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A Quick History of the Drug Discovery Process

For many centuries, people treated disease with locally gathered, naturally occurring substances like herbs, flowers, and molds. Fast forward to today, and some of these same compounds are still in use—though accompanied by a wide array of other natural and synthetic drugs developed in laboratories around the world. The types of medicinal drugs we use today have certainly grown and developed over time. This is due largely in part to the evolution of the drug discovery process.

Drug Discovery in the 20th Century

The history of drug treatments in humans is firmly rooted in the use of natural extracts. For thousands of years, people identified an organic compound’s medicinal potential through sheer trial and error—and, eventually, medicinal chemistry. Even the discovery of penicillin in the early 20th century occurred largely by accident and was refined through repeated experiments with the antibiotic.

The antibiotic age eventually changed the way people studied the effects compounds have on disease-causing agents. As tuberculosis, pneumonia, and diarrhea began to recede with the use of antibiotics—even as they began to develop resistance to common antibiotics—other, more complex diseases emerged. It soon became clear that accidental discovery and manual compound testing was simply too time-consuming.

Synthetic Organic Chemistry

When there were no obvious organic candidates to treat the diseases that emerged after World War II, synthetic organic chemistry offered researchers the opportunity to create them. Researchers discovered that they could identify a potential biological target and use lead discovery to identify known compounds that could affect it. 

As researchers synthesized more and more compounds through the 1970s and ’80s, it became clear that compounds with similar functional groups could have similar effects on the same disease target. Renewed focus on natural organic substances structures also enabled the research community to screen organic compounds with structures most likely to affect the disease in question. Once a large number of organic and synthetic compounds had been analyzed and identified, they could be placed into large panels of assays and grouped by potential molecular activity.

Empirical Methods

In the 80’s and 90’s, computerized drug design emerged. Screening technologies, robotics, and assay techniques allowed lead discovery on a level that never could have been imagined during the start of the 20th century. The refinement of these technologies has allowed researchers access to entire libraries of thousands of molecules that can be screened for activity on a drug target.

Current high-throughput screening requires a diverse catalog of compounds to increase the chances of drug development that will result in clinical trials. Additional advances in synthetic and organic chemistry are necessary to continue to identify potential compounds. 

Hope for the Future

As research continues, drug discovery has the potential to identify the compounds that will lead to the most beneficial medicinal drugs of our time. Attention to chemistry, pharmacology, and biology remains crucial—as does the continual development of effective laboratory technology. With advances in these areas, the drug discovery process will grow, and new treatments will become available for future generations.