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The evaluation of interactions between drug candidates and transporters such as P‐glycoprotein (P‐gp) has gained considerable interest in drug discovery and development. Inhibition of P‐gp can be assessed by performing bi‐directional permeability studies with in vitro P‐gp‐expressing cellular model systems such as Caco‐2 (human colon carcinoma) cells, using digoxin as a substrate probe. Existing methodologies...
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