Discovery and Development of Statins

摘要

Mevastatin (Compactin) belonging to the statin class is a hypolipidemic agent. It was isolated from the ascomycetous fungus, Pemcillium citrinum by A. Endo in the 1970s, and he discovered that it acted as 3-hydroxy-3-methyl-glutaryl (HMG)-CoA reductase inhibitor. Mevastatin is considered the first statin drug. The clinical trials on mevastatin were carried out in the late 1970s in Japan. The first commercial statin drug was lovastatin, the second statin, which was found in Aspergillus terreus by Merc and Endo, independently in 1979. Since lovastatin was commercialized, 10 statins were synthesized among which paravastatin was launched to the market by Sankyo in 1989. Pravastatin is used in the lowering of cholesterol and preventing cardiovascular disease. At present, statins are the largest-selling class of drugs currently taken by patients throughout the world. Sales for this one class of drugs on 2005 were $25 billion. Today an estimated 40 million people worldwide are taking statin drugs.