By Jie Jack Li
Over 25 million humans within the U.S. on my own have benefited from statins--such medicinal drugs as Lipitor, Zocor, Crestor, Pravachol, and different cholesterol-lowering medicines--in fighting stroke, middle assault, and other kinds of heart ailment. yet how did those notable, life-saving medicines come into being? In Triumph of the Heart, Dr. Jie Jack Li, a medicinal chemist and professional on drug discovery, tells for the 1st time the interesting tale of statins. Drawn from discussions with many scientists fascinated with the invention and improvement of those medications, the booklet illuminates the human facet of technological know-how via revealing the function performed via patience, good fortune, and surprising perception that signify significant discoveries. For scientists within the drug undefined, overall healthiness care pros, scholars of drugs, and all these intrigued through the elemental human force to discover and notice, Triumph of the Heart deals a compelling view of 1 of crucial drug discoveries of our time.
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Additional resources for Triumph of the Heart: The Story of Statins
Example text
In 1965, Sami A. Hashim and Theodore B. 3 g of cholestyramine resin each day in four doses. The patients’ serum cholesterol and cholesterol ester levels were reduced 50–80. This was a resounding success, although that kind of phenomenal reduction of cholesterol has not been consistently reproduced. Hashim and van Itallie’s report generated much excitement in cardiology. Merck, Sharp & Dohme tried to develop a drug for lowering cholesterol using cholestyramine, but the problem was that cholestyramine smelled like decaying fish and tasted little better.
After completing his fellowship, Endo returned to the Fermentation Research Laboratories at Sankyo in 1968. Two years later, he hypothesized that levels of plasma cholesterol could be effectively decreased by inhibiting hepatic HMG-CoA reductase, an enzyme that promotes the ratedetermining (slowest) step in cholesterol biosynthesis. His theory was actually very straightforward. During evolution, some fungi such as mushrooms developed a defense mechanism in which they produce a substance (called secondary metabolites in microbiology) that blocks the biosynthesis genesis of statins 37 of cholesterol.
Parson and coworkers at the Mayo Clinic also reported on the effect of nicotinic acid. 2 In the same year, massive doses of nicotinic acid were first used widely in Germany for lowering cholesterol. At that time, nicotinic acid was the only effective drug available for that purpose. Since then, nicotinic acid has established itself as a weapon in a doctor’s arsenal to treat people with high cholesterol levels. How does nicotinic acid work in lowering cholesterol? When Altschul, Hoffer, and Stephen published their landmark article, they had little clue as to nicotinic acid’s mechanism of action.
