P-gp Induction, Inhibition & Substrate Determinations
In drug development, it is helpful to know whether a compound is a substrate or an inhibitor of the multi-drug resistance protein, P-gp (MDR1), a ubiquitous transport protein that facilitates efflux of a wide variety of substrates. Inhibition of this transport protein may result in increased bioavailability, decreased clearance, and elevated AUC levels of the affected drug. Drug interactions due to induction of P-gp also have been reported. For this reason, the FDA recommends evaluating the substrate and inhibition potential of compounds towards P-gp.
Transporter assays available from CellzDirect include absorption (MDCK), substrate and inhibition potential measurements (MDCK/MDR1); and induction potential (hepatocytes). Transport is determined by LC-MS/MS or scintillation counting for radiolabeled compounds and induction potential by TaqMan® analysis.
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