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bioRxiv · 10.1101/2025.03.19.644079

Plasma Protein Binding as an Optimizable Parameter for In Vivo Efficacy

Zhao, H.
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Abstract

Plasma protein is crucial for understanding pharmacokinetics, pharmacodynamics, and safety, yet it is often not recommended as a primary parameter for optimization in drug design. This study challenges this view by revisiting established pharmacokinetic models to elucidate a bidirectional strategy for clearance-dependent optimization of plasma protein binding. The analysis shows that strategically modulating plasma protein binding can enhance drug efficacy and safety, supporting its consideration as a key factor in the drug design process.

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Zhao, H.. 2025-03-19. Plasma Protein Binding as an Optimizable Parameter for In Vivo Efficacy. https://doi.org/10.1101/2025.03.19.644079

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