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The P-gp PREDIVEZ^TM kit is a breakthrough in P-gp interaction assessment. This assay measures drug-transporter interaction in membrane vesicles expressing human P-gp or rat Mdr1b.

Background:
FDA requires studies to investigate the interaction of drug candidates with P-gp.

The vesicular transport assay is a widely-used tool to study drug-transporter interactions in a simple and high throughput assay setup, and offers the choice of direct or indirect measurement options. Membranes prepared from human or insect cells overexpressing the efflux transporter contain inside-out membrane vesicles in which the transported compound accumulates. Typical detection methods include scintillation counting, fluorescence or LC-MS. The indirect vesicular transport assay is an inhibitory-type approach, performed with cold test compounds. It provides information on any interaction between the transporter and the drug candidate that would affect the transport of the reporter substrate.

P-gp PREDIVEZTM kit theory and data:
P-gp (ABCB1, MDR1) is the most commonly studied ABC transporter with important roles not only in tumor multidrug resistance but in the ADMETox properties of drugs and nutrients. As most of the substrates of P-gp are highly membrane permeable, the challenge was to develop a vesicular transport assay with a low permeability reporter substrate. SOLVO’s new P-gp PREDIVEZ^TM Kit operates with a low permeability cationic radio-labeled substrate that is transported by both MDR1 and ratMdr1b transporters. The typical dynamic range (cpms in ATP+/cpms in ATP-) is ~ 10 in the P-gp and ~ 3 in the ratMdr1b assay.

Human P-gp PREDIVEZ^TM kit works with human membrane vesicles while the rat Mdr1b PREDIVEZ^TM kit contains insect membrane preparation expressing the rodent ABC transporter.

Compound	LY335979	GF 120918	Cyclosporin A	Ketoconazole	Verapamil	Digoxin
IC50 / µM	0.3	0.3	0.43	1.3	9.5	320

P-gp PREDIVEZ^TM kit components:
P-gp PREDIVEZ^TM VT kit and rat Mdr1b-PREDIVEZ^TM VT kits are available in three sizes: 3, 6 and 9 compounds. Each kit contain sufficient amount of reagents and membrane preparation for testing 3 compounds per 96-well plate. Negative control membranes and positive control reference materials are also included. Each kit is accompanied by a CD that includes the assay protocol, Excel spreadsheet with data processing template, MSDS and reference curves with known interactors. Radio-labeled substrate not included.