Table 2.
AZ’9567 | 3 mg/kg, BID | 10 mg/kg, BID | 30 mg/kg, BID | |||
---|---|---|---|---|---|---|
day 1 | day 7 | day 1 | day 7 | day 1 | day 7 | |
Free AUC24h (µM*h) | 0.69 ± 0.07 | 0.76 ± 0.11 | 2.6 ± 1.1 | 3.9 ± 0.70 | 12 ± 1.1 | 9.9 ± 2.2 |
Free Cmax (µM) | 0.04 ± 0.004 | 0.05 ± 0.01 | 0.21 ± 0.06 | 0.27 ± 0.11 | 0.87 ± 0.19 | 0.68 ± 0.19 |
Free Cmin24h (µM) | 0.01 ± 0.001 | 0.01 ± 0.002 | 0.04 ± 0.02 | 0.08 ± 0.03 | 0.14 ± 0.04 | 0.15 ± 0.05 |
Fold cover of 1MAT2A biochemical IC50 at mean free Cmin24h | 9 | 9 | 35 | 78 | 143 | 147 |
Mean, SD, n = 5
1as shown in Table 1