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. 2022 Oct 17;15(12):2899–2908. doi: 10.1111/cts.13417

TABLE 4.

Simulated percentage of participants with minimum Bruton's tyrosine kinase receptor occupancy above the four thresholds of interest (70%, 80%, 90%, and 95%) over 24 h at steady‐state for different dose/regimen and food state combinations

BTKO threshold Prandial state 25 mg 50 mg 75 mg 100 mg 200 mg
Simulated % of participants
q.d. dosing regimen
0.70 Fasted 98 100 100 100 100
0.80 88 97 99 99 100
0.90 36 59 71 77 87
0.95 4 13 20 24 39
0.70 Fed 99 100 100 100 100
0.80 95 99 99 99 100
0.90 54 74 82 85 92
0.95 10 22 29 34 51
b.i.d. dosing regimen
0.70 Fasted 100 100 100 100 100
0.80 99 100 100 100 100
0.90 88 97 99 100 100
0.95 38 68 81 86 94
0.70 Fed 100 100 100 100 100
0.80 100 100 100 100 100
0.90 96 99 100 100 100
0.95 59 85 90 93 97

Abbreviations: b.i.d., twice‐daily; BTKO, Bruton's tyrosine kinase occupancy; q.d., once‐daily.