Small molecule
PubChem CID 54454
Simvastatin
Zocor
- Mechanism of action
- HMG-CoA reductase inhibitor
- In plain language
- Blocks a liver enzyme your body uses to make cholesterol, prompting the liver to pull more “bad” cholesterol out of your bloodstream.
- How it works
- Simvastatin is a prodrug hydrolyzed to its active form, simvastatin acid, which competitively inhibits HMG-CoA reductase, the rate-limiting enzyme converting HMG-CoA to mevalonate in the cholesterol biosynthesis pathway. Reduced hepatic cholesterol synthesis upregulates LDL-receptor expression on hepatocytes, increasing clearance of circulating LDL cholesterol from plasma. This also lowers total cholesterol and VLDL levels. Maximal LDL-C reduction is typically reached within about four weeks of consistent dosing.
- Therapeutic applications
- Indicated to reduce the risk of coronary heart disease death, non-fatal myocardial infarction, stroke, and revascularization in adults at high cardiovascular risk; as an adjunct to diet to reduce elevated LDL-C in adults with primary hyperlipidemia and in pediatric patients 10 and older with heterozygous familial hypercholesterolemia; and as adjunctive therapy in homozygous familial hypercholesterolemia and other lipid disorders.
- Class
- Small molecule
- Therapeutic area
- Cardiovascular
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