Hit-to-lead strategies

Table 2.2 Breakdown of hit-to-lead strategies in published FBDD.lS7]...

Table 12.2 Examples of technology-based strategies to optimize hit-to-lead process...

Glaser V. Optimizing strategies for hit-to-lead process. Gen. Engin. Biotech. News. 2005 25 31-37. 

Fig. 3 Diagramatic representation of Old and New strategies for lead optimization of new pharmaceutical molecules. The top section indicates the Old (and in some cases, current) way in which pharmaceutical companies take Hits to lead development candidate through discovery and early preclinical development testing. Essentially, no high-throughput formal lead optimization exists in this model but is developed for backup compounds by using biomarkers identified during lead compound failure in vivo. The bottom section indicates the New way forward (used now by most major pharmaceutical companies). In this model, a formal in vitro PLOT battery is inserted early in development before preliminary in vivo ADME-Tox screening and subsequent lead development candidate selection.

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