TABLE 4.
BTKO threshold | Food state | Simulated % of participants | |||||||
---|---|---|---|---|---|---|---|---|---|
10 mg | 25 mg | 35 mg | 45 mg | 50 mg | 75 mg | 100 mg | 200 mg | ||
q.d. dosing regimen | |||||||||
0.70 | Fasted | 93 | 99 | 100 | 100 | 100 | 100 | 100 | 100 |
0.80 | 79 | 95 | 97 | 98 | 98 | 99 | 99 | 100 | |
0.90 | 43 | 70 | 77 | 81 | 83 | 88 | 90 | 94 | |
0.95 | 12 | 31 | 39 | 46 | 48 | 55 | 60 | 72 | |
0.70 | Fed | 97 | 100 | 100 | 100 | 100 | 100 | 100 | 100 |
0.80 | 89 | 97 | 98 | 99 | 99 | 100 | 100 | 100 | |
0.90 | 57 | 79 | 85 | 87 | 88 | 92 | 93 | 96 | |
0.95 | 20 | 43 | 51 | 55 | 57 | 64 | 70 | 79 | |
b.i.d. dosing regimen | |||||||||
0.70 | Fasted | 99 | 100 | 100 | 100 | 100 | 100 | 100 | 100 |
0.80 | 96 | 100 | 100 | 100 | 100 | 100 | 100 | 100 | |
0.90 | 78 | 94 | 97 | 98 | 99 | 99 | 100 | 100 | |
0.95 | 45 | 72 | 81 | 85 | 87 | 92 | 94 | 96 | |
0.70 | Fed | 100 | 100 | 100 | 100 | 100 | 100 | 100 | 100 |
0.80 | 98 | 100 | 100 | 100 | 100 | 100 | 100 | 100 | |
0.90 | 88 | 97 | 99 | 99 | 99 | 100 | 100 | 100 | |
0.95 | 60 | 84 | 89 | 93 | 93 | 95 | 96 | 98 |
Abbreviations: b.i.d., twice daily; BTKO, Bruton's tyrosine kinase occupancy; q.d., once daily.