The American biochemist Alfred Alberts has just died at the age of 87. Unknown, it is nevertheless at the origin of the first anticholesterol drug in the world, lovastatin.
He passed away at the age of 87 in Colorado. According to New York Times, who devotes a portrait to him, Alfred Alberts was greeted as a hero at the hospital, when caregivers knew they had before them the inventor of one of the most famous drugs in the world. The American biochemist is at the origin of the first marketed statin: lovastatin.
In the 1970s, the prevention of heart attacks and strokes was limited to advice on lifestyle and a few molecules with limited efficacy. Thanks in particular to the work of Brown and Goldstein at the University of Texas, awarded the Nobel Prize for Medicine in 85, we know that cholesterol – in its variant LDL, the “bad” cholesterol – induces the formation of plaques in the arteries. , which increases the risk of occurrence of a cardiovascular accident.
Since 1964, we even know of an enzyme (HMG-CoA reductase) that modulates the synthesis of cholesterol in the body. By blocking its action, it should be possible to limit the level of bad cholesterol in the blood. It remains to find the right molecule, effective and safe. Easier said than done.
Discovered within a week
Two laboratories are in the running: the Japanese Sankyo and the American Merck, where Alberts entered in 1959 as a laboratory technician before climbing the ladder. The competition promises to be tough, especially since Sankyo has already managed to isolate a candidate: mevastatin. In 1978, Alberts and his assistant Julie Chen tested cultured mushrooms from a Madrid laboratory. In just one week, they have just discovered lovastatin…
In September 1980, a commotion within the Alberts team. The Japanese competitor Sankyo has just interrupted its trials in dogs: according to rumors, mevastatin causes intestinal tumours. Merck management immediately halted clinical trials of lovastatin. It will take three years to demonstrate the absence of toxicity, and resume human trials.
A controversial success
It was in 87, seven years later, that lovastatin received its marketing authorization in the United States, under the name Mervacor. In the meantime, the drug has shown its effectiveness by reducing the level of “bad” cholesterol by more than a quarter. It is the first of a long series of statins, which will prevent cardiovascular risk in millions of patients. More than 200 million are treated today worldwide.
This success was not without controversy. Sometimes used wrongly and through since the 90s, in the context of an extremely lucrative market (tens of billions of dollars per year), statins have sometimes seen their interest violently called into question. Now that the dust has settled and the data is accumulating, experts agree on their effectiveness in high-risk patients and in preventing recurrence.
Since the 1980s, when chemists reigned supreme, the development of small molecules has marked time in favor of biotechnology, and high-throughput screening technologies tend to replace researchers’ intuition. “Too many computers, not enough brains,” grumbled Alberts when asked through Science in 2005. In any case, he will go down in history as an exceptional brain.
Source: Triumph of the Heart: The Story of Statins, by Jie Jack Li.
.
