Mevastatin

Mevastatin is a competitive HMG-CoA reductase inhibitor (Ki = 0.1 µM). In vivo, mevastatin (50 mg/kg) inhibits cholesterogenesis in the liver and ileum of normolipidemic rats, as well as enhances suppression of cholesterogenesis in cholesterol-fed rats or rats administered cholestyramine. Mevastatin also suppresses TNF-induced NF-κB activation (IC50 = ~17 µM) and potentiates apoptosis in human myeloid leukemia cells. It also suppresses induced ferroptosis in HT-1080 cells. Formulations containing mevastatin have been used in the treatment of familial hypercholesterolemia.