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Updated: Mar 26, 2026
07:54
Cholesterol Efflux Assay
Published on: March 6, 2012
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Cholesteryl Ester Transfer Protein Inhibition Is Not Yet Dead--Pro
Philip J Barter1, Kerry-Anne Rye2
1From the School of Medical Sciences, University of New South Wales, Sydney, Australia. pbarter@ozemail.com.au p.barter@unsw.edu.au.
Arteriosclerosis, Thrombosis, and Vascular Biology
|February 6, 2016
Summary
Cholesteryl ester transfer protein (CETP) inhibition may lower cardiovascular disease risk. While past trials failed, ongoing studies will determine if CETP inhibitors offer cardio-protection.
Area of Science:
- Cardiovascular Science
- Lipid Metabolism
- Pharmacology
Background:
- Cholesteryl ester transfer protein (CETP) facilitates lipid transfer between lipoproteins.
- Genetic and cohort studies link reduced CETP activity to lower atherosclerotic cardiovascular disease (ASCVD) risk.
- CETP inhibition in animal models reduces atherosclerosis.
Purpose of the Study:
- To evaluate the potential of CETP inhibition as a cardio-protective strategy.
- To assess the impact of CETP inhibition on lipid profiles and ASCVD risk.
- To address the uncertainty surrounding CETP inhibition efficacy due to previous trial failures.
Main Methods:
- Analysis of human genetic and cohort studies.
- Review of animal studies on CETP inhibition.
- Examination of human clinical trials investigating CETP inhibitors.
- Consideration of the ongoing REVEAL trial design.
Main Results:
- Human genetic data suggest CETP polymorphisms are associated with reduced ASCVD risk.
- CETP inhibition in humans alters lipid profiles, lowering non-HDL cholesterol and raising HDL cholesterol.
- Previous randomized clinical trials with CETP inhibitors have failed to demonstrate efficacy.
Conclusions:
- The hypothesis that CETP inhibition reduces ASCVD risk remains to be definitively tested.
- Previous trial failures may be attributed to off-target effects or trial design issues.
- The outcome of the REVEAL trial is critical for determining the future of CETP inhibition for cardio-protection.
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