TABLE 3

Pharmacokinetic parameters following multiple ascending doses (day 7) of inhaled AV-101 or simulated oral imatinib 400 mg at steady state

AV-101
10 mg
AV-101
30 mg
AV-101
90 mg
Simulated
steady-state oral imatinib
400 mg
Imatinib898
 Cmax,ss, ng·mL−169.2±31.1214.8±88.2890.4±236.82155
 Cav, ng·mL−149.1±24.0159.6±64.5663.8±208.51251
tmax, h0.7 (0.1–2.0)0.1 (0.1–2.0)1.6 (0.17–2.1)3.3
 Cmin,ss, ng·mL−131.7±14.3118.2±47.4533.6±183.4
 AUCτ, ng·h·mL−1589.6±288.21915.6±773.87965.2±2501.7
 AUC0–24, ng·h·mL−130 033
N-desmethyl imatinib898
 Cmax,ss, ng·mL−19.9±6.530.0±12.5116.6±48.3
tmax, h1.0 (0.7–6.0)1.1 (0.7–9.0)2.1 (1.1–9.1)
 Cmin,ss, ng·mL−16.6±3.922.6±9.083.5±38.8
 AUCτ, ng·h·mL−1100.2±64.3322.2±134.71198.5±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.