TABLE 1

Summary of mean (± S.D.) AUC0-8 and Cmax of tamoxifen, NDM, 4OHT, and endoxifen when administered 20 mg/kg tamoxifen orally following vehicle or rifampin treatment for 3 days (N = 4)

Tg-CompositeWThPXR-CAR
VehicleRifampinVehicle/Rifampin RatioVehicleRifampinVehicle/Rifampin RatioVehicleRifampinVehicle/Rifampin Ratio
Tamoxifen
 AUC0-8 (μM*h)0.82 ± 0.140.20 ± 0.12*4.10.92 ± 0.321.4 ± 1.00.661.0 ± 0.260.42 ± 0.06*2.4
 Cmax (μM)0.15 ± 0.030.048 ± 0.0133.10.28 ± 0.150.69 ± 0.200.400.33 ± 0.070.17 ± 0.091.9
NDM
 AUC0-8 (μM*h)0.84 ± 0.220.18 ± 0.04*4.70.21 ± 0.100.24 ± 0.310.880.29 ± 0.050.16 ± 0.05*1.8
 Cmax (μM)0.13 ± 0.040.037 ± 0.0023.50.046 ± 0.0050.094 ± 0.0680.490.081 ± 0.0150.057 ± 0.0231.4
4OHT
 AUC0-8 (μM*h)3.4 ± 0.51.0 ± 0.4*3.40.25 ± 0.070.28 ± 0.100.890.80 ± 0.250.43 ± 0.01*1.9
 Cmax (μM)0.64 ± 0.170.19 ± 0.043.40.053 ± 0.0240.056 ± 0.0210.950.26 ± 0.080.19 ± 0.031.4
Endoxifen
 AUC0-8 (μM*h)0.94 ± 0.130.74 ± 0.03*1.30.38 ± 0.150.26 ± 0.081.60.53 ± 0.120.28 ± 0.13*1.9
 Cmax (μM)0.18 ± 0.040.11 ± 0.031.60.080 ± 0.0040.080 ± 0.0161.00.12 ± 0.020.10 ± 0.041.2