mevastatin

Mevastatin is a naturally derived cholesterol-lowering agent, originally isolated from the mold Penicillium citrinum. It was the first discovered member of the statin class (HMG-CoA reductase inhibitors), identified in the early 1970s by Akira Endo at Sankyo. Mevastatin acts as a prodrug that is hydrolyzed in vivo to its active form, which competitively inhibits 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase)—the rate-limiting enzyme in cholesterol biosynthesis. This inhibition leads to decreased hepatic cholesterol synthesis and increased uptake of LDL cholesterol from circulation, thereby lowering plasma cholesterol levels. Although it demonstrated efficacy in reducing serum lipids and showed antiproliferative effects on certain cancer cells and potential benefits for wound healing, mevastatin was never marketed due to safety concerns observed during clinical trials. Its structure served as a lead compound for later statins such as pravastatin[1][2][3][4].

Other names

compactinML-236BML236BML 236B