Varespladib methyl in cardiovascular disease

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 A₂ (sPLA₂) in experimental atherosclerosis, the involvement of various sPLA₂ isozymes as mediators of pro-atherogenic lipoprotein remodeling and participants in vascular and systemic inflammatory responses, and the evidence that sPLA₂ 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 sPLA₂ 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.

Keywords::

• anti-inflammatory agents
• lipid-lowering therapy
• phospholipase inhibitors
• secretory phospholipase A₂
• varespladib methyl