PCSK9 inhibition - a novel mechanism to treat lipid disorders?

Curr Pharm Des. 2013;19(21):3869-77. doi: 10.2174/13816128113199990303.

Abstract

Plasma low-density lipoprotein cholesterol (LDL-C) is one of the biomarkers of cardiovascular disease (CVD) risk. LDL is cleared from the circulation preferentially through the LDL receptor (LDLR) pathway. Proprotein convertase subtilisin/kexin 9 (PCSK9) promotes the degradation of the LDLR. PCSK9 inhibition is attractive as a new strategy for lowering LDL-C levels, especially in combination with lipid lowering drugs such as statins. We review data from the available studies which focus on PCSK9 as a potential target in the treatment of hyperlipidemia. Further studies are still necessary to investigate the potential underlying mechanisms involved.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Cardiovascular Diseases / etiology
  • Cardiovascular Diseases / prevention & control
  • Cholesterol, LDL / blood
  • Humans
  • Hyperlipidemias / complications
  • Hyperlipidemias / drug therapy*
  • Hypolipidemic Agents / pharmacology
  • Hypolipidemic Agents / therapeutic use*
  • Molecular Targeted Therapy
  • Proprotein Convertase 9
  • Proprotein Convertases / antagonists & inhibitors*
  • Proprotein Convertases / metabolism
  • Risk
  • Serine Endopeptidases / metabolism

Substances

  • Cholesterol, LDL
  • Hypolipidemic Agents
  • PCSK9 protein, human
  • Proprotein Convertase 9
  • Proprotein Convertases
  • Serine Endopeptidases