Unlike torcetrapib, anacetrapib raises HDL-C by 138% without elevating blood pressure or disturbing electrolytes (Cardiol Rev 2014)

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.