Health Dictionary
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Mevastatin
Introduction
Overview
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
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.[1] It causes cells to arrest early in the G1 phase. [2] [3]
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.
References
References
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]