Do We Need to Change the Definition of Drug-Like Properties?

In this webinar Mike Shultz (Novartis) presented; two decades have passed since the Rule of Five (Ro5) ushered in the concept of “drug-like” properties. Examination of oral drug parameters approved before and after the original Ro5 analysis demonstrates that some parameters such as clogP and HBD remained constant while the cut-offs for parameters such as molecular weight and HBA have increased substantially. The time dependent increase in the molecular weight of oral drugs during the past 20 years provides compelling evidence to disprove the hypothesis that molecular weight is a “drug-like” property. This analysis does not validate parameters that have not changed as being “drug-like” but instead calls into question the entire hypothesis that “drug-like” properties exist.

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