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CETP Inhibitors: Back With a New Target.
Stephen J Nicholls1, Kausik K Ray2, Adam J Nelson1,3
1Victorian Heart Institute, Monash University, Clayton, Australia (S.J.N., A.J.N.).
Circulation Research
|June 4, 2026
Summary
Cholesteryl ester transfer protein (CETP) inhibitors show promise for reducing cardiovascular disease risk by lowering atherogenic lipids and improving glycemic control, not just by raising HDL cholesterol.
Area of Science:
- Lipid metabolism and cardiovascular disease research.
- Pharmacological intervention targeting CETP.
- Neurodegenerative disease biomarker investigation.
Background:
- Cholesteryl ester transfer protein (CETP) is crucial for lipid metabolism, with low CETP levels linked to reduced cardiovascular disease, diabetes, and neurodegeneration.
- Previous CETP inhibitor development faced challenges including toxicity and limited efficacy.
- Genomic studies and re-evaluation of prior programs suggest a new therapeutic pathway for CETP inhibitors.
Purpose of the Study:
- To review the evolving understanding of CETP inhibition for therapeutic benefit.
- To highlight the potential of selective CETP inhibitors like obicetrapib.
- To explore applications beyond cardiovascular risk reduction, including neurodegeneration.
Main Methods:
- Review of genetic and cohort studies on CETP function and its association with disease.
- Analysis of outcomes from previous pharmacological CETP inhibitor development programs.
- Examination of preclinical data for novel selective CETP inhibitors, such as obicetrapib.
Main Results:
- Low CETP activity is associated with protection against cardiovascular disease, diabetes, and neurodegeneration.
- Selective CETP inhibition, exemplified by obicetrapib, demonstrates favorable effects on atherogenic lipids, lipoproteins, and glycemic control.
- Obicetrapib also shows positive impacts on biomarkers related to Alzheimer disease pathology in preclinical models.
Conclusions:
- CETP inhibition offers a promising strategy for cardiovascular risk reduction through improved lipid profiles and glycemic control.
- Selective CETP inhibitors represent a refined approach to drug development in this class.
- Emerging evidence suggests broader therapeutic potential for CETP inhibition in areas like neurodegenerative diseases.
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