Fluvastatin sodium is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonic acid. Fluvastatin markedly inhibits the formation of thiobarbituric acid reactive substances in iron (II)-supported peroxidation of liposomes with IC50 of 12 μM. Fluvastatin sodium inhibits vascular smooth muscle proliferation in vitro (IC50 = 70 nM) and exhibits antihypercholesterolemic and antioxidant activity in vivo. When fluvastatin was administered in a clinical trial to patients undergoing percutaneous coronary intervention, LDL cholesterol levels were reduced by 27% after six weeks of treatment with a dose of 40 mg/kg twice a day compared to placebo. Fluvastatin sodium is antilipemic and is used to reduce plasma cholesterol levels and prevent cardiovascular disease. Fluvastatin is currently in a phase IV clinical trial in patients with Metabolic Syndrome.
Pak J Pharm Sci. 2016 May;29(3 Suppl):1043-51.
Chromatographic resolution of drug analogues: 3-hydroxy-3-methylglutarylcoenzyme A reductase inhibitors (statins)
Fluvastatin sodium purchased from AbMole
|Source||Pak J Pharm Sci (2016). Figure 1. Fluvastatin sodium (Abmole Bioscience)|
|Results||The results summarized in (table 1) obtained for pravastatin, rosuvastatin, pitavastatin, atorvastatin, fluvastatin, lovastatin and simvastatin were comparable with the corresponding labeled amounts.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 80 mg/mL|
Antioxidative effect of fluvastatin, an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase, on peroxidation of phospholipid liposomes.
Yamamoto A, et al. J Pharm Pharmacol. 2001 Feb;53(2):227-32. PMID: 11273020.
HMG-CoA reductase activity in human liver microsomes: comparative inhibition by statins.
Dansette PM, et al. Exp Toxicol Pathol. 2000 May;52(2):145-8. PMID: 10965989.
|Related HMG-CoA Reductase Products|
Atorvastatin is an inhibitor of HMG-CoA reductase used as a cholesterol-lowering medication that blocks the production of cholesterol.
Atorvastatin Calcium is an inhibitor of HMG-CoA reductase used as a cholesterol-lowering medication that blocks the production of cholesterol.
Clinofibrate inhibits hydroxymethylglutaryl coenzyme A reductase (HMGCR) with IC50 of 0.47 mM, is a lipid-lowering agent used for controlling high cholesterol and triacylglyceride levels in the blood.
Pravastatin sodium is an HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM.
Lovastatin is an inhibitor of HMG-CoA reductase with IC50 of 3.4 nM in a cell-free assay, used for lowering cholesterol (hypolipidemic agent).
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