Table 3.
Study 003: Pharmacokinetic Parameters on Days 1 and 14 After Multiple Doses of Lemborexant in Healthy Adult Japanese and White Subjects
| Lemborexant | ||||
|---|---|---|---|---|
| Japanese | White | |||
| Parameter | 2.5 mg (n = 6) | 10 mg (n = 6) | 25 mg (n = 6) | 10 mg (n = 6) |
| Cmax, ng/mL | ||||
| Day 1 | ||||
| Geometric mean (CV) | 10.0 (13.0) | 40.6 (63.5) | 140 (37.8) | 41.9 (54.5) |
| Mean (SD) | 10.0 (1.4) | 46.5 (25.8) | 148 (56.5) | 47.3 (28.1) |
| Day 14 | ||||
| Geometric mean (CV) | 12.8 (27.9) | 64.5 (48.6) | 203 (35.8) | 54.6 (48.3) |
| Mean (SD) | 13.2 (3.4) | 70.2 (30.2) | 213 (66.3) | 59.4 (26.1) |
| tmax, median (range), h | ||||
| Day 1 | 1.5 (1.0‐4.0) | 1.0 (0.5‐6.0) | 2.5 (1.0‐4.0) | 1.0 (1.0‐3.0) |
| Day 14 | 1.3 (0.5‐2.0) | 1.5 (0.5‐2.0) | 1.0 (1.0‐1.5) | 1.3 (1.0‐3.0) |
| AUC0‐24h, ng•h/mL | ||||
| Day 1 | ||||
| Geometric mean (CV) | 53.3 (26.9) | 229 (16.8) | 736 (21.2) | 194 (41.4) |
| Mean (SD) | 54.8 (13.1) | 231 (40.2) | 750 (154) | 208 (83.4) |
| Day 14 | ||||
| Geometric mean (CV) | 93.8 (21.1) | 446 (28.0) | 1480 (35.6) | 385 (55.3) |
| Mean (SD) | 95.6 (21.4) | 459 (110) | 1560 (559) | 431 (226) |
| t½,eff, mean (SD), h | 16.2 (5.5) | 16.7 (5.5) | 20.3 (9.5) | 15.8 (4.0) |
| RacCmax | ||||
| Day 14 | ||||
| Geometric mean (CV) | 1.3 (31.6) | 1.6 (25.1) | 1.5 (46.1) | 1.3 (47.2) |
| Mean (SD) | 1.3 (0.4) | 1.6 (0.4) | 1.6 (0.6) | 1.4 (0.7) |
| RacAUC0‐24h | ||||
| Day 14 | ||||
| Geometric mean (CV) | 1.8 (27.0) | 2.0 (27.2) | 2.0 (25.2) | 2.0 (18.4) |
| Mean (SD) | 1.8 (0.5) | 2.0 (0.5) | 2.1 (0.5) | 2.0 (0.4) |
AUC0‐24h indicates area under the concentration‐time curve from time 0 to time 24 hours; Cmax, maximum drug concentration; CV, coefficient of variation; Rac, accumulation ratio based on Cmax and AUC0‐24h; t½,eff, effective half‐life; tmax, time to reach maximum (peak) concentration following drug administration.