NYMC Faculty Publications

Anacetrapib: A Potential New Therapy for Dyslipidemia

Author Type(s)

Faculty

Journal Title

Cardiology in Review

First Page

253

Last Page

261

Document Type

Article

Publication Date

1-1-2014

Department

Pharmacology

Keywords

Anticholesteremic Agents, Cholesterol Ester Transfer Proteins, Cholesterol, HDL, Dyslipidemias, Humans, Oxazolidinones

Disciplines

Medicine and Health Sciences

Abstract

Anacetrapib is a cholesteryl ester transfer protein (CETP) inhibitor currently in Phase III of development as a treatment for those with dyslipidemia and the risk of cardiovascular disease. The agent acts by inhibiting the CETP, which mediates the transfer of cholesterol esters from high-density lipoprotein cholesterol (HDL-C) to other lipoproteins. HDL-C has been inversely linked to cardiac risk and is thus a potential target for decreasing residual cardiovascular risk, which remains despite aggressive low-density lipoprotein cholesterol therapy with statin drugs. Anacetrapib has been shown to raise HDL-C by up to 138% and decrease low-density lipoprotein cholesterol by up to 39% compared with placebo. The HDL-C molecules treated with anacetrapib have also been shown to retain their function in cholesterol efflux and reverse cholesterol transport and their anti-inflammatory properties. Unlike the previously tested CETP inhibitor torcetrapib, anacetrapib has not been shown to elevate blood pressure, alter electrolytes, or cause any significant side effects. Future studies will determine whether these alterations in the lipid profile decrease the cardiovascular risk of morbidity and mortality. If these studies show promising results, anacetrapib could become a vital pharmacologic therapy for decreasing cardiovascular risk in patients.

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