TABLE 1

Effect of AZD1208 on CYP3A4 mRNA in HepaRG and human hepatocytes

Cell TypeMaximum Concentration TestedCYP3A4 mRNACYP3A4 Activity
Observed Fold InductionaPercentage Rifampicin InductionbObserved Fold InductionPercentage Rifampicin Induction
μM
HepaRG303.35.4Not testedNot tested
Hepatocyte lot 321302.42.5Concentration-dependent decrease
Hepatocyte lot 349303.41.6Concentration-dependent decrease
Hepatocyte lot 295103.4<1.01.1Not calculated

  • ↵a Observed fold induction data are the mean from triplicate wells at the concentration stated.

  • ↵b Induction as percentage of positive control data are the mean of triplicate wells in each group.