The Story of Statin Drugs
Monday, April 27th, 2009For many years cholesterol was the supposed culprit for arteriosclerosis and atherosclerosis, and the drug companies were looking for a way to stop high cholesterol.
Cholesterol, discovered as a major constituent of gallstones, was identified in 1775 as the first known steroid. Steroids are a member of the vast array of natural products known as terpenoids. Mankind has used these substances since antiquity as ingredients of flavors, preservatives, perfumes, medicines, narcotics, soaps and pigments. The name terpene was derived from research into the manufacture of camphor from turpentine by 1894. But the relationship of steroids to the terpennoids wasn’t discovered until the late 1950s. (1)
“The biogenesis of cholesterol starts from a simple chemical reaction: Under the influence of ultraviolet radiation, photosynthetic plants combine water with carbon dioxide, the well-known gas we exhale in every breath, to form glucose, the fuel of our bodies.
“From the humble origin, the first step toward the production of cholesterol in the human body involves the process of glycolosis in which glucose is converted into the two-carbon molecule, building blocks of life known as acetyl-CoA. These simple fragments then combine to start the cholesterol biosynthetic pathway. Next, three molecules of Acetyl-CoA combine stepwise to form the six-carbon hydroxymethyl glutaric acid part of the intermediate complex know as HMG-CoA, which has proven to be the Achilles heel of cholesterol biosynthesis.
“This is the weak point in the chain of events the pharmaceutical industry was looking for and the one that enabled them to develop their statin drugs, for when two molecules of HMG-CoA next combined to form the ubiquitous mevalonic acid, the enzyme, HMG-CoA reductase was required. This enzyme was quite easily inhibited and suddenly a multibillion-dollar industry was born with the development of the HMG-CoA reductase inhibitors known as the statin drugs. Whether Lipitor, Mevacor, Zocor, Pravachol, or the ill-fated Baycol, all use the same mechanism and are merely variations of the same theme as marketed by different pharmaceutical companies to obtain market share.
“One can imagine the chagrin of the pharmaceutical industry to discover in a simple yeast from the Orient that Mother Nature already had provided her very own “completely natural” HMG-CoA inhibitor, red yeast rice. For thousands of years this yeast, known as Monascus purpureus, has been used to ferment rice into wine and as both a spice and preservative. Needless to say, any possible interference of this oriental fermentation product with our emerging statin drug industry was obviated by Merck’s patent—the first ever filed on a naturally occurring substance. Mother Nature’s cholestin would never compete with Merck’s identical product, lovastatin, which has the trade name of Mevacor.
“Research biochemists soon identified the HMG-CoA reductase step as a natural control point for cholesterol synthesis since the reaction was not reversible and it was the slowest step of the entire cholesterol pathway. It seemed a natural point for the cholesterol control—the pharmaceutical companies now had their ‘corral.’ One can almost feel the pulse of the industry leaders quicken in anticipation of the potential market size.” (2)
Next blog will tell of the Achilles heel of the statin drugs.
1. Graveline, Duane, M.D., LIPITOR, THIEF OF MEMORY, Published by Duane Graveline MD. 2006, p. 55
2. Ibid. pp.53-54