Simvastatin sodium is a lactone prodrug, can be hydrolysed to active hydroxy-acid by non-specific carboxyesterases or non-enzymatic processes. Simvastatin sodium shows a inhibition of HMG-CoA reductase with a K_i value of 0.12 nM^[1][2]. In Vitro: Simvastatin sodium shows a inhibition of HMG-CoA reductase in human lymphoblasts and SV40 transformed MRCS fibroblasts^[1].
Simvastatin sodium (100 μM) inhibits the Na⁺/H⁺ antiport activity leading to a fall of intracellular pH and to a reduced cell proliferation.And the inhibitory effect is prevented by mevalonate but not dolichol or squalene^[1].
In Vivo: Simvastatin sodium (oral administration; 8 mg/kg; 18 days) reduces plasma cholesterol levels 33%, simvastatin can be used in combination with ezetimibe to treat dyslipidemia^[1].