TABLE 4.
Tolebrutinib BTK occupancy part B (MAD)
| Dose (h postdose) | Placebo a | 7.5 mg | 15 mg | 30 mg | 60 mg | 90 mg |
|---|---|---|---|---|---|---|
| D1 (4) | 4 ± 5 | 21 ± 16 | 56 ± 13 | 71 ± 22 | 94 ± 1 | 94 ± 1 |
| D1 (24) | 4 ± 7 | 21 ± 18 | 51 ± 13 | 64 ± 22 | 93 ± 2 | 91 ± 2 |
| D10 (4) | 7 ± 8 | 87 ± 5 | 95 ± 1 | 96 ± 1 | 96 ± 1 | 97 ± 1 |
| D10 (24) | 4 ± 8 | 78 ± 6 | 88 ± 3 | 82 ± 2 | 93 ± 2 | 93 ± 2 |
| D10 (48) | 4 ± 6 | 62 ± 10 | 74 ± 3 | 74 ± 3 | 85 ± 3 | 82 ± 4 |
| D10 (168) | 1 ± 1 | 7 ± 8 | 13 ± 13 | 12 ± 10 | 6 ± 9 | 26 ± 7 |
Abbreviations: BTK, Bruton’s tyrosine kinase; MAD, multiple ascending dose.
a
Placebo from all MAD cohorts at respective nominal time points.