Accidents, Molds, and the Origins of Modern Drugs
Aspirin’s active ingredient traces back to a folk remedy older than written medicine: Hippocrates himself, in the fifth century BCE, recommended chewing willow bark to relieve pain and fever, a use that persisted in traditional medicine for well over two thousand years before anyone understood why it worked. That understanding arrived in stages — French chemist Charles Frédéric Gerhardt first synthesized a crude form of acetylsalicylic acid in 1853, but it was Felix Hoffmann, a chemist at the German company Bayer, who in 1897 refined the synthesis into a stable, usable compound, reportedly motivated by a search for something to relieve his own father’s arthritis pain without the stomach irritation that plain salicylic acid caused. Bayer began marketing the drug as Aspirin in 1899, and it remains, well over a century later, one of the most widely used medications in the world.
Not every major drug discovery followed such a deliberate path. Japanese biochemist Akira Endo spent years in the early 1970s screening thousands of fungal compounds in search of a substance that could lower cholesterol by blocking an enzyme involved in the body’s own cholesterol production. In 1973, he isolated compactin from a strain of Penicillium citrinum mold — the same genus of mold, coincidentally, that had already changed medicine once through the discovery of penicillin decades earlier. Compactin itself was never approved for use, but Endo’s discovery opened the door to an entire class of drugs, and in 1987 the first approved statin, lovastatin, reached the market, launching what would become one of the most prescribed drug classes in modern medicine, a commercial and public-health impact Endo himself reportedly never fully anticipated when he began his original screening work in a Tokyo laboratory more than a decade earlier.
From Folk Remedy to Laboratory Molecule
Some of the most consequential drugs in modern history were developed not by accident but through years of deliberate, controversial research. The combined oral contraceptive pill was developed in the 1950s through the collaboration of biologist Gregory Pincus, physician John Rock, and chemist Carl Djerassi, who had already synthesized a key progesterone-like compound in 1951. Their work — funded substantially by birth control advocate Margaret Sanger and heiress Katharine McCormick — culminated in the FDA’s 1960 approval of the first oral contraceptive, a decision that arrived after clinical trials conducted partly in Puerto Rico, a choice made in part because contraception research faced legal restrictions in much of the mainland United States at the time.
Modern psychiatric drug discovery followed a very different research path. Fluoxetine — better known by its brand name, Prozac — was developed by researchers at Eli Lilly throughout the 1970s, built around a then-new hypothesis that selectively blocking the reabsorption of serotonin, rather than affecting multiple neurotransmitter systems at once as older antidepressants did, could treat depression with fewer side effects. Approved by the FDA in 1987, Prozac became the first widely prescribed selective serotonin reuptake inhibitor, or SSRI, and its commercial and cultural success reshaped both psychiatric treatment and the pharmaceutical industry’s approach to drug development for decades afterward.
Source: National Institutes of Health (NIH) and Encyclopaedia Britannica.