Table 3.
BKI-1812 | 60 mg/kg | 30 mg/kg | 15 mg/kg |
---|---|---|---|
Time sampled | Plasma concentration (μM) | ||
predose | 15.7 ± 11.7 | 2.1 ± 0.2 | 1.5 ± 0.3 |
1 h post dose | 258.9 ± 22.5 | 111.4 ± 71 | 49.4 ± 26.3 |
2 h post dose | 250.5 ± 48.4 | 115.7 ± 65.9 | 37.4 ± 19.3 |
4 h post dose | 170.1 ± 110.8 | 54.6 ± 31.7 | 14.1 ± 9.2 |
BKI-1814 | 60 mg/kg | 30 mg/kg | 15 mg/kg |
Time sampled | Plasma concentration (μM) | ||
predose | 1.83 ± 1.4 | 0.03 ± 0.06 | 0.24 ± 0.2 |
0.5 h post dose | 17.5 ± 10.7 | 7.1 ± 2.5 | 1.68 ± 0.6 |
1 h post dose | 19.5 ± 9.8 | 6.88 ± 1.5 | 2.46 ± 0.5 |
2 h post dose | 18.2 ± 10.2 | 5.86 ± 1.6 | 2.25 ± 0.8 |
BKI-1649* | 60 mg/kg | 30 mg/kg | 15 mg/kg |
Time sampled | Plasma concentration (μM) | ||
predose | 346 ± 78 | 113 ± 31 | 76 ± 1.2 |
0.5 h post dose | 340 ± 177 | 110 ± 65 | 79 ± 44 |
1 h post dose | 345 ± 188 | 111 ± 66 | 82 ± 46 |
2 h post dose | 360 ± 199 | 134 ± 81 | 93 ± 51 |
BKI-1649 formed in vivo by demethylation of ether on BKI-1814