TABLE 1

CYP3A4 inactivation kinetic 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 SubstrateKIkinactkinact/KIt1/2Partition Ratio
μMmin−1min-1mM−1min
Testosterone3.26 ± 0.610.027 ± 0.0028.425.40N.D
Midazolam9.03 ± 2.850.088 ± 0.0119.87.85N.D
Rivaroxaban4.17 ± 0.930.068 ± 0.00516.410.1241
  • N.D., not determined.