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We evaluate test compounds for potential to alter CYP activity via direct or time-dependent inhibition mechanisms, for the following CYPs: 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A4/5.
A probe substrate, selective to each CYP of interest, is used to evaluate CYP activity in pooled human liver microsomes in the presence and absence of the test compound. Typically, the test compound is evaluated in triplicate at seven concentrations. Positive control direct inhibitors are assessed in parallel by determining IC50 values in duplicate and positive control time-dependent inhibitors assessed in triplicate at a single concentration (with a 30-minute preincubation ± NADPH). Potency of CYP inhibition is assessed by determining the IC50 value, the concentration of inhibitor that reduces CYP activity by 50%, if inhibition is observed.
As part of our project we provide a full, non-clinical, eCTD-compliant report.