2024
DOI: 10.3390/pharmaceutics16070846
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Conquering the beyond Rule of Five Space with an Optimized High-Throughput Caco-2 Assay to Close Gaps in Absorption Prediction

Patricia Muschong,
Khader Awwad,
Edward Price
et al.

Abstract: Current drug development tends towards complex chemical molecules, referred to as “beyond rule of five” (bRo5) compounds, which often exhibit challenging physicochemical properties. Measuring Caco-2 permeability of those compounds is difficult due to technical limitations, including poor recovery and detection sensitivity. We implemented a novel assay, with optimized incubation and analytics, to measure permeability close to equilibrium. In this setup an appropriate characterization of permeability for bRo5 co… Show more

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