ADME-PK Screening Benchmarks

Clinical Efficacy Formulation PK/ Commercial Toxicology Cost Unknown/ safety bioavailability of goods other 

FIGURE 2.5 Reasons for attrition for lead compounds in drug discovery in 1991 and 2000. In 1991, PK/bioavailability was the leading cause of attrition in drug discovery. By 2000 the attrition due to bioavailability decreased to below 10% because drug candidates were routinely screened for desirable bioavailability properties earlier in the process. (Courtesy of Nature Publishing Group, 2004. With permission.) 

And as a consequence, a more proactive study of toxicology and drug safety has recently emerged within drug discovery [18-20], Interestingly, efficacy remained a critical issue and was essentially unchanged during this timeframe with an attrition 

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