Drug | Treatment | CYP3A4 mRNAa | ||
---|---|---|---|---|
Donor 1 | Donor 2 | Donor 3 | ||
ASV | Donor | HC3-15 | HC1-18 | HC5-10 |
DMSO (0.1%) | 1 | 1 | 1 | |
0.049 µg/ml | 3.73b | 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 | 8.7c | 4.73c | 3.7 | |
20 µg/ml | 4.95c | 2.39c | 1.74c | |
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 | 3.88c | 2.09 | 2.45 | |
15 µg/ml | 2.70c | 1.38c | 1.43c | |
30 µg/ml | 0.29c | 0.08c | 0.26c | |
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 | 5.24c | 2.14 | 1.89c | |
15 µg/ml | 3.78c | 1.87c | 3.08 | |
30 µg/ml | 0.32c | 0.15c | 0.14c | |
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 Emaxvalue.