Substrate-related parameters for victims of CYP3A4
| Victim Drug | fm | fm, CYP3A4 | fgut (Static Model) | Linear Dose Range from Clinical Phase I Studies |
|---|---|---|---|---|
| mg | ||||
| AZ5 | 1 | 1 | 0.5 | 50–500; small departure from linearity at 500 mg |
| AZ6 | 0.87 | 1 | 0.56 | 50–500 |
| AZ7 | 1 | 1 | 0.43 | 70–220 |
| AZ8 | 1 | 1 | 0.23 | Up to 180 |
| AZ9 | 0.53 | 0.16 | 0.5 | 3–15 |
| AZ10 | 1 | >0.7 | 0.5 | Up to 400 |
| Midazolam | 0.94 | 1 | 0.57 | |
| Simvastatin | 0.93 | 0.99 | 0.66 |
fm, fraction metabolized in the liver; fm,CYP3A4, fraction metabolized by CYP3A4; fgut, fraction escaping gut metabolism, assumed to be 0.5 for AZ5, AZ9, and AZ10.