Application of Hepatocytes for In Vitro Uptake Assays
Presented by: David Buckley, Ph.D. – CSO
This webinar provides a basic review of concepts applicable to a structure-based approach for the evaluation of hepatic uptake with in vitro hepatocyte experiments.
Key concepts discussed in this webinar will include:
- Selection of appropriate in vitro study type and design based on predictions from a drug candidate’s phys-chem properties
- Description of the basic in vitro methodologies using hepatocytes, both suspension and plated, to evaluate drug uptake, namely whole-system versus medium loss, oil-spin method and uptake into plated cells
- Discussion of the practical challenges associated with these experiments
- Basic review on the estimation of active and passive uptake components from these in vitro hepatocyte experiments
- Impact of phys-chem properties, active and passive uptake and metabolism on the estimation of free intracellular drug concentrations
- Brief review of the prediction of in vivo hepatic clearance from in vitro uptake experiments and potential scaling techniques
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