CYP3A4 reversible inhibition parameters for INF derived using either testosterone 6β-hydroxylation, midazolam 1’-hydroxylation, or morpholinone hydroxylation of rivaroxaban as surrogate markers of residual CYP3A activity
Data are presented as means ± S.D.
| Probe Substrate | IC50 | Ki | Mode of Inhibition |
|---|---|---|---|
| μM | μM | ||
| Testosterone | 2.04 ± 0.29 | N.D | N.D |
| Midazolam | 2.91 ± 0.54 | N.D | N.D |
| Rivaroxaban | 0.80 ± 0.08 | 0.97 ± 0.06 | Noncompetitive |
N.D., not determined.