New Drugs for Lowering LDL-Cholesterol

Rev Med Chir Soc Med Nat Iasi. 2016 Jul-Sep;120(3):485-90.

Abstract

LDL-Cholesterol (LDL-C) is a well-known risk factor for cardiovascular disease. Although statins are the mainstream treatment for lowering LDL-C level, additional LDL-lowering therapies are needed to reduce residual cardiovascular risk, especially in patients at very high risk, or with hereditary lipid disorderes or statin intolerance. The proprotein convertase subtilisin/kexin type 9 (PCSK9) is a key regulator for LDL-Receptor activity and an attractive target for the treatment of hypercholesterolaemia. From its discovery in 2003, several therapeutic approaches to the inhibition of PCSk9 have been proposed. Monclonal antibodies that bind to PCSJ9 received marketing approval in 2015 (alirocumab and evolucumab) or are being evaluated in phase III trials (bococizumab). Many other molecules are in preclinical studies, phase I or II clinical trials. Another point of interest carefully investigated is the cardiovascular benefit of reducing LDL-C using these new molecules. High hopes are invested in them.

Publication types

  • Review

MeSH terms

  • Antibodies, Monoclonal / therapeutic use
  • Antibodies, Monoclonal, Humanized
  • Anticholesteremic Agents / therapeutic use*
  • Cardiovascular Diseases / etiology
  • Cholesterol, LDL / blood*
  • Humans
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / therapeutic use
  • Hypercholesterolemia / drug therapy*
  • PCSK9 Inhibitors*
  • Proprotein Convertase 9 / physiology

Substances

  • Antibodies, Monoclonal
  • Antibodies, Monoclonal, Humanized
  • Anticholesteremic Agents
  • Cholesterol, LDL
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors
  • PCSK9 Inhibitors
  • PCSK9 protein, human
  • Proprotein Convertase 9
  • evolocumab
  • alirocumab