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Review updates the pipeline of emerging hyperlipidaemia drugs, focused mainly on anacetrapib and evacetrapib (Expert Opin Emerg Drugs 2014)

Original title: Emerging drugs for hyperlipidaemia: an update

Expert Opin Emerg Drugs · · 4

Florentin M, Kostapanos MS, Kei A, Elisaf MS

Although statins reduce cardiovascular morbidity and mortality by targeting LDL cholesterol, many cardiovascular events still occur, likely reflecting lipid abnormalities beyond high LDL-C or other unaddressed risk factors, since statins do not eliminate residual cardiovascular risk. This review updates developments since 2010 in lipid-modifying drugs, focusing primarily on cholesteryl ester transfer protein inhibitors, mainly anacetrapib and evacetrapib, alongside microsomal triglyceride transfer protein inhibitors, antisense oligonucleotides, PCSK9 inhibitors, and HDL mimetics. The authors conclude several novel agents may benefit specific patient populations but that ongoing and future clinical outcome studies will be needed to clarify their actual role in practice.

Read the paper (DOI)PubMed

Original abstract

Introduction: Hypercholesterolaemia is a significant risk factor for cardiovascular disease (CVD), a major cause of morbidity and mortality. Up to now, the appropriate management has been aggressive hypolipidaemic therapy, particularly with statins, aiming at certain low-density lipoprotein cholesterol (LDL-C) levels for each patient population. This strategy has reduced CVD-related morbidity and mortality. However, many cardiovascular events still occur, probably as a consequence of lipid disorders other than high LDL-C concentration or other risk factors. Because statins do not eliminate the residual CVD risk, there seems to be place for novel lipid modifying drugs with different mechanisms of action.

Areas Covered: This review is an update since 2010 regarding lipid-modifying drugs in development and their potent role in clinical practice. It focuses on cholesterol ester transfer protein inhibitors, mainly anacetrapib and evacetrapib, microsomal triglyceride transfer protein inhibitors, antisense oligonucleotides, pre-protein convertase subtilisin kexin-9 inhibitors and high-density lipoprotein mimetics.

Expert Opinion: Several novel lipid-modifying drugs may be beneficial for certain patient populations. However, ongoing and future studies with clinical outcomes will clarify their actual role in clinical practice.

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Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.