IC50-based approaches as an alternative method for assessment of time-dependent inhibition of CYP3A4.

Abstract

The predictive utility of two in vitro methods (empirical IC(50)-based and mechanistic k(inact)/K(I)) for the assessment of time-dependent cytochrome P450 3A4 (CYP3A4) inhibition has been compared. IC(50) values were determined at multiple pre-incubation time points over 30 min for five CYP3A4 time-dependent inhibitors (verapamil, diltiazem, erythromycin… (More)
DOI: 10.3109/00498251003698555

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