TABLE 4

In vitro induction of human CYP3A4 and CYP1A2 by SB939 after incubation in hepatocytes

CompoundCYP3A4Fold Induction Relative to Positive ControlCYP1A2Fold Induction Relative to Positive Controla
%%
SB939 (0.1 μM)0.774 ± 0.06614.7b, 19.2c1.19 ± 0.09*27.6
SB939 (1 μM)0.727 ± 0.089*13.8b, 18.0c1.37 ± 0.06**31.8
SB939 (10 μM)0.222 ± 0.012**4.2b, 5.5c1.38 ± 0.10**32.0
Rifampicin (10 μM)5.24 ± 0.74**100NANA
Dexamethasone (50 μM)4.03 ± 0.21**100NANA
Omeprazole (50 μM)NANA4.30 ± 0.02**100

  • NA, not applicable.

  • ↵* P < 0.05, significantly different from 0.1% DMSO control.

  • ↵** P < 0.01, significantly different from 0.1% DMSO control.

  • ↵a Omeprazole.

  • ↵b Rifampicin.

  • ↵c Dexamethasone.