Anacetrapib, a novel CETP inhibitor: pursuing a new approach to cardiovascular risk reduction

DE Gutstein, R Krishna, D Johns… - Clinical …, 2012 - Wiley Online Library
Cholesteryl ester transfer protein (CETP) inhibition is a promising experimental strategy to
raise high‐density lipoprotein cholesterol (HDL‐C) and reduce cardiovascular risk. This …

Anacetrapib: hope for CETP inhibitors?

R Gurfinkel, TR Joy - Cardiovascular therapeutics, 2011 - Wiley Online Library
Inhibition of cholesteryl ester transfer protein (CETP), a key protein involved in reverse
cholesterol transport, can lead to increases in high‐density lipoprotein cholesterol (HDL‐C) …

Invention of MK-8262, a cholesteryl ester transfer protein (CETP) inhibitor backup to anacetrapib with best-in-class properties

P Vachal, JL Duffy, LC Campeau… - Journal of Medicinal …, 2021 - ACS Publications
Cholesteryl ester transfer protein (CETP) represents one of the key regulators of the
homeostasis of lipid particles, including high-density lipoprotein (HDL) and low-density …

Cholesteryl ester transfer protein inhibitors for dyslipidemia: focus on dalcetrapib

AS Goldberg, RA Hegele - Drug design, development and therapy, 2012 - Taylor & Francis
Among the noteworthy recent stories in the management and prevention of atherosclerotic
cardiovascular disease (CVD) is the saga of the development of pharmacological inhibitors …

Cholesteryl ester transfer protein inhibition as a strategy to reduce cardiovascular risk

PJ Barter, KA Rye - Journal of lipid research, 2012 - ASBMB
Human and rabbit plasma contain a cholesteryl ester transfer protein (CETP) that promotes
net mass transfers of cholesteryl esters from high density lipoproteins (HDL) to other plasma …

Lipids, safety parameters, and drug concentrations after an additional 2 years of treatment with anacetrapib in the DEFINE study

AM Gotto Jr, U Kher, MS Chatterjee… - Journal of …, 2014 - journals.sagepub.com
Anacetrapib is a cholesteryl ester transfer protein (CETP) inhibitor that has previously been
shown to reduce low-density lipoprotein cholesterol (LDL-C) and raise high-density …

An update on the clinical development of dalcetrapib (RO4607381), a cholesteryl ester transfer protein modulator that increases HDL cholesterol levels

D Rhainds, BJ Arsenault, MR Brodeur… - Future Cardiology, 2012 - Taylor & Francis
CETP is the target of CETP inhibitors such as anacetrapib and the modulator dalcetrapib.
Both molecules have entered Phase III clinical trials, with the ultimate goal of reducing …

Systematic review of CETP inhibitors for increasing high-density lipoprotein cholesterol: where do these agents stand in the approval process?

BM Bishop - American Journal of Therapeutics, 2015 - journals.lww.com
The role that low levels of high-density lipoprotein cholesterol (HDL-C) plays in coronary
artery disease and ischemic heart disease is well established. As such, therapies targeting …

Cholesteryl ester transfer protein inhibitors: trials and tribulations

JH McLain, AJ Alsterda… - Journal of cardiovascular …, 2017 - journals.sagepub.com
The cholesteryl ester transfer protein (CETP) is a plasma protein that plays an important role
in the transfer of lipids between plasma lipoproteins. The CETP inhibitors have been widely …

Evacetrapib: another CETP inhibitor for dyslipidemia with no clinical benefit

VA Eyvazian, WH Frishman - Cardiology in review, 2017 - journals.lww.com
Evacetrapib is a cholesteryl ester transfer protein (CETP) inhibitor that has been recently
studied as a cholesterol modifying agent to reduce cardiovascular risk and mortality in high …