael V Holmes; Holly J Exeter; Lasse Folkersen; Christopher P Nelson; Montse Guardiola; Jackie A Cooper; Reecha Sofat; S Matthijs Boekholdt; Kay-Tee Khaw; Ka-Wah Li; Andrew J P Smith; Ferdinand Van't Hooft; Per Eriksson; Anders Franco-Cereceda; Folkert W Asselbergs; Jolanda M A Boer; N Charlotte Onland-Moret; Marten Hofker; Jeanette Erdmann; Mika Kivimaki; Meena Kumari; Alex P Reiner; Brendan J Keating; Steve E Humphries; Aroon D Hingorani; Ziad Mallat; Nilesh J Samani; Philippa J Talmud
Journal:  Circ Cardiovasc Genet       Date:  2014-02-21

2.  Discovery of a Series of Indole-2 Carboxamides as Selective Secreted Phospholipase A2 Type X (sPLA2-X) Inhibitors.

Authors:  Laurent Knerr; Fabrizio Giordanetto; Peter Nordberg; Daniel Pettersen; Nidhal Selmi; Hans-Georg Beisel; Hannah de la Motte; Thomas Olsson; Tim D J Perkins; Margareta Herslöf; Åsa Månsson; Mikael Dahlström; Ingemar Starke; Johan Broddefalk; Gabrielle Saarinen; Fredrik Klingegård; Eva Hurt-Camejo; Birgitta Rosengren; Johan Brengdahl; Frank Jansen; Mattias Rohman; Jenny Sandmark; Kenth Hallberg; Tomas Åkerud; Robert G Roth; Marie Ahlqvist
Journal:  ACS Med Chem Lett       Date:  2018-06-23       Impact factor: 4.345

3.  Identification of distant drug off-targets by direct superposition of binding pocket surfaces.

Authors:  Marcel Schumann; Roger S Armen
Journal:  PLoS One       Date:  2013-12-31       Impact factor: 3.240

  3 in total

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