Abstract:Approximately 6% of orally administered drugs have physicochemical properties that are beyond Lipinski's rule of five (bRo5). However, in the past five years, there have been 22 new oral bRo5 drugs approved by the FDA, which account for 21% of new oral drug approvals. The significant increase in the percentage of bRo5 drug approvals represents a shift in the types of drug targets undertaken by medicinal chemists including a larger number of protein–protein interaction (PPI) inhibitors, such as BCL‐2 inhibitors… Show more
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