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Fosinopril, A Potential Substrate For Mrp2, Competes With Several High Use Pharmaceuticals For Elimination, Benjamin Green

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The multidrug-resistance associated protein 2 (MRP2) is a membrane-bound transporter responsible for the efflux of a variety of drugs and endogenous compounds. MDCK cells transfected with the human MRP2 gene were used to assess whether several highly used pharmaceuticals were potential substrates by examining their differential toxicity, accumulation, and efflux. Fosinopril, an ACE inhibitor, was 2.4-fold less toxic to the MRP2 transfected cells compared to mock transfected cells, suggesting that fosinopril is a potential MRP2 substrate. In addition, fosinopril was effluxed more rapidly, as the MRP2 cells only retained 13 % of the dosed fosinopril after 20 minutes compared with …