Small molecule
PubChem CID 446157
Rosuvastatin
Crestor
- Mechanism of action
- HMG-CoA reductase inhibitor
- In plain language
- Lowers cholesterol by blocking a liver enzyme the body uses to make it, prompting the liver to pull more “bad” LDL cholesterol out of the bloodstream.
- How it works
- Rosuvastatin competitively inhibits HMG-CoA reductase, the rate-limiting enzyme in the hepatic mevalonate pathway that converts HMG-CoA to mevalonate, a cholesterol precursor. Reduced intracellular cholesterol synthesis upregulates hepatic LDL-receptor expression, increasing hepatic clearance and catabolism of circulating LDL cholesterol. This also modestly lowers triglycerides and raises HDL cholesterol. Maximal LDL-C reduction is typically achieved within about four weeks of consistent dosing.
- Therapeutic applications
- Indicated to reduce the risk of major adverse cardiovascular events in adults at increased CV risk; as an adjunct to diet and exercise to lower LDL-C in adults with primary hypercholesterolemia, to slow atherosclerosis progression, and in pediatric patients with familial hypercholesterolemia; and as an adjunct to diet for primary dysbetalipoproteinemia and hypertriglyceridemia.
- Class
- Small molecule
- Therapeutic area
- Cardiovascular
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