Table 3.
Pharmacokinetic results for single dose of simotinib
| Parameters(mean ± SD) | 100 mg N=2 |
200 mg N=3 |
300 mg N=3 |
400 mg N=15 |
500 mg N=12 |
650 mg N=6 |
|---|---|---|---|---|---|---|
| T1/2, h | 5.3±0.3 | 12.2±3.5 | 9.2±1.0 | 13.3±6.3 | 28.0±33.8 | 29.7±32.2 |
| Tmax, h | 1.8 (1.5–2.0) | 2.0 (2.0–2.0) | 1.5 (1.5–2.0) | 2.0 (1.0–8.0) | 1.8 (0.5–4.0) | 2.0 (1.0–6.0) |
| Cmax, ng/mL | 56.5±18.2 | 333.0±35.4 | 552.5±388.2 | 566.4±372.0 | 514.5±316.4 | 828.5±849.0 |
| AUC0-last, ng•hr/mL | 405.6±94.8 | 2,339.6±479.9 | 2,814.0±764.5 | 3,581.9±1,868.5 | 3,791.0±2,741.1 | 4,652.1±3,442.1 |
| AUC0-∞, ng•hr/mL | 466.2±129.9 | 2,955.0±564.0 | 3,243.8±776.1 | 4,962.1±3,141.7 | 6,483.8±5,008.4 | 7,648.4±3,028.7 |
| CL, L/h | 223.1±62.2 | 68.9±13.2 | 95.2±22.8 | 127.4±117.6 | 200.5±300.1 | 97.7±39.2 |
| Vd, L | 1,704.0±385.8 | 1,250.1±579.7 | 1,286.1±438.6 | 2,097.2±1,506.8 | 7,166.6±12,246.1 | 3,873.8±3,378.1 |
Abbreviations: AUC0-t, area under the curve from time 0 to the last measurable plasma concentration; AUC0-∞, area under the curve from time 0 to infinity; CL, total body clearance; Cmax, maximum plasma concentration; Tmax, time to maximum concentration; T1/2, half-life; Vd, volume distribution.