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Antihyperlipidemic Agents

  1. Michael L. Sierra

Published Online: 15 JAN 2003

DOI: 10.1002/0471266949.bmc047

Burger's Medicinal Chemistry and Drug Discovery

Burger's Medicinal Chemistry and Drug Discovery

How to Cite

Sierra, M. L. 2003. Antihyperlipidemic Agents. Burger's Medicinal Chemistry and Drug Discovery. 339–383.

Author Information

  1. Centre de Recherches, Laboratoire GlaxoSmithKline, Les Ulis, France

Publication History

  1. Published Online: 15 JAN 2003


Coronary heart disease (CHD) is the leading cause of morbidity and mortality in developed nations and atherosclerotic cardiovascular disease accounts for approximately half of all deaths attributed to CHD. Dyslipidemia, including hypercholesterolemia, hypertriglyceridemia, and hypoalphalipoproteinemia, is a major risk factor for CHD. Clinical studies have demonstrated the link between elevated serum cholesterol and coronary disease. Randomized controlled studies investigating the benefit of therapies that lower serum levels of low density lipoprotein cholesterol have demonstrated improvements in coronary morbidity and mortality in patients with or without diagnosed CHD. Furthermore, data are accumulating based on the VA-HIT trial and several other ongoing trials with fibrates that the treatment of high serum triglycerides and low concentrations of high density lipoprotein cholesterol can also lead to improvements in coronary morbidity and mortality. This review discusses the development of the HMG-CoA reductase inhibitors and how they have, thanks to their excellent efficacy and good safety profile, revolutionized the clinical management of hypercholesterolemia. Other treatments such as fibrates, bile acid sequestrants, cholesterol absorption inhibitors, and nicotinic acid derivatives as well as new emerging treatments are also discussed.


  • cardiovascular disease;
  • atherosclerosis;
  • myocardial infarction;
  • dyslipidemia;
  • hypercholesterolemia;
  • hypertriglyceridemia;
  • LDL cholesterol;
  • HDL cholesterol;
  • triglycerides;
  • HMG-CoA reductase inhibitors;
  • fibric acid derivatives;
  • bile acid sequestrants;
  • cholesterol absorption inhibitors;
  • nicotinic acid;
  • statins;
  • fibrates;
  • lipid-lowering drugs