Pharmacokinetic parameters following single ascending dose of inhaled AV-101 or oral imatinib 400 mg
| AV-101 1 mg | AV-101 3 mg | AV-101 10 mg | AV-101 30 mg | AV-101 90 mg | Oral imatinib 400 mg | |
| Imatinib | 6 | 6 | 6 | 6 | 6 | 8 |
| Cmax, ng·mL−1 | 1.2±0.6 | 3.8±0.5 | 20.2±4.8 | 73.8±9.2 | 423.8±253.1 | 1712.1±483.7 |
| tmax, h | 3.0 (0.1–4.0) | 2.0 (0.1–2.0) | 0.2 (0.1–1.1) | 2.0 (0.7–6.1) | 2.1 (1.1–2.1) | 4.0 (2.0–4.0) |
| AUC0-t, ng·h·mL−1 | 9.9±10.9 | 65.4±13.7 | 319.0±54.0 | 1279.3±306.0 | 6673.9±3251.8 | 32 665.8±7641.0 |
| MRT0-t, h | 4.8±3.1 | 15.0±4.2 | 21.0±0.7 | 18.4±2.1 | 17.2±2.3 | 19.5±1.2 |
| t½, h | 9.0±2.2# | 19.6±4.0 | 20.0±1.1 | 19.3±2.9 | 16.1±2.5 | 15.4±1.4 |
| N-desmethyl imatinib | 4 | 6 | 6 | 6 | 6 | 8 |
| Cmax, ng·mL−1 | 0.1±0.1 | 0.4±0.1 | 1.4±0.3 | 6.2±1.3 | 33.2±14.7 | 228.9±61.3 |
| tmax, h | 6.0 (4.0–6.2) | 6.0 (6.0–6.0) | 6.0 (6.0–6.0) | 6.1 (1.0–9.0) | 6.1 (2.1–9.1) | 2.0 (2.0–4.0) |
| AUC0-t, ng·h·mL−1 | 2.6±NR¶ | 11.8±4.1 | 45.8±8.6 | 182.6±45.7 | 986.5±433.6 | 4783.9±1457.3 |
| MRT0-t, h | 9.0±NR¶ | 22.0±7.0 | 28.4±1.0 | 25.3±2.8 | 26.4±1.5 | 24.9±1.2 |
| t½, h | NR±NC+ | 34.8±9.2 | 40.5±8.4 | 32.2±3.5 | 31.9±5.6 | 32.5±4.5 |
Data are presented as n, mean±sd or median (range). Pharmacokinetic parameters were estimated using noncompartment analyses. Cmax: maximum observed concentration; tmax: time of maximum observed concentration; AUC0-t: area under the concentration–time curve from dose administration at time 0 to tlast, where tlast is the time of last measurable observed concentration; MRT: mean residence time; t½: half-life; NR: not reportable; NC: not calculated. #: n=3; ¶: n=2; +: n=1.