Inactivation parameters estimated for ERY, nd-ERY, DTZ, and nd-DTZ with CYP3A4 (+b5) and HLMs
Data are presented as mean ± S.D.
rCYP3A4 (+b5) | HLMs | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| KI | kinact | kinact/KI | KI | kinact | kinact/KI | |||||
| μM | min-1 | min-1 mM-1 | μM | min-1 | min-1 mM-1 | |||||
| ERY | 5 ± 2.3 | 0.34 ± 0.07 | 70 | 15.7 ± 1.9 | 0.09 ± 0.01 | 6 | ||||
| nd-ERY | 5.7 ± 1.3 | 0.34 ± 0.13 | 60 | 11.6 ± 1.9 | 0.10 ± 0.15 | 9 | ||||
| DTZ | 1.3 ± 0.1 | 0.28 ± 0.01 | 220 | 3.7 ± 1.7 | 0.07 ± 0.01 | 20 | ||||
| nd-DTZ | 0.3 ± 0.1 | 0.4 ± 0.03 | 1333 | 0.6 ± 0.1 | 0.08 ± 0.02 | 133 | ||||