Key result
MK-8262, a novel CETP inhibitor, demonstrated preclinical and clinical safety and efficacy by increasing HDL and reducing LDL as biomarkers for reduced coronary heart disease risk.
Why the study?
Following clinical evidence that CETP inhibition reduces coronary heart disease risk, researchers sought to discover MK-8262 as a potentially best-in-class CETP inhibitor optimized against key clinical adverse effect profiles.
Does MK-8262 improve lipid profiles (HDL increase and LDL reduction) in preclinical and clinical models?
Does MK-8262 improve lipid profiles (HDL increase and LDL reduction) in preclinical and clinical models?
MK-8262 is a novel CETP inhibitor that demonstrates favorable safety and efficacy profiles in preclinical and early clinical studies by increasing HDL and reducing LDL.
Does not yet support clinical use of novel CETP inhibitors; leaves open translation of preclinical findings to CHD outcomes.
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 lipoprotein (LDL) particles. Epidemiological evidence correlates increased HDL and decreased LDL to coronary heart disease (CHD) risk reduction. This relationship is consistent with a clinical outcomes trial of a CETP inhibitor (anacetrapib) combined with standard of care (statin), which led to a 9% additional risk reduction compared to standard of care alone. We discuss here the discovery of MK-8262, a CETP inhibitor with the potential for being the best-in-class molecule. Novel in vitro and in vivo paradigms were integrated to drug discovery to guide optimization informed by a critical understanding of key clinical adverse effect profiles. We present preclinical and clinical evidence of MK-8262 safety and efficacy by means of HDL increase and LDL reduction as biomarkers for reduced CHD risk.
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Váchal et al. (2021) studied Coronary heart disease risk. MK-8262 was evaluated on Safety and efficacy by means of HDL increase and LDL reduction. MK-8262, a novel CETP inhibitor, demonstrated preclinical and clinical safety and efficacy by increasing HDL and reducing LDL as biomarkers for reduced coronary heart disease risk.
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