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History And Development Of HMG-CoA Reductase Inhibitors

S. Bellosta, R. Paoletti, A. Corsini
Published 2002 · Medicine

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Coronary heart disease (CHD) is the leading cause of mortality in Western countries [1, 2]. A strong, positive correlation between high levels of plasma total and low-density lipoprotein (LDL) cholesterol and CHD is well established [3]. Dietary and/or pharmacological approaches aimed at lowering elevated plasma LDL appears therefore to be a logical intervention to reduce incidence of CHD or even reversing the development of coronary atherosclerosis [1, 4, 5, 6, 7, 8]. A number of cholesterol-lowering drugs are currently available for human use [1, 2, 9]. Among these, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors, the so-called statins: atorvastatin, cerivastatinl, fluvastatin, pitavastatin, pravastatin, lovastatin, rosuvastatin and simvastatin, can achieve relatively large reductions in plasma cholesterol levels and are a well-established class of drugs for the treatment of hypercholesterolemia [10]. Clinical trials have demonstrated that they can induce regression of vascular atherosclerosis, as well as reduction of cardiovascular-related morbidity and mortality, in patients with and without coronary artery disease CAD [11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21]. These trials provide a powerful endorsement of the value of lipid-lowering therapy with a statin in patients who are at risk for CAD.
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