Illustration: Anthony Canamucio
In response to increased economic pressures, research-based pharmaceutical companies are attempting to streamline and accelerate their drug discovery and development processes. With the advent of genomics, proteomics, and bioinformatics, these companies now have access to an unprecedented abundance of potential therapeutic targets. With the emergence of combinatorial chemistry and innovative robotic-based technologies for conducting high throughput screening, these companies can also rapidly identify chemical leads that interact with these potential therapeutic targets. Using rational drug design strategies, promising leads can be rapidly optimized into high affinity ligands, referred to in the industry as new chemical entities (NCEs).

While these new technologies have enhanced the output of drug discovery groups, the quality of NCEs, as measured by their success in preclinical and clinical development, has not improved significantly. For example, less than 40 percent of NCEs produced by drug discovery groups survive preclinical testing and eventually undergo human...

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