Our August issue review highlights includes:
• Pharmacokinetics and the drug-target residence time concept
• Tox21 robotic platform for assessment of environmental chemicals
• Matched molecular pair analysis in drug discovery
• Nano bio research approach by microtechnology
Cover Story
The leading story of this issue of Drug Discovery Today considers the combined effect of pharmacokinetics (PK) and binding kinetics (BK) on the duration of effect of a drug. Using a simple model that takes both PK and BK into account, Göran Dahl and Tomas Åkerud discuss how prolongation of binding owing to a long drug–target residence time can only occur when the binding dissociation is slower than the PK elimination. In addition, they discuss how data for a number of drugs and/or drug candidates in the literature indicate that the opposite is observed, that is, they have a slower elimination compared with dissociation. These observations greatly reduce the usability of drug–target residence times for estimating the duration of effect of a drug in vivo.
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