LCAT Inhibitors

Inhibitors of LCAT (Lecithin-Cholesterol Acyltransferase) mainly involve compounds that influence cholesterol and lipid metabolism, thereby indirectly modulating LCAT activity. LCAT plays a pivotal role in the esterification of cholesterol and is integral to the process of reverse cholesterol transport. Compounds such as Anacetrapib, Torcetrapib, Dalcetrapib, and Evacetrapib are CETP (Cholesteryl Ester Transfer Protein) inhibitors. While their primary action is to inhibit CETP, they may indirectly affect LCAT function by altering the dynamics of cholesterol and lipoprotein metabolism, particularly impacting HDL cholesterol levels.

Statins, such as Atorvastatin, and other lipid-lowering agents like Fenofibrate and Gemfibrozil, work by modulating lipid levels. Their action can indirectly influence LCAT activity by altering cholesterol homeostasis and potentially affecting the availability of substrates for esterification. Niacin and Ezetimibe have distinct mechanisms - Niacin improves overall lipid profiles, particularly increasing HDL cholesterol, while Ezetimibe reduces intestinal cholesterol absorption. Both may have indirect effects on LCAT activity due to changes in cholesterol levels and distribution. Omega-3 Fatty Acids, known for their beneficial effects on lipid profiles, could indirectly modulate LCAT function by altering lipid composition and membrane characteristics. Polyphenols, like Resveratrol, with their antioxidative properties, might also impact LCAT indirectly through effects on lipid metabolism and oxidative stress.