Rosuvastatin Calcium is a lipid-regulating drug belonging to the class of HMG-CoA (β-hydroxy-β-methylglutaryl-coenzyme A) reductase inhibitors. It is primarily used in the treatment of hyperlipidemia and hypercholesterolemia.
By inhibiting HMG-CoA reductase, it reduces cholesterol synthesis, thereby lowering plasma cholesterol and lipoprotein levels.
Pharmacological and Toxicological Properties
The inhibitory effect of Rosuvastatin Calcium on HMG-CoA reductase has been studied in rat and human liver microsomes as well as in cloned and purified human HMG-CoA reductase fragments.
Studies have shown that Rosuvastatin Calcium is more potent than existing statins and exhibits higher affinity for the human enzyme at its active site.
Its enzyme inhibition is reversible and competitive with the substrate HMG-CoA, not with the common substrate nicotinamide-adenine dinucleotide phosphate (NADPH).