The class
A review asks whether genomic analyses and post hoc trial insights can revive CETP inhibitors for cardiovascular prevention after past disappointments (Curr Opin Lipidol 2022)
Original title: Can we revive CETP-inhibitors for the prevention of cardiovascular disease?
This review examines recent developments in CETP inhibition from clinical trials and genomic analyses that could influence future clinical programs. CETP plays an important role in lipoprotein remodeling, and substantial evidence suggests low CETP activity should favorably affect lipid profiles and cardiovascular risk, yet several pharmacological CETP-inhibitor development programs proved disappointing, marked by toxicity and clinical futility, leading many to consider abandoning the strategy. The authors argue that recent genomic analyses and post hoc observations from prior clinical trials have provided greater insight into the relationship between CETP inhibition and cardiovascular risk, highlighting the importance of lowering atherogenic lipoproteins specifically. The review concludes these findings offer a pathway for ongoing clinical development of new CETP inhibitors that may still play a meaningful role in cardiovascular disease prevention.
Original abstract
Purpose Of Review: To review recent developments in the field of cholesteryl ester transfer protein (CETP) inhibition from clinical trials and genomic analyses which have the potential to impact future clinical programs.
Recent Findings: CETP plays an important role in remodelling of lipoproteins. A large body of evidence suggests that the presence of low CETP activity should have favourable effects on lipid profiles and cardiovascular risk. However, a number of clinical development programs of pharmacological CETP inhibitors have been disappointing with reports of toxicity and clinical futility. These findings have led many to consider abandoning CETP inhibition as a potential strategy for cardiovascular prevention. However, recent observations from genomic analyses and post hoc observations of prior clinical trials have given greater insights into the potential relationship between CETP inhibition and cardiovascular risk. This has highlighted the importance of lowering levels of atherogenic lipoproteins.
Summary: These findings provide a pathway for ongoing clinical development of CETP inhibitors, where the potential to play an important role in the prevention of cardiovascular disease may still be possible. The lessons learned and pathway forward for new CETP inhibitors will be reviewed.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.