ML-236B, Mevastatin (compactin)

New Drug Approvals

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

It was isolated from the mold Penicillium citrinum by Akira Endo in the 1970s, and he identified it as a HMG-CoA reductase inhibitor,^[1] i.e., a statin. Mevastatin might be considered the first statin drug;^[2] clinical trials on mevastatin were performed in the late 1970s in Japan, but it was never marketed.^[3] The first statin drug available to the general public was lovastatin.

In vitro, it has antiproliferative properties.^[4]

A British group isolated the same compound from Penicillium brevicompactum, named it compactin, and published their results in 1976.^[5] The British group mentions antifungal properties with no mention of HMG-CoA reductase inhibition.

High doses inhibit growth and proliferation of melanoma cells.^[6]

Systematic (IUPAC) name
(1S,7R,8S,8aR)-8-{2-[(2

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