Lipid-lowering agents

J Cardiovasc Pharmacol Ther. 2013 Sep;18(5):401-11. doi: 10.1177/1074248413492906. Epub 2013 Jun 27.

Abstract

The role of lipid lowering in reducing the risk of mortality and morbidity from cardiovascular disease (CVD) is well established. Treatment particularly aimed at decreasing low-density lipoprotein cholesterol (LDL-C) is effective in reducing the risk of death from coronary heart disease and stroke. Statins form the cornerstone of treatment. However, in some individuals with a high risk of CVD who are unable to achieve their target LDL-C due to either intolerance or lack of efficacy, there is the need for alternative therapies. This review provides an overview of the different classes of currently available lipid-lowering medications including statins, fibrates, bile acid sequestrants (resins), and omega-3 fatty acids. Data are presented on their indications, pharmacology, and the relevant end point clinical trial data with these drugs. It also discusses the human trial data on some novel therapeutic agents that are being developed including those for homozygous familial hypercholesterolemia--the antisense oligonucleotide mipomersen and the microsomal transfer protein inhibitor lomitapide. Data are presented on phase II and III trials on agents with potentially wider applications, cholesterol ester transfer protein inhibitors and proprotein convertase subtilisin kexin 9 inhibitors. The data on a licensed gene therapy for lipoprotein lipase deficiency are also presented.

Keywords: bile acid sequestrant; cardiovascular disease; dyslipidemia; fibrate; lipid lowering; statin.

Publication types

  • Review

MeSH terms

  • Cardiovascular Diseases / etiology
  • Cardiovascular Diseases / mortality
  • Cardiovascular Diseases / prevention & control*
  • Cholesterol, LDL / blood
  • Cholesterol, LDL / drug effects
  • Coronary Disease / etiology
  • Coronary Disease / mortality
  • Coronary Disease / prevention & control
  • Drug Design
  • Dyslipidemias / complications
  • Dyslipidemias / drug therapy*
  • Genetic Therapy / methods
  • Humans
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / pharmacology
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / therapeutic use
  • Hyperlipoproteinemia Type I / therapy
  • Hyperlipoproteinemia Type II / drug therapy
  • Hypolipidemic Agents / therapeutic use*
  • Risk Factors
  • Stroke / etiology
  • Stroke / mortality
  • Stroke / prevention & control

Substances

  • Cholesterol, LDL
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors
  • Hypolipidemic Agents