Statins 1973 – The Discovery of Cholesterol Drugs

Journalist Peter Landers writes: 

"Akira Endo spent two years and thousands of mouldy  culture dishes finding something that lowered cholesterol. From a mould-like fungus growing on an orange, he  obtained  his big discovery, the first in a class that brought pharmaceutical companies an annual  $25 billion (in 2006)  in revenue.”

Cholesterol  is important for the function of every cell in our bodies, but it also causes a condition resulting from cholesterol-containing deposits accumulating inside artery walls, called  atherosclerosis. These deposits, or plaques, can rupture and lead to blood clotting. Plaques or clots can reduce blood flow. Blockage of the coronary arteries can cause angina (chest pain) or a heart attack. Atherosclerosis is also associated with inflammation of artery walls.

• Statins are a class of drugs used to lower cholesterol levels by inhibiting the  HMG-CoA  reductase enzyme that the liver uses to produce cholesterol. In 1973, Japanese  biochemist Akira Endo discovered mevastatin, the first cholesterol-inhibiting statin, isolated from Penicillium citrinum  fungus. The American pharmaceutical company  Merck & Co.  was inspired by Endo's work and, in 1978, isolated another statin from the fungus  Aspergillus terreus. It was first marketed in 1987 under the name  Mevacor.

Statins appear to have many benefits. For example:

• They reduce LDL cholesterol (low-density lipoprotein cholesterol – the "bad" form of cholesterol that contributes to plaque formation in arteries) and inflammation while maintaining plaque stability.
• In addition, when liver cells detect a statin-related decrease in liver cholesterol, they compensate by increasing LDL uptake and producing LDL receptors that draw cholesterol out of the general circulation.
• Statins are generally considered beneficial in reducing mortality (the rate of loss of life) in people with pre-existing cardiovascular disease and those at high risk.

However, potential adverse effects  include:

• Abnormally elevated liver enzymes 
• The release into the bloodstream of products harmful to the kidneys
• Breakdown of skeletal muscle, which can lead to kidney failure

Description of the article image: Plaque restricting blood flow in an artery.

Historical figures mentioned in the article: Akira Endo (b. 1933)

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