The first step in discovering a new medicine is to
identify a therapeutic target. Drugs in today’s market as well as those in recent clinical
testing target less than 500 biomolecules, with more than 10 times that many potential
therapeutic targets waiting to be discovered and developed (Drews, 2000). More than
50% of the newly approved drugs result from R&D involving previously clinically
tested and validated targets. Once a target has been validated (proven to be related
to the disease process), high-throughput screening methods may be used to determine
initial structural leads. Compounds are assessed for target affinity and for their “druglike”
properties, including absorption, distribution, metabolism, and excretion
(ADME) using a series of in vivo and in vitro tests. The results of these tests are
used to improve the structure and therefore the properties of the next round of test
compounds, until ultimately one or more acceptable compounds are advanced
forward in the process. This stage of discovery, which can be lengthy and difficult
to predict, is generally referred to as lead optimization.
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