CYP3A4 and CYP2J2 inactivation kinetic parameters for amiodarone, NDEA, dronedarone, and NDBD using morpholinone hydroxylation of rivaroxaban as a surrogate measurement of residual enzymatic activity
Data represent means ± S.D.
| P450 | KI | kinact | kinact/KI |
|---|---|---|---|
| μM | min−1 | min−1/mM−1 | |
| CYP3A4 | |||
| Amiodarone | 0.45 ± 0.12 | 0.058 ± 0.0045 | 129 |
| NDEA | 0.095 ± 0.070 | 0.037 ± 0.0056 | 389 |
| Dronedarone | 0.30 ± 0.087 | 0.056 ± 0.0046 | 185 |
| NDBD | 0.88 ± 0.26 | 0.047 ± 0.0052 | 53.7 |
| CYP2J2 | |||
| Amiodarone | NA | NA | NA |
| NDEA | NA | NA | NA |
| Dronedarone | 0.031 ± 0.017 | 0.021 ± 0.0017 | 677 |
| NDBD | 0.037 ± 0.014 | 0.025 ± 0.0014 | 676 |
NA, not applicable.