TABLE 2.
Source | KI | kinact | Reference |
---|---|---|---|
μM | h−1 | ||
Human liver microsomes | 5.49 | 4.32 | Mayhew et al., 2000 |
CYP3A4 + b5 Supersomes | 4.12 | 13.8 | Jones et al., 2007 |
Human liver microsomes | 37.0–41.4 | 2.5–2.8 | Ito et al., 2003 |
Recombinant CYP3A4a | 2.25 | 2.4 | Polasek and Miners, 2006 |
Human liver microsomesa | 29.5 | 3.0 | Polasek and Miners, 2006 |
In vivo estimate | 5.3 | 0.4 (liver); 4 (intestine) |
Determined by 6β-hydroxylation of testosterone.