More than 40 companies are pursuing new approaches to lead optimization.
During the lead optimization process, active compounds ("hits") that
were identified during the lead discovery and selection stage are modified so
that the resulting compound has the desired properties for use in the clinic.
Companies are focusing on several approaches to improve lead optimization,
including developing better assays to provide information about the activity of
the compound in the cellular or biological context.
This report evaluates the many efforts that are under way to make lead
optimization less time-consuming and linear. A compound that fails near the end
of the process can potentially waste significant resources; the ability
to optimize a compound for several characteristics simultaneously could save
considerable time and potentially reduce the number of late-stage failures in
the lead optimization process. Thus, this report is crucial reading for
pharmaceutical executives as they seek means to accelerate drug discovery while
reducing costs in order to meet their business goals. New approaches for
predicting toxicity are also examined in this report,
particularly the efforts of some groups to develop better animal model systems
and to look at ways to introduce these assays earlier in the process.
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