Darapladib for the treatment of cardiovascular disease

Expert Rev Cardiovasc Ther. 2015 Jan;13(1):33-48. doi: 10.1586/14779072.2015.986466.

Abstract

Elevated levels of phospholipase A2 have been linked to atherosclerotic plaque progression, instability via promoting inflammation and subsequent acute coronary events. Epidemiological studies have demonstrated the correlation between elevated levels associated phospholipase A2 and cardiovascular events. Therefore, specific inhibition of lipoprotein-associated phospholipase A2 with darapladib has been tested as a therapeutic option for atherosclerosis. The aim of this profile is to review the physiologic aspects of lipoprotein-associated phospholipase A2 and to revisit the clinical evidence of darapladib as therapeutic option for atherosclerosis.

Keywords: atherosclerosis; darapladib; inflammation; phospholipase A2.

Publication types

  • Review

MeSH terms

  • 1-Alkyl-2-acetylglycerophosphocholine Esterase / drug effects*
  • Animals
  • Atherosclerosis / drug therapy*
  • Benzaldehydes / therapeutic use*
  • Humans
  • Inflammation / drug therapy*
  • Oximes / therapeutic use*
  • Plaque, Atherosclerotic / drug therapy*
  • Risk

Substances

  • Benzaldehydes
  • Oximes
  • 1-Alkyl-2-acetylglycerophosphocholine Esterase
  • darapladib