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Updated: Jun 22, 2026
07:54
Cholesterol Efflux Assay
Published on: March 6, 2012
Cholesteryl ester transfer protein (CETP) inhibitors
1Merck Research Laboratories, Rahway, NJ 07065, USA. julianne_hunt@merck.com
Current Topics in Medicinal Chemistry
|June 13, 2009
Summary
Inhibiting cholesteryl ester transfer protein (CETP) increases high-density lipoprotein cholesterol (HDL-C). While this boosts HDL-C levels, its impact on reducing coronary heart disease (CHD) requires further investigation.
Area of Science:
- Cardiovascular Medicine
- Lipid Metabolism
- Pharmacology
Background:
- Epidemiological studies show lower high-density lipoprotein cholesterol (HDL-C) correlates with higher coronary heart disease (CHD) incidence.
- Cholesteryl ester transfer protein (CETP) facilitates lipid transfer from HDL to apoB lipoproteins.
- Targeting CETP is a strategy to elevate HDL-C levels.
Purpose of the Study:
- To review the role of CETP in lipid metabolism.
- To discuss recent advancements in small-molecule CETP inhibitors.
- To explore the future potential of CETP inhibitors for CHD treatment.
Main Methods:
- Review of epidemiological data on HDL-C and CHD.
- Analysis of CETP function in lipid transfer.
- Examination of pharmacological CETP inhibition studies in humans.
Main Results:
- CETP inhibition demonstrably increases plasma HDL-C concentrations.
- Pharmacological inhibition of CETP in humans leads to elevated HDL-C levels.
- The clinical benefit of CETP inhibition on reducing CHD incidence remains to be established.
Conclusions:
- CETP plays a complex role in regulating lipid profiles.
- Small-molecule inhibitors offer a promising avenue for modulating CETP activity.
- Further research is needed to confirm the efficacy of CETP inhibitors in preventing cardiovascular events.
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