In vitro P450 inhibition parameters for AMIO and MDEA
| Inhibition of CYP2C9 | Inhibition of CYP2D6 | Inhibition of CYP3A | ||||
|---|---|---|---|---|---|---|
| Ki | TDI (KI, kinact) | Ki | TDI (KI, kinact) | Ki | TDI (KI, kinact) | |
| μM | μM | μM | ||||
| AMIO | 94.6 | 7.89 μM, 0.005 min-1 a | 45.1 | No | 271.6 | 13.4 μM, 0.06 min−1 |
| MDEA | 2.3 | No | 4.5 | 1.3 μM, 0.12 min−1 | 12.1 | No |
↵a In-house data following the methodology referred to Sodhi et al. (2014); all other data from Ohyama et al. (2000b). Ki and KI here are apparent values, and are corrected for free fraction in microsome (fu,mic = 0.012) estimated in the Simcyp model.