[PCSK9 inhibitors: emerging treatment to lower cholesterol?]

Rev Med Suisse. 2014 Mar 5;10(420):539-42, 544.
[Article in French]

Abstract

The achievement rate of recommended low-density lipoprotein cholesterol (LDL-C) targets of < 1.8 mmol/l for secondary prevention in very high risk patients is difficult. Observational studies reported that loss of function mutation of the PCS9 was associated with LDL-C decrease level and reduction of cardiovascular events. Monoclonal antibodies to PCSK9 (REGN727 and AMG 145, PSCK9 inhibitors) have been tested in clinical studies of phase I and II and showed LDL-C level reduction of 60-70% compared to placebo. This approach appears safe and well-tolerated. The PCSK9 inhibitors are now tested in large phase III clinical studies to assess the long-term safety and efficacy of this new promising approach.

MeSH terms

  • Anticholesteremic Agents / pharmacology
  • Anticholesteremic Agents / therapeutic use*
  • Cholesterol, LDL / blood
  • Humans
  • Hyperlipoproteinemia Type II / drug therapy*
  • Proprotein Convertase 9
  • Proprotein Convertases / antagonists & inhibitors*
  • Serine Endopeptidases

Substances

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