Lead Optimization
During the Lead Optimization process, lead compounds that survived the initial screening are then “optimized,” or altered to make them more effective and safer. By changing the structure of a compound, scientists can give it different properties. For example, they can make it less likely to interact with other chemical pathways in the body, thus reducing the potential for side effects.
Hundreds of different variations or “analogues” of the initial leads are made and tested. During the Lead Optimization process, teams of biologists and chemists work together closely: The biologists test the effects of analogues on biological systems while the chemists take this information to make additional alterations that are then retested by the biologists. The resulting compound is the candidate drug.
Even at this early stage of Lead Optimization, researchers begin to think about how the drug will be made, considering formulation (the recipe for making a drug, including inactive ingredients used to hold it together and allow it to dissolve at the right time), delivery mechanism (the way the drug is taken – by mouth, injection, inhaler) and large-scale manufacturing (how you make the drug in large quantities).
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