Discovery
Drug Discovery is the name given to the first stage of producing a new medications.
During Discovery, a scientific search is conducted to find pharmaceutical or biologic products that go through as series of preclinical and clinical studies to become a marketed drugs. Discovery utilizes the talents of biologists, chemists, pharmacologists, computer scientists and support teams.
Drugs may be discovered in a variety of ways.
Identifying and refining traditional remedies
Willow bark was used for centuries as a pain reliever and fever reducer. In the early 1800’s chemists isolated salicin as the active ingredient in willow bark. Salicin is metabolized to salicylic acid. Unfortunately, salicylic acid is irritating to the digestive tract. In the mid-1800’s, chemists combined sodium salicylate with acetyl chloride to produce acetylsalicylic acid (ASA), a less irritating compound. In the late 1800’s, a German pharmaceutical company called Bayer, developed efficient methods to produce acetylsalicylic acid and sold it around the world under the brand name “Aspirin”. Over time, additional companies made the product and the trademark protection for the name “Aspirin” was lost or sold. The term aspirin began to be used as a generic name.
Finding Drug Targets
Researchers may develop new insights into a disease and identify genes, enzymes, ion channels, or receptors that play important roles in the pathophysiology of the disorder. These can become “drug targets”. Then pharmacologist look for chemical or biologic compounds that can bind to these drug targets to modulate the disease. Researchers can screen thousands of potential chemical to find a potential drug or can use or used computer models to design a new drug that will “fit” the drug target.
In the early 1980’s, researchers learned that a mutated gene called HER2 (human epidermal growth factor receptor 2) could stimulate excessive growth of tumor cells.
HER2 was studied as a potential drug target. Eventually, Genentech developed an HER2 receptor antibody that is used to treat breast cancer and sold as the biologic product Herceptin® (trastuzumab).
Serendipity
Serendipity means making a fortunate discovery by chance. Sometimes a chemical will have an unwanted or unexpected side effects that makes it suitable for a drug product. For example, minoxidil is a compound with vasodilatory properties. In the 1970’s, the pharmaceutical company, Upjohn, developed minoxidil for use as an oral drug to treat high blood pressure. People taking the drug reported hair growth as a side effect and the drug was subsequently redeveloped as a topical treatment to regrow hair and sold under the brand name Rogaine® (minoxidil).
For additional information about Drug Discovery and Drug Targets, I would suggest starting with these review articles:
Principles of Early Drug Discovery written by P Hughes, S Rees, SB Kalindjian, and KL Philpott and published in the British Journal of Pharmacology in 2011
Target validation: A door to drug discovery by Xiu-Ping Chen, Guan-Hua Du published in Drug Discovery and Therapeutics in 2007.
The Role of the Medicinal Chemist in Drug Discovery by Dr. Stevan W Djuric in the journal called Drug Discovery World. Although this review article focuses on Medicinal Chemistry, it explains the importance of teamwork and in using expertise from many disciplines.
Drug Discovery is the name given to the first stage of producing a new medications.
During Discovery, a scientific search is conducted to find pharmaceutical or biologic products that go through as series of preclinical and clinical studies to become a marketed drugs. Discovery utilizes the talents of biologists, chemists, pharmacologists, computer scientists and support teams.
Drugs may be discovered in a variety of ways.
Identifying and refining traditional remedies
Willow bark was used for centuries as a pain reliever and fever reducer. In the early 1800’s chemists isolated salicin as the active ingredient in willow bark. Salicin is metabolized to salicylic acid. Unfortunately, salicylic acid is irritating to the digestive tract. In the mid-1800’s, chemists combined sodium salicylate with acetyl chloride to produce acetylsalicylic acid (ASA), a less irritating compound. In the late 1800’s, a German pharmaceutical company called Bayer, developed efficient methods to produce acetylsalicylic acid and sold it around the world under the brand name “Aspirin”. Over time, additional companies made the product and the trademark protection for the name “Aspirin” was lost or sold. The term aspirin began to be used as a generic name.
Finding Drug Targets
Researchers may develop new insights into a disease and identify genes, enzymes, ion channels, or receptors that play important roles in the pathophysiology of the disorder. These can become “drug targets”. Then pharmacologist look for chemical or biologic compounds that can bind to these drug targets to modulate the disease. Researchers can screen thousands of potential chemical to find a potential drug or can use or used computer models to design a new drug that will “fit” the drug target.
In the early 1980’s, researchers learned that a mutated gene called HER2 (human epidermal growth factor receptor 2) could stimulate excessive growth of tumor cells.
HER2 was studied as a potential drug target. Eventually, Genentech developed an HER2 receptor antibody that is used to treat breast cancer and sold as the biologic product Herceptin® (trastuzumab).
Serendipity
Serendipity means making a fortunate discovery by chance. Sometimes a chemical will have an unwanted or unexpected side effects that makes it suitable for a drug product. For example, minoxidil is a compound with vasodilatory properties. In the 1970’s, the pharmaceutical company, Upjohn, developed minoxidil for use as an oral drug to treat high blood pressure. People taking the drug reported hair growth as a side effect and the drug was subsequently redeveloped as a topical treatment to regrow hair and sold under the brand name Rogaine® (minoxidil).
For additional information about Drug Discovery and Drug Targets, I would suggest starting with these review articles:
Principles of Early Drug Discovery written by P Hughes, S Rees, SB Kalindjian, and KL Philpott and published in the British Journal of Pharmacology in 2011
Target validation: A door to drug discovery by Xiu-Ping Chen, Guan-Hua Du published in Drug Discovery and Therapeutics in 2007.
The Role of the Medicinal Chemist in Drug Discovery by Dr. Stevan W Djuric in the journal called Drug Discovery World. Although this review article focuses on Medicinal Chemistry, it explains the importance of teamwork and in using expertise from many disciplines.