Background:

Mevastatin is an inhibitor of HMG-CoA reductase with Ki value of 1nM [1].

Mevastatin inhibits HMG-CoA reductase reversibly and competes with HMG-CoA. It shows a Ki value of about 1nM. Mevastatin inhibits sterol synthesis from acetate in various cells at low concentration of nanomolar. It also inhibits acetate incorporation with IC50 value of 1nM. Besides that, mevastatin completely suppresses the growth of L cells at 1.3μM. Mevastatin is also found to affect the cell cycle and change cell morphology in cultured fibroblasts [1].

In rats, administration of mevastatin inhibits sterol synthesis in the liver and reduces plasma cholesterol levels. In patients with familial hypercholesterolemia, mevastatin also shows potent effects on reducing plasma cholesterol. Mevastatin at dose of 50 mg/day reduces 25% total cholesterol in a FH heterozygote patient treated with 2 months [1].

参考文献:
[1] Endo A. The discovery and development of HMG-CoA reductase inhibitors. Journal of lipid research, 1992, 33(11): 1569-1582.