Novel HDL-based therapeutic agents

Pharmacol Ther. 2012 Jul;135(1):18-30. doi: 10.1016/j.pharmthera.2012.03.004. Epub 2012 Mar 23.

Abstract

Reduction in low-density lipoprotein cholesterol (LDL-C) levels has been associated with a 25-30% reduction in cardiovascular disease risk. However, there still remains a significant and quantifiable risk. Since epidemiologic data have demonstrated that low levels of high-density lipoprotein cholesterol (HDL-C) are associated with an increased risk for cardiovascular disease, novel therapeutic agents are currently being developed to either raise HDL-C levels or enhance HDL functionality. This review will highlight some of these therapeutic agents including cholesteryl ester transfer protein inhibitors, apolipoprotein A-I mimetics, RVX-208, and apolipoprotein A-I based infusion therapies. For each therapeutic class, an overview of the mechanism of action, pharmacokinetic data, and efficacy/safety evidence will be provided.

Publication types

  • Review

MeSH terms

  • Animals
  • Apolipoprotein A-I / therapeutic use
  • Biomarkers / blood
  • Cardiovascular Diseases / blood
  • Cardiovascular Diseases / etiology
  • Cardiovascular Diseases / prevention & control*
  • Cholesterol Ester Transfer Proteins / antagonists & inhibitors
  • Cholesterol Ester Transfer Proteins / blood
  • Cholesterol, HDL / blood*
  • Cholesterol, LDL / blood
  • Dyslipidemias / blood
  • Dyslipidemias / complications
  • Dyslipidemias / drug therapy*
  • Humans
  • Hypolipidemic Agents / adverse effects
  • Hypolipidemic Agents / pharmacokinetics
  • Hypolipidemic Agents / therapeutic use*
  • Molecular Mimicry
  • Quinazolines / therapeutic use
  • Quinazolinones
  • Treatment Outcome

Substances

  • Apolipoprotein A-I
  • Biomarkers
  • CETP protein, human
  • Cholesterol Ester Transfer Proteins
  • Cholesterol, HDL
  • Cholesterol, LDL
  • Hypolipidemic Agents
  • Quinazolines
  • Quinazolinones
  • apabetalone