Statins dramatically lower blood cholesterol, and the likelihood of heart attacks. Akira Endo discovered statins.

Akira Endo & His Molds

Endo is a Japanese researcher with a lifelong fascination related to fungi. Recalling that Fleming accidentally discovered penicillin, he theorized that fungi might hold other miracle drugs.

Endo noted that Americans are much heavier than Japanese people while studying in New York. Specifically, he noted elderly overweight people suffering from heart attacks. In contrast, Japanese people are slimmer. However, they are more likely to suffer a genetic abnormality resulting in excessive cholesterol levels leading to heart attacks. Children with this genetic problem suffered heart attacks as young as five years old. Therefore, high cholesterol was a serious health problem in both the US and Japan.

Back in Japan, Endo worked with thousands of molds searching for one that lowered cholesterol. In 1972, working at Sankyo, he came across a mold that worked which he and his team called compactin. Originally, the mold was found on a bag of old rice.

Concurrently, Michael Brown and Joseph Goldstein published a 1973 paper showing the receptor for cholesterol is regulated by genetics and other substances. In essence, they proved in a paper what Endo was seeing in the lab. Brown and Goldstein won the Nobel Prize.

Commercialization of Statins

Development of compactin continued. The compound demonstrated enormous promise in humans. However, dogs administered far higher doses of compactin — about 200x the correct dose — developed lymphoma cancer. Subsequently, Sankyo ceased work on compactin but licensed the drug and research to Merck.

Merck slightly changed the compactin molecule (Endo argues it is the same molecule) and renamed it lovastatin. The Japanese studies worked in the US and, by avoiding the extreme dosages, there were no side effects. The FDA approved lovastatin in September 1987. Since then, there have been several new statins developed. Statins are widely prescribed around the world and have dramatically decreased cholesterol and the resulting risk of a heart attack.

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