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Lipid-lowering agents, also sometimes referred to as hypolipidemic agents, cholesterol-lowering drugs, or antihyperlipidemic agents are a diverse group of pharmaceuticals that are used to lower the level of lipids and lipoproteins, such as cholesterol, in the blood (hyperlipidemia). The American Heart Association recommends the descriptor ...
ATC code C10 Lipid modifying agents is a therapeutic subgroup of the Anatomical Therapeutic Chemical Classification System, a system of alphanumeric codes developed by the World Health Organization (WHO) for the classification of drugs and other medical products. [1] [2] [3] Subgroup C10 is part of the anatomical group C Cardiovascular system. [4]
Low-density lipoprotein (LDL) carriers of cholesterol play a key role in the development of atherosclerosis and coronary heart disease via the mechanisms described by the lipid hypothesis. As lipid-lowering medications, statins are effective in lowering LDL cholesterol; they are widely used for primary prevention in people at high risk of ...
Managing cholesterol at the site of absorption is an increasingly popular strategy in the treatment of hypercholesterolemia [citation needed].Cholesterol absorption inhibitors are known to have a synergistic effect when combined a class of antihyperlipidemics called statins, to achieve an overall serum cholesterol target.
Drugs in this class substantially increase HDL cholesterol, lower LDL cholesterol, and enhance reverse cholesterol transport. [citation needed]CETP inhibitors inhibit cholesterylester transfer protein (CETP), which normally transfers cholesterol from HDL cholesterol to very low density or low density lipoproteins (VLDL or LDL).
This enzyme is the target of the widely available cholesterol-lowering drugs known collectively as the statins, which help treat dyslipidemia. HMG-CoA reductase is anchored in the membrane of the endoplasmic reticulum , and was long regarded as having seven transmembrane domains, with the active site located in a long carboxyl terminal domain ...
Figure 1: Lanosterol synthase mechanism. The discrete carbocation intermediates show the non-concerted nature of the mechanism. Though some data on the mechanism has been obtained by the use of suicide inhibitors, mutagenesis studies, and homology modeling, it is still not fully understood how the enzyme catalyzes the formation of lanosterol.
Following up from that study the researchers explored a novel way to lower blood cholesterol levels without modifying the diet and lifestyle of subjects suffering with elevated blood cholesterol levels. The primary goal was to inhibit the cholesterol biosynthesis in the body. Hence HMG-CoA reductase (HMGR) became a natural target.