(1) Rosuvastatin (Crestor(TM)) is a new synthetic agent for the treatment and prevention of lipid disorders, a risk factor for coronary heart disease. (2) Rosuvastatin is undergoing phase III clinical trials. A New Drug Application was submitted to the U.S. Food and Drug Administration in June, 2001. No information on the regulatory status in Canada is currently available. (3) Limited evidence ...

Objectives. This study compared the effects of rosuvastatin on left ventricular infarct size in mice following permanent coronary occlusion versus 60 minutes ischemia/24 hours reperfusion and evaluated the effects of rosuvastatin on potential beneficial mechanisms of infarct size reduction including neutrophil accumulation, NO synthase expression and stem cell mobilization following ischemia an...

Background and objective: Many clinical trials have revealed that HMG-CoA reductase inhibitors (statins) anti-inflammatory effects through their pleiotropic activities there by decreasing the risk of cardiovascular disease (CVD). This study intended to evaluate effect rosuvastatin on level inflammatory markers (hsCRP, IL-6, sCD40L, Lp-PLA2, cystatin C) in normotensive hypertensive rats. Methods...

The aim of study was to investigate the anti-proliferative and inflammatory effects atorvastatin, rosuvastatin, simvastatin in lung cancer. statins were investigated Vero, BEAS-2B, A549 cell lines. In addition expressions BAX, BCL-2, TNFα, IL-10, IL-6, protein levels IL-6 determined. Cell viability MDA also measured. While numbers groups with low doses found be approximately 1x106/mL, prolifera...

Rosuvastatin is a widely prescribed antihyperlipidemic which undergoes limited metabolism, but is an in vitro substrate of multiple transporters [organic anion transporting polypeptide 1B1 (OATP1B1), OATP1B3, OATP1A2, OATP2B1, sodium-taurocholate cotransporting polypeptide, breast cancer resistance protein (BCRP), multidrug resistance protein 2 (MRP2), MRP4, organic anion transporter 3]. It is ...

The intestinal efflux transporter breast cancer resistance protein (BCRP) restricts the absorption of rosuvastatin. Of the transporters important to rosuvastatin disposition, fostamatinib inhibited BCRP (IC50 = 50 nM) and organic anion-transporting polypeptide 1B1 (OATP1B1; IC50 > 10 μM), but not organic anion transporter 3, in vitro, predicting a drug-drug interaction (DDI) in vivo through inh...

The hepatobiliary transport and local disposition of rosuvastatin in pig were investigated, along with the impact of concomitant dosing with two known multiple transport inhibitors; cyclosporine and gemfibrozil. Rosuvastatin (80 mg) was administered as an intrajejunal bolus dose in treatments I, II, and III (TI, TII, and TIII, respectively; n = 6 per treatment). Cyclosporine (300 mg) and gemfib...

OBJECTIVE Dysregulated apolipoprotein (apo)C-III metabolism may account for hypertriglyceridemia and increased cardiovascular risk in the metabolic syndrome. This study investigated the dose-dependent effect of rosuvastatin on VLDL apoC-III transport in men with the metabolic syndrome. RESEARCH DESIGN AND METHODS Twelve men with the metabolic syndrome were studied in a randomized double-blind...

OBJECTIVE It is controversial whether statins improve high-density lipoprotein (HDL) function, which plays an important role in reverse cholesterol transport in vivo. The aim of the present study was to clarify the effects of rosuvastatin and atorvastatin on reverse cholesterol transport in macrophage cells in vivo and their underlying mechanisms. APPROACH AND RESULTS Male C57BL mice were div...

Studies have demonstrated that the acute administration of 3-hydroxy-3 methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors has protective effects in the setting of ischemia-reperfusion (IR). Previously, we demonstrated that a single dose of rosuvastatin prevented IR-induced endothelial dysfunction in humans through a cyclooxygenase-2-dependent mechanism. Whether the chronic administration ...