What Are Statins Made of?

Statins, a class of medications first introduced in the late 1980s, reduce blood levels of low-density lipoproteins (LDLs), the so-called bad cholesterol, and boost levels of high-density lipoproteins (HDLs), the good cholesterol. Statins accomplish this task by inhibiting HMG-CoA reductase, an enzyme that plays a key role in the body's production of cholesterol. The active ingredients in statin drugs are derived either from a fermentation process or manufactured synthetically.

Early Research

• The discovery in 1959 of the HMG-CoA enzyme and the role it plays in cholesterol production prompted scientists all over the world to search for a substance that could effectively inhibit this enzyme and thus help to reduce blood cholesterol levels in humans. In 1976 Japanese biochemist Akira Endo isolated the first such inhibitor, compactin, from mold cultures, laying the groundwork for the development of life-saving statin drugs, according to an article by Thomas P. Stossel, M.D.

Merck Makes History

• Building on Endo's work, researchers at Merck, the American pharmaceuticals giant, in 1979 isolated a natural substance they called lovastatin from a strain of Aspergillus terreus, a fungal microorganism, according to a case study on the website of the University of Michigan Business School. Although lovastatin eventually was brought to market in 1987 as Mevacor, the first commercially available statin drug, the path between the initial discovery and approval by the Food and Drug Administration (FDA) was a rocky one.

Road to FDA Approval

• Merck's early clinical trials of lovastatin were shut down in September 1980 after a parallel Japanese testing program of compactin was halted by Japanese drug manufacturer Sankyo on the basis of unsubstantiated rumors that the substance caused cancer in dogs. In July 1982 the FDA gave Merck permission to supply Mevacor to a select group of doctors for patients whose high cholesterol had not responded to any other form of therapy. The results were startlingly successful, and a short time later Merck restarted animal testing. On Sept. 1, 1987, the FDA gave Merck the green light to begin marketing Mevacor.

Active Ingredients

• The active ingredients in most statin drugs are derived either through fermentation or produced synthetically in the laboratory, according to the Statin Answers website. The generic name of each statin drug identifies its active ingredient. As previously noted, lovastatin, marketed as Mevacor, was isolated from a strain of Aspergillus terreus, a fungus. The other fermentation-derived statins are simvastatin and pravastatin. The synthetic statins include fluvastatin, atorvastatin and rosuvastatin.

Inactive Ingredients

• As with all medications, the active ingredients in the statin drugs are accompanied by a variety of inactive ingredients. Some of these inactive ingredients are preservatives, others are responsible for the color or texture of the drug, while still others may help to deliver the active ingredient to patients in the most effective way. Because such ingredients vary from one statin to another, it's a good idea to check out product labels and/or product description brochures carefully to ensure that the drug contains no product to which you have an allergy.