What is the mechanism of action of statins?

Statins function primarily by inhibiting the enzyme HMG-CoA reductase, which is a key player in the cholesterol biosynthesis pathway. This enzyme catalyzes the conversion of HMG-CoA to mevalonate, an early and rate-limiting step in the production of cholesterol in the liver. By blocking this enzyme, statins effectively lower the intracellular levels of cholesterol, which leads to an increase in LDL receptors on hepatocyte surfaces. This, in turn, enhances the clearance of circulating LDL cholesterol from the bloodstream, thereby reducing overall cholesterol levels and decreasing the risk of atherosclerotic cardiovascular diseases.

Understanding the mechanism of action is critical for comprehending the clinical use of statins in lowering cholesterol and mitigating cardiovascular risks, which is their primary therapeutic role.