TABLE 3.
Mean pharmacokinetic parameters of tolebrutinib part B (MAD)
| Dose, mg | Day 1 | Day 10 | ||||||
|---|---|---|---|---|---|---|---|---|
| Cmax, ng/ml | Tmax, h a | AUC0‐24, ng.h/ml | t 1/2, h | Cmax, ng/ml | Tmax, h a | AUC0‐24, ng.h/ml | t 1/2, h | |
| 7.5 (n = 8) | 1.17 (57%) | 1.0 (0.5–1.5) | 2.12 (51%) | 1.45 (22%) | 1.32 (31%) | 1.0 (0.5–2.0) | 3.07 (51%) | 1.57 (50%) |
| 15 (n = 8) | 1.96 (41%) | 1.0 (0.5–1.5) | 3.82 (43%) | 1.40 (16%) | 2.51 (60%) | 1.0 (1.0–1.5) | 5.85 (33%) | 1.68 (21%) |
| 30 (n = 8) | 6.25 (75%) | 0.75 (0.5–1.0) | 9.67 (68%) | 1.6 (24%) | 7.46 (74%) | 1.0 (0.5–2.0) | 14.9 (75%) | 2.02 (34%) |
| 60 (n = 8) | 8.47 (80%) | 1.25 (1.0 −3.0) | 24.3 (61%) | 1.98 (45%) | 6.69 (66%) | 1.5 (1.0–2.0) | 18.2 (55%) | 2.37 (44%) |
| 90 (n = 8) | 19.3 (48%) | 1.0 (0.5–1.0) | 35.5 (46%) | 2.1 (30%) | 21.7 (60%) | 1.5 (1.0–2.5) | 56.6 (54%) | 2.83 (30%) |
Abbreviations: AUC, area under the time‐concentration curve; Cmax, peak serum concentration after a single dose; MAD, multiple ascending dose; t 1/2, terminal half‐life; Tmax, time at which Cmax is obtained.
a
Median value (min – max).