It was isolated from the mold Penicillium citrinum by Akira Endo in the 1970s, and he identified it as a HMG-CoA reductase inhibitor, i.e., a statin. Mevastatin might be considered the first statin drug; clinical trials on mevastatin were performed in the late 1970s in Japan, but it was never marketed. The first statin drug available to the general public was lovastatin.
A British group isolated the same compound from Penicillium brevicompactum, named it compactin, and published their results in 1976. The British group mentions antifungal properties with no mention of HMG-CoA reductase inhibition.
High doses inhibit growth and proliferation of melanoma cells.
^Endo, Akira; Kuroda M.; Tsujita Y. (December 1976). "ML-236A, ML-236B, and ML-236C, new inhibitors of cholesterogenesis produced by Penicillium citrinium". Journal of Antibiotics (Tokyo)29 (12): 1346–8. doi:10.7164/antibiotics.29.1346. PMID1010803.
^Wachtershauser, A.; Akoglu, B; Stein, J (2001). "HMG-CoA reductase inhibitor mevastatin enhances the growth inhibitory effect of butyrate in the colorectal carcinoma cell line Caco-2". Carcinogenesis22 (7): 1061–7. doi:10.1093/carcin/22.7.1061. PMID11408350.
^Brown, Allan G.; Smale, Terry C.; King, Trevor J.; Hasenkamp, Rainer; Thompson, Ronald H. (1976). "Crystal and molecular structure of compactin, a new antifungal metabolite from Penicillium brevicompactum.". J. Chem. Soc., Perkin Trans. 1 (11): 1165–1170. doi:10.1039/P19760001165. PMID945291.