The class
Unlike torcetrapib, dalcetrapib, evacetrapib, and anacetrapib do not raise blood pressure or aldosterone (Curr Opin Lipidol 2012)
Original title: Safety of CETP inhibition
In 2007, torcetrapib unexpectedly showed increased fatality and cardiovascular events, possibly linked to its off-target effects raising blood pressure and aldosterone levels, prompting scrutiny of the safety of all CETP-inhibiting drugs. This review finds that the novel CETP inhibitors dalcetrapib, evacetrapib, and anacetrapib did not show harmful effects on blood pressure or aldosterone. Ultrasound brachial artery flow-mediated vasodilation, carotid MRI, and 18F-fluorodeoxyglucose PET imaging studies found dalcetrapib had neither harmful nor beneficial effects on endothelial function, atherosclerosis progression, or vessel wall inflammation, and its clinical endpoint study was subsequently terminated early after an interim analysis showed a lack of clinically meaningful efficacy. The review concludes that CETP inhibition itself appears well tolerated, without the torcetrapib-specific adverse effects, though clinical benefit remained unproven pending the phase III anacetrapib study.
Original abstract
Purpose Of Review: Cholesteryl ester transfer protein (CETP)-inhibiting drugs effectively raise HDL cholesterol. In 2007, the CETP inhibitor torcetrapib unexpectedly showed increased fatality and cardiovascular events, possibly related to increased blood pressure and aldosterone levels caused by torcetrapib. Since then, novel CETP inhibiting drugs have been investigated. This review will discuss the safety of the CETP-inhibiting drugs.
Recent Findings: The novel CETP inhibitors dalcetrapib, evacetrapib and anacetrapib did not show harmful effects on blood pressure or aldosterone levels. Ultrasound brachial artery flow-mediated vasodilation, carotid MRI and (18)F-fluordeoxyglucose PET imaging studies, showed that dalcetrapib therapy had neither harmful nor beneficial effects on endothelial function, atherosclerosis progression, or vessel wall inflammation. Recently, the clinical endpoint study investigating dalcetrapib was announced to be terminated early, after the second interim analysis showed that dalcetrapib lacked clinically meaningful efficacy.
Summary: Dalcetrapib, evacetrapib and anacetrapib did not show the harmful effects on aldosterone and blood pressure that were exhibited by torcetrapib, indicating that CETP inhibition is well tolerated. So far CETP inhibition did not show beneficial effects on clinical outcome. The phase III study with anacetrapib will give final answers on whether CETP inhibition can reduce cardiovascular events.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.