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Simovastatin Essay

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Statins are recommended as a first-line therapy for the management of lipid disorders, particularly elevations in low-density lipoprotein cholesterol. In the 1950s and 1960s, it became obvious that elevated concentrations of plasma cholesterol represent a major risk factor for the development of heart disease, which led to the quest for drugs that could reduce it.

Since lovastatin had been commercialized, six statins – including two semi-synthetic statins (known as simvastatin and pravastatin) and four synthetic statins (fluvastatin, rosuvastatin and pitavastatin and atorvastatin) – have been introduced to the market. The most popular statin today is atorvastatin.

The discovery of statins

While working at the Sankyo Company in 1976, the Japanese biochemist Akira Endo isolated a factor from the fungus Penicillium citrinum which he identified as a competitive inhibitor of 3-hydroxy-3-methyl-glutaryl-coenzyme A …show more content…

Nevertheless, some researchers stayed skeptical as compactin did not lower plasma cholesterol in the rat, which was subsequently demonstrated to result from massive induction of HMG-CoA reductase in rat liver by inhibitors of the enzyme.

Clinical studies of compactin in Japan ensued soon after that, as well as experimental studies around the world. In 1978, Alfred Alberts with his colleagues at Merck Research Laboratories discovered a potent inhibitor of HMG-CoA reductase in a fermentation broth of Aspergillus terreus, which was named lovastatin, mevinolin or monacolin K. Conicidentally, Akira Endo independently identified a same compound within a year of Alberts’ discovery.

After animal safety studies have shown no adverse effects, Merck began clinical trials of lovastatin in April 1980. Still, promising start was interrupted because the trials with structurally similar compactin were stopped by Sankyo Company in September 1980, supposedly due to serious animal

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