Simvastatin is a competitive inhibitor of HMG-CoA reductase (K
i = 0.12 nM).
1 Simvastatin reduces plasma cholesterol levels in rats and dogs when administered at doses of 1.2 and 8 mg/kg, respectively.
2 Simvastatin suppresses TNF-induced NF-κB activation (IC
50 =
~13 μM) and potentiates apoptosis in human myeloid leukemia cells.
3 It also inhibits glutathione peroxidase 4 (GPX4) activity, increases malondialdehyde (MDA) levels, and induces ferroptosis in MDA-MB-231 and MCF-7 breast cancer cells.
4 Formulations containing simvastatin have been used in the treatment of dyslipidemias.