Drug intelligence / Profile preview

rosuvastatin

Development stage
Approved
Lead developer
AstraZeneca
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Rosuvastatin is a synthetic statin medication used to lower lipid levels and reduce the risk of cardiovascular disease, including myocardial infarction and stroke. It acts as a competitive inhibitor of the enzyme HMG-CoA reductase in the liver, which catalyzes an early rate-limiting step in cholesterol biosynthesis. By inhibiting this enzyme, rosuvastatin decreases hepatic cholesterol concentrations and upregulates hepatic LDL receptors, increasing uptake and breakdown of LDL cholesterol from the blood. This results in reduced plasma levels of total cholesterol, LDL-C (bad cholesterol), VLDL (very low-density lipoprotein), triglycerides, and increased HDL-C (good cholesterol). Rosuvastatin is indicated for hypercholesterolemia (including familial forms), mixed dyslipidemia, hypertriglyceridemia, prevention of cardiovascular disease events such as heart attack or stroke in high-risk individuals. The drug was originally developed by Shionogi and AstraZeneca[2][4][8].

Brand names
CrestorEzallorEzallor SprinkleRoszet
Other names
rosuvastatin calcium
02

Targets

HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)

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