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Mevastatin

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]


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

  1. A. Endo J. Lipid Res. 1992 33 1569
  2. V. Quesney-Huneeus et al. J. Biol. Chem. 1983 258 378
  3. V. Quesney-Huneeus et al. Proc. Natl. Acad. Sci. USA 1979 76 5056

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