Drug | Treatment | CYP3A4 mRNA^{a} | ||
---|---|---|---|---|

Donor 1 | Donor 2 | Donor 3 | ||

ASV | Donor | HC3-15 | HC1-18 | HC5-10 |

DMSO (0.1%) | 1 | 1 | 1 | |

0.049 µg/ml | 3.73^{b} | ND | 0.802 | |

0.15 µg/ml | 1.53 | 1.86 | 1.13 | |

0.49 µg/ml | 4.72 | 3.58 | 1.77 | |

1 µg/ml | 7.79 | 5.5 | 2.92 | |

2 µg/ml | 8.6 | ND | 3.66 | |

4.9 µg/ml | 12.1 | 6.7 | 4.3 | |

10 µg/ml | 8.7^{c} | 4.73^{c} | 3.7 | |

20 µg/ml | 4.95^{c} | 2.39^{c} | 1.74^{c} | |

Rifampin (10 µM) | 26 | 18.1 | 8.15 | |

DCV | Donor | HC3-15 | HC1-18 | HC5-10 |

DMSO (0.1%) | 1 | 1 | 1 | |

0.16 µg/ml | 1.38 | 1.45 | 1.21 | |

0.32 µg/ml | 1.44 | 1.66 | 1.34 | |

0.75 µg/ml | 2.5 | 2.27 | 1.47 | |

1.6 µg/ml | 5.59 | 5.7 | 4.91 | |

2.5 µg/ml | 7.48 | 9.22 | 3.7 | |

4 µg/ml | 12.8 | 12.1 | 6.35 | |

6 µg/ml | 20.3 | 13.2 | 6.68 | |

9.6 µg/ml | 27.3 | 13 | 8.76 | |

Rifampin (10 µM) | 26 | 18.1 | 8.15 | |

BCV | Donor | HC3-15 | HC3-17 | HC5-10 |

DMSO (0.1%) | 1.00 | 1.00 | 1.00 | |

0.15 µg/ml | 1.96 | 1.45 | 1.90 | |

0.35 µg/ml | 3.27 | 1.99 | 1.67 | |

0.8 µg/ml | 5.64 | 2.59 | 2.67 | |

1.5 µg/ml | 6.36 | 2.61 | 2.43 | |

3.5 µg/ml | 5.77 | 2.18 | 2.64 | |

8 µg/ml | 3.88^{c} | 2.09 | 2.45 | |

15 µg/ml | 2.70^{c} | 1.38^{c} | 1.43^{c} | |

30 µg/ml | 0.29^{c} | 0.08^{c} | 0.26^{c} | |

Rifampin (10 µM) | 29.80 | 3.70 | 7.93 | |

BCV-M1 | Donor | HC3-15 | HC3-17 | HC5-10 |

DMSO (0.1%) | 1.00 | 1.00 | 1.00 | |

0.028 µg/ml | 1.04 | 1.15 | 0.97 | |

0.08 µg/ml | 1.63 | 1.26 | 1.05 | |

0.28 µg/ml | 3.57 | 1.99 | 1.61 | |

0.8 µg/ml | 7.17 | 2.49 | 2.22 | |

2.8 µg/ml | 8.23 | 2.26 | 2.41 | |

8 µg/ml | 5.24^{c} | 2.14 | 1.89^{c} | |

15 µg/ml | 3.78^{c} | 1.87^{c} | 3.08 | |

30 µg/ml | 0.32^{c} | 0.15^{c} | 0.14^{c} | |

Rifampin (10 µM) | 29.80 | 3.70 | 7.93 |

ND, not determined due to sample analysis error.

↵

^{a}Values are relative to vehicle control, normalized to glyceraldehyde 3-phosphate dehydrogenase and are the average of triplicate determinations.↵

^{b}Anomalous data, possibly due to sample analysis error. Data were excluded from the curve fitting.↵

^{c}Data were excluded from the curve fitting because fold increase was <80% of the observed*E*_{max}value.