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Cloe Screen MDR1-MDCK: A Predictive Model of Drug Permeability
EP20158
Poster Title: Cloe Screen MDR1-MDCK: A Predictive Model of Drug Permeability
Submitted on 19 Dec 2013
Author(s): David Turner, Boris Pufong, Susan Hinchliffe, Gayle Corkill, Deborah Slamon, Peter Dykstra, Helen Gill, Clive Dilworth and Darwin Cheney
Affiliations: Cyprotex Discovery Ltd.
Poster Views: 1,131
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Poster Information
Abstract: Madin Darby Canine Kidney cells transfected with the human MDR1 gene (MDR1-MDCK), express the membrane transporter P-glycoprotein (P-gp). We have developed an MDR1-MDCK permeability screen for assessing the membrane permeability properties of early drug discovery compounds.

This study measured the bi-directional transport of compounds with a range of permeabilities across MDR1-MDCK monolayers. Drug concentrations were analysed by LC-MS/MS, from which apparent permeability (Papp) values in apical-basolateral (A-B) and basolateral-apical (B-A) directions and asymmetry index (B-A Papp /A-B Papp) were calculated. Experiments were also carried out in the presence or absence of the P-gp inhibitor cyclosporin A.

Results were compared with those from Caco-2 permeability studies as well as human intestinal absorption values and brain uptake classification obtained from literature. These results indicate that Cloe Screen MDR1-MDCK permeability assay is a useful predictive tool for assessing human intestinal absorption and uptake across the blood brain barrier in early drug discovery.
Summary: A MDR1-MDCK permeability screen for assessing the membrane permeability properties of early drug discovery compounds has been developed. This study measured the bi-directional transport of compounds with a range of permeabilities across MDR1-MDCK monolayers. Drug concentrations were analysed by LC-MS/MS, from which apparent permeability values in apical-basolateral and basolateral-apical directions and asymmetry index were calculated. Report abuse »
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