History and Biochemistry of Statins

Statins: HMG-CoA Reductase Inhibitors as Potential Anticancer Agents against Malignant Neoplasms in Women

“…Of note, a series of clinical trials have proven the ability of this compound to reduce the levels of both total and LDL cholesterol in patients with severe hypercholesterolemia [22][23][24][25][26][27][28]. The promising hypocholesterolemic effects of lovastatin led finally to its introduction to clinical therapy in 1987 as the first statin in history [3]. Since a natural lovastatin had been commercialized, six semi-synthetic and synthetic statins have been introduced to the markets in the last 30 years [7].…”

“…In the group of well-known factors that may initiate and further promote CVDs is a high plasma level of low density-lipoprotein (LDL) cholesterol [2]. With respect to the biosynthetic pathway of cholesterol, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase plays a pivotal role in the control of the rate limiting step in its production, and thus the inhibition of the activity of this crucial enzyme has been pinpointed as the prime target of effective cholesterol-lowering therapies [3]. In this context, the treatment strategies with the use of statins have been found to significantly reduce the elevated levels of atherogenic lipoproteins, primarily LDL cholesterol, mainly through the inhibition of HMG-CoA reductase [4].…”