Induction effects of apixaban on P450 enzyme activities in primary cultures of human hepatocytes
| Treatment Group | Concentration | -Fold Inductiona | ||
|---|---|---|---|---|
| CYP1A2b | CYP2B6b | CYP3A4/5b | ||
| DMSO | 0.1% | 1.00 ± 0.37 | 1.00 ± 0.30 | 1.00 ± 0.27 |
| Apixaban | 0.2 μM | 0.973 ± 0.003 | 0.892 ± 0.049 | 0.984 ± 0.005 |
| Apixaban | 2.0 μM | 0.934 ± 0.028c | 0.934 ± 0.044 | 0.907 ± 0.134 |
| Apixaban | 20 μM | 0.928 ± 0.037c | 1.12 ± 0.20 | 1.23 ± 0.21 |
| Omeprazole | 100 μM | 37.4 ± 1.2 | 11.0 ± 10.9 | 2.50 ± 1.34 |
| Phenobarbital | 750 μM | 2.03 ± 0.44 | 22.0 ± 22.4 | 7.36 ± 3.99 |
| Rifampin | 10 μM | 2.19 ± 0.14 | 13.1 ± 6.8 | 8.97 ± 5.16 |
↵a -Fold induction determined from rate for treatment group divided by rate for control. Values are the mean ± S.D. of three human hepatocyte preparations.
↵b Significance found among treatment groups (where 0.1% DMSO is the vehicle control) according to Kruskal-Wallis one-way analysis on ranks (p < 0.05) but unable to specify the groups that statistically differ from the other groups according to Dunnett's test with positive controls.
↵c Statistically significant according to Dunnett's test (p < 0.05) without positive controls.