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Cholesteryl ester transfer protein (CETP) inhibitors: is there life after torcetrapib?

Hemanth Neeli1, Daniel J Rader

  • 1Section of Hospital Medicine, Temple University Hospital, 1316 West Ontario Street, Philadelphia, PA 19140, USA.

Cardiology Clinics
|October 22, 2008
PubMed

Insights

Despite advances in coronary heart disease (CHD) management, researchers are exploring new treatments targeting high-density lipoprotein cholesterol (HDL-c). Novel CETP inhibitors may offer cardiovascular benefits by improving lipid profiles.

Area of Science:

  • Cardiovascular Medicine
  • Pharmacology
  • Lipid Metabolism

Background:

  • Coronary heart disease (CHD) remains a leading cause of mortality despite therapeutic advancements.
  • Low high-density lipoprotein cholesterol (HDL-c) is a recognized modifiable risk factor for CHD.
  • Previous attempts at HDL-targeted therapy, such as torcetrapib, faced setbacks due to off-target effects.

Purpose of the Study:

  • To re-evaluate the potential of cholesteryl ester transfer protein (CETP) inhibition as a therapeutic strategy for cardiovascular risk reduction.
  • To explore the possibility of developing 'clean' CETP inhibitors that improve plasma lipids without adverse effects.

Main Methods:

  • Review of existing literature on CETP inhibition and HDL-targeted therapies.
  • Analysis of the torcetrapib experience and its implications for future drug development.
  • Consideration of genetic CETP deficiency data.

Main Results:

  • The torcetrapib trial indicated substantial off-target effects that may have negated potential cardiovascular benefits.
  • Uncertainty persists regarding the precise cardiovascular implications of both genetic CETP deficiency and pharmacologic CETP inhibition.
  • The fundamental mechanism of CETP inhibition remains a plausible target for improving cardiovascular outcomes.

Conclusions:

  • Despite the challenges posed by torcetrapib, CETP inhibition is still considered a viable therapeutic approach.
  • Development of selective CETP inhibitors holds promise for improving lipid profiles and reducing cardiovascular risk.
  • Further research is warranted to elucidate the safety and efficacy of novel CETP inhibitors.

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