Do structural differences in statins correlate with clinical efficacy?

• Published in: Current opinion in lipidology Vol. 21; no. 4; p. 298
• Main Authors: Arnaboldi, Lorenzo, Corsini, Alberto
• Format: Journal Article
• Language: English
• Published: England 01.08.2010
• Subjects: Acute Coronary Syndrome - drug therapy; Animals; Cardiovascular System - drug effects; Cardiovascular System - metabolism; Humans; Hydroxymethylglutaryl-CoA Reductase Inhibitors - chemistry; Hydroxymethylglutaryl-CoA Reductase Inhibitors - pharmacology; Hydroxymethylglutaryl-CoA Reductase Inhibitors - therapeutic use; Structure-Activity Relationship; Time Factors
• ISSN: 1473-6535
• DOI: 10.1097/MOL.0b013e32833b776c

Statins, by inhibiting 3-hydroxy-3-methylglutaryl-coenzyme A reductase, decrease the synthesis not only of cholesterol but also of nonsteroidal mevalonate derivatives. While the first effect translates into plasma cholesterol reductions, the second is related to nonlipid-lowering (pleiotropic) properties. Purpose of this review is to assess the correlation between differences in statin structures and clinical effects. While the cardiovascular benefits of statin chronic therapy are achieved by lowering low-density lipoprotein cholesterol (LDL-C) and should be considered a class effect, the acute ones may reflect structure differences and pleiotropic properties of these drugs. Clinical studies conducted in acute coronary syndrome patients suggest that some benefits achieved by early statin treatment could be related to their pleiotropic properties. Indeed, ex-vivo studies showed the ability of sera from hypercholesterolemic patients treated with a single dose of atorvastatin (but not of simvastatin), to inhibit smooth muscle cell proliferation, independently of LDL-C lowering. These findings give a clinical ground to statins' potentially structure-related anti-inflammatory and pleiotropic properties, opening the possibility to control different aspects of atherosclerosis, by choosing the appropriate statin (tailored therapy), particularly in high-cardiovascular-risk patients.