Inactivation parameters KI (μM) and kinact (min−1) for time-dependent P450 inactivation by deleobuvir, CD 6168, and deleobuvir-AG
| P450 Isoform | Deleobuvir | CD 6168 | Deleobuvir-AG | ||||||
|---|---|---|---|---|---|---|---|---|---|
| KI | kinact | KI | kinact | KI | kinact | ||||
| Total | Freea | Total | Free | Total | Free | ||||
| μM | μM | min–1 | μM | μM | min–1 | μM | μM | min–1 | |
| CYP1A2 | 28.1 | 8.99 | 0.0256 | NA | NA | NA | 54.6 | 8.74 | 0.044 |
| CYP2B6 | NA | NA | NA | NA | NA | NA | NA | NA | NA |
| CYP2C8 | 0.107 | 0.066 | 0.0268 | 0.206 | 0.045 | 0.022 | 0.0521 | 0.0083 | 0.0521 |
| CYP3A4 | 103 | 13.4 | 0.0485 | 201 | 46.6 | 0.0875 | NA | NA | NA |
NA, no inactivation observed.
↵a Adjusted for protein binding in HLM.