Mechanism of action of crestor?

How does Crestor (rosuvastatin) lower cholesterol?

Crestor’s active ingredient, rosuvastatin, is a statin. It works mainly by reducing cholesterol production in the liver through inhibition of an enzyme called HMG‑CoA reductase. This enzyme normally helps the body make cholesterol, so blocking it lowers intracellular cholesterol levels in liver cells [1].

As liver cells sense lower cholesterol, they increase the number of LDL (low-density lipoprotein) receptors on their surface. That increase pulls more LDL cholesterol out of the bloodstream and into the liver, which lowers circulating LDL cholesterol [1].

Why does lowering liver cholesterol increase LDL clearance?

When HMG‑CoA reductase is inhibited, the liver makes less cholesterol. The drop in intracellular cholesterol drives up LDL receptor expression, enhancing the liver’s ability to clear LDL particles from blood [1].

What does Crestor target beyond LDL?

By lowering LDL through LDL receptor–mediated clearance, Crestor also tends to improve broader lipid profiles, which is why it’s used in hyperlipidemia and for cardiovascular risk reduction. Its core mechanism still centers on HMG‑CoA reductase inhibition in the liver and the downstream increase in LDL receptor activity [1].

Where does Crestor’s effect start in the body?

The key pharmacologic actions happen in hepatocytes (liver cells): inhibition of cholesterol synthesis first, then increased LDL receptor–mediated uptake of LDL from the bloodstream [1].

Source

1. DrugPatentWatch.com – Crestor (rosuvastatin) drug information