Mevastatin

Overview
Mevastatin, compactin, ML-236B is a hypolipidemic agent that belongs to the statins class.

It was the first compound isolated in the 1970s during research into HMG-CoA reductase inhibitors produced by a mould Penicillium citrinum.

Nowadays, Mevastatin is not used in therapy of hyperlipidemias because of multiple side effects but it is the only source for production of other statin - pravastatin.

Mechanisms of Action
Mevastatin inhibits isoprenoid biosynthesis by inhibition of HMG-CoA reductase (Ki for acid form is 1 nM)1 and therefore blocks protein isoprenylation and reduces plasma cholesterol levels in humans. It causes cells to arrest early in the G1 phase.

Mevastatin is a close structural analog of lovastatin and both agents have the same biochemical and pharmacological activities. Mevastatin is inactive in cell-free assays. In cells however, it is hydrolyzed to the active free acid form by intracellular esterases.