This last point is the reason for the interest of regulatory authorities around the world, several of which (most notably the U.S. FDA and the EMA) now require that all new molecular entities (NMEs) be evaluated as P-gp substrates and inhibitors. This chapter will cover model test systems...
Compounds that interact with Pgp can be identified as stimulators or inhibitors of its ATPase activity. Compounds that are substrates for transport by Pgp typically stimulate its ATPase activity (1). The Pgp-Glo™ Assay detects the effects of compounds on recombinant human Pgp in a cell ...