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Multiple Choice

What is the mechanism of action of inclisiran?

Inclisiran uses RNA interference to silence PCSK9 gene expression in the liver. By reducing PCSK9 production, less PCSK9 protein is available to bind and promote the degradation of LDL receptors on hepatocytes. With more LDL receptors remaining on the liver surface, they can bind and clear more LDL cholesterol from the bloodstream, leading to lower LDL-C levels. This direct mechanism is distinct from what statins do (inhibit HMG-CoA reductase, lowering cholesterol synthesis) or ezetimibe (block intestinal cholesterol absorption). The increase in LDL receptor activity is a downstream consequence of lowering PCSK9, but the primary action of inclisiran is inhibition of PCSK9 production.

Inclisiran uses RNA interference to silence PCSK9 gene expression in the liver. By reducing PCSK9 production, less PCSK9 protein is available to bind and promote the degradation of LDL receptors on hepatocytes. With more LDL receptors remaining on the liver surface, they can bind and clear more LDL cholesterol from the bloodstream, leading to lower LDL-C levels. This direct mechanism is distinct from what statins do (inhibit HMG-CoA reductase, lowering cholesterol synthesis) or ezetimibe (block intestinal cholesterol absorption). The increase in LDL receptor activity is a downstream consequence of lowering PCSK9, but the primary action of inclisiran is inhibition of PCSK9 production.