Table 1.
Sotrastaurin pharmacokinetics
| Parameter | Sotrastaurin alone | Sotrastaurin with ketoconazole |
|---|---|---|
| Sotrastaurin | ||
| tmax (h) | 2 (0.5–3) | 2.5 (1.5–4) |
| Cmax (ng ml−1) | 285 ± 128 | 678 ± 189 |
| AUC(0,t) (ng ml−1 h) | 1619 ± 807 | 7282 ± 2972 |
| AUC (ng ml−1 h) | 1666 ± 808 | 7378 ± 3011 |
| t1/2 (h) | 5.9 ± 1.7 | 10.6 ± 2.5 |
| N-desmethyl-sotrastaurin | ||
| tmax (h) | 2.5 (1–3.1) | 4 (2–6) |
| Cmax (ng ml−1) | 7.5 ± 3.6 | 9.6 ± 2.9 |
| AUC(0,t) (ng ml−1 h) | 20 ± 13 | 98 ± 49 |
| Metabolic ratio | 0.012 ± 0.007 | 0.014 ± 0.008 |
Values are mean ± SD except for tmax which is median (range). tmax is time to reach maximum concentration; Cmax is maximum concentration; AUC is area under the concentration–time curve; t1/2 is half-life.