Drug Development Of The Drug Imatinib

1050 Words Sep 9th, 2016 5 Pages
TRM6002 Essay 2 – Drug Development
State what the target for the drug imatinib is, and why that target was a good choice for a drug discovery project.
Until the 1990’s, drug discovery relied on forward pharmacology where trial and error produced medications that were usually involved in changing DNA synthesis and/or cell division. These medications were efficacious, but had issues with systemic toxicities due to their non-selectivity of diseased cells or disease causing proteins. With the discovery of specific genetic changes that occur in Chronic Myeloid Leukemia, a haematological malignancy, a target was identified which was only seen in diseased cells; thus, rational drug design came about. Imatinib is the first medication of rational drug design with action only in diseased cells.


Historically, drug discovery projects were aimed at developing drugs that were involved in changing DNA synthesis and/or cell division. These medications included alkylating agents which were very effective but due to the large range of non targeted action within the body, had multiple side effects and toxicities. Since the discovery of specific and varied genetic changes that can occur within cancerous cells, the approach to drug development has changed significantly. Imatinib was one of the first drugs developed where its site of action was only on diseased but not on non-diseased cells.

Drug discovery programs start when there is a…
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