Table 2.
Cohort | ID | Drug | Study state | Dose, mg | Plasma conc., μg/mL | SV2A occupancy, % | V ND, mL/cm3 | IC 50, μg/mL, individual | IC 50, μg/mL, global |
---|---|---|---|---|---|---|---|---|---|
2 | 5 | BRV | Postdose | 100 | 1.04 | 66 | 2.28 | N/A | 0.51 |
6 | 100 | 0.98 | 70 | 3.06 | |||||
7 | 200 | 3.61 | 85 | 2.93 | |||||
8 | 200 | 2.94 | 84 | 2.36 | |||||
9 | 50 | 0.53 | 50 | 1.50 | |||||
5 | LEV | 1500 | 16.2 | 78 | 2.57 | N/A | 4.90 | ||
6 | 1500 | 16.5 | 78 | 2.79 | |||||
7 | 1500 | 23.1 | 84 | 2.86 | |||||
8 | 1500 | 23.6 | 78 | 2.76 | |||||
3 | 10 | BRV | Postdose | 100 | 1.63 | 74 | 3.25 | 0.54 | 0.45 |
SS peak | 2.91 | 86 | 3.05 | ||||||
SS trough | 1.7 | 76 | 3.80 | ||||||
11 | Postdose | 50 | 0.98 | 72 | 3.73 | 0.44 | |||
SS peak | 1.61 | 76 | 3.78 | ||||||
SS trough | 0.84 | 64 | 3.97 | ||||||
12 | Postdose | 100 | 1.23 | 80 | 3.08 | 0.32 | |||
SS peak | 2.53 | 87 | 2.90 | ||||||
SS trough | 1.43 | 82 | 3.24 | ||||||
13 | Postdose | 50 | 0.91 | 67 | 3.04 | 0.50 | |||
SS peak | 1.99 | 78 | 2.71 | ||||||
SS trough | 1.22 | 70 | 2.89 | ||||||
12 | LEV | Postdose | 250 | 3.65 | 58 | 4.01 | N/A | 3.58 | |
13 | Postdose | 600 | 10.7 | 68 | 2.51 | ||||
11 | Postdose | 250 | 4.25 | 52 | 2.10 | ||||
2 and 3 | BRV | 0.46 | |||||||
LEV | 4.02 |
BRV, brivaracetam; conc., concentration; ID, subject identifier; LEV, levetiracetam; N/A, not available; SS, steady state.