Drug intelligence / Profile preview

simvastatin acid

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

**Simvastatin acid** is the pharmacologically active form of simvastatin, a statin medication used primarily to lower blood cholesterol and reduce the risk of cardiovascular events. Simvastatin acid acts as a competitive inhibitor of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, the rate-limiting step in hepatic cholesterol biosynthesis. Simvastatin is administered as an inactive lactone prodrug (simvastatin), which is hydrolyzed in vivo to simvastatin acid; this open-acid form is the direct inhibitor of HMG-CoA reductase responsible for the drug’s lipid-lowering effects[4][5].

Other names
simvastatin beta-hydroxyacidsimvastatin hydroxy acidsimvastatin active formsimvastatin open acidsimvastatin β-hydroxyacid
02

Targets

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

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