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Determination of IC50 for rolapitant inhibition of CYP2D6. CYP2D6 supersomes (2 pmol) were incubated with dextromethorphan (10 µM) and varying concentrations of rolapitant (0.05–100 µM). Log concentration is plotted against percentage of activity of dextrorphan product formation relative to a 0 µM inhibitor control. The IC50 value was 24 µM for rolapitant. Each point represents the mean ± S.D. of an experiment completed in triplicate.
