evacetrapib and Coronary-Disease

evacetrapib has been researched along with Coronary-Disease* in 1 studies

Other Studies

1 other study(ies) available for evacetrapib and Coronary-Disease

ArticleYear
Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.
    Journal of medicinal chemistry, 2021, 09-23, Volume: 64, Issue:18

    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.

    Topics: Animals; Anticholesteremic Agents; Cholesterol Ester Transfer Proteins; Coronary Disease; Dogs; Humans; Macaca mulatta; Mice, Inbred C57BL; Molecular Structure; Oxazolidinones; Rats, Wistar; Structure-Activity Relationship

2021