Understanding P-gp & BCRP Inhibition Assay Design & Outcomes
Presenter: Andrea Wolff, XenoTech Director of Services Logistics
Synopsis:
In vitro drug transporter inhibition studies are recognized for their importance due to the major role transporters play in absorption, distribution and excretion of compounds, and the toxicological and pharmacological consequences of transporter-mediated drug-drug interactions (DDI). P-gp and BCRP transporters limit intestinal absorption and blood-brain barrier penetration, and facilitate excretion into bile and urine.
Andrea Wolff, XenoTech Director of Services Logistics, recently provided a webinar to the SimCyp transporter discussion group on P-gp and BCRP Inhibition. For those who did not have the opportunity to hear her presentation, we hosted a follow-up webinar on Dec. 11th.
Key concepts discussed in this webinar will include:
- Description of the in vitro test systems used to evaluate P-gp and BCRP inhibition at XenoTech and the advantages/disadvantages of these assays
- Description of the test system qualification process that takes places prior to offering these assays in definitive studies
- Comparison of IC50 values obtained from the different test systems
- Comparison of IC50 and Ki values determined with the vesicle test system
- How IC50 and Ki values are used to evaluate clinical relevance
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