Lovastatin is an HMG-CoA reductase inhibitor that was initially isolated from A. terreus.1 It is a prodrug of its more potent metabolite, lovastatin hydroxy acid (Item No. 10010339). Both competitively inhibit HMG-CoA reductase with Ki values of 1.4 and 0.6 nM for lovastatin and the open ring, hydroxy acid form, respectively.2 Lovastatin (8 mg/kg/day) reduces plasma cholesterol in dogs by 29% over a three week period. It also suppresses TNF-induced NF-κB activation (IC50 ~ 15 µM), which potentiates apoptosis in human myeloid leukemia cells and thus, may be useful in treating cancer.3 Formulations containing lovastatin were the first HMG-CoA reductase inhibitors to be used in the treatment of hypercholesterolemia.
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