A Fast and Simple Method For Measuring P-Glycoprotein (Pgp) Inhibition

This application note reports on a novel assay specific for measuring inhibition of the P-glycoprotein multidrug transporter. The assay can be used with 96 well or 384 well microplates, it has a low sample requirement and an IC50 determination can be produced within 10 minutes. The system provides a rapid, sensitive and specific reconstituted Pgp liposome assay for identification of compounds that interact with the transporter. Pgp expression has been linked to the efflux of chemotherapeutic drugs in human cancers leading to multidrug resistance.