AV-101 10 mg | AV-101 30 mg | AV-101 90 mg | Simulated steady-state oral imatinib 400 mg | |
Imatinib | 8 | 9 | 8 | |
Cmax,ss, ng·mL−1 | 69.2±31.1 | 214.8±88.2 | 890.4±236.8 | 2155 |
Cav, ng·mL−1 | 49.1±24.0 | 159.6±64.5 | 663.8±208.5 | 1251 |
tmax, h | 0.7 (0.1–2.0) | 0.1 (0.1–2.0) | 1.6 (0.17–2.1) | 3.3 |
Cmin,ss, ng·mL−1 | 31.7±14.3 | 118.2±47.4 | 533.6±183.4 | |
AUCτ, ng·h·mL−1 | 589.6±288.2 | 1915.6±773.8 | 7965.2±2501.7 | |
AUC0–24, ng·h·mL−1 | 30 033 | |||
N-desmethyl imatinib | 8 | 9 | 8 | |
Cmax,ss, ng·mL−1 | 9.9±6.5 | 30.0±12.5 | 116.6±48.3 | |
tmax, h | 1.0 (0.7–6.0) | 1.1 (0.7–9.0) | 2.1 (1.1–9.1) | |
Cmin,ss, ng·mL−1 | 6.6±3.9 | 22.6±9.0 | 83.5±38.8 | |
AUCτ, ng·h·mL−1 | 100.2±64.3 | 322.2±134.7 | 1198.5±532.6 |
Data are presented as n, mean±sd or median (range). Pharmacokinetic parameters were estimated using noncompartmental analyses. Cmax,ss: maximum observed concentration during a dosing interval at steady state; Cav: average concentration during a dosing interval at steady state; tmax: time of the maximum observed concentration; Cmin,ss: minimum observed concentration during a dosing interval at steady state; AUCτ: area under the curve for the 0–12-h dosing interval at steady state; AUC0–24: area under the curve from 0 to 24 h.