Table 2.
Study 002: Pharmacokinetic Parameters on Days 1 and 14 After Multiple Doses of Lemborexant in Healthy Adult and Elderly Subjects
| Lemborexant | |||||||
|---|---|---|---|---|---|---|---|
| Parameter | 2.5 mg(n = 6) | 5 mg(n = 6) | 10 mg(n = 6) | 25 mg(n = 6) | Elderly 25 mg (n = 5) | 50 mg(n = 6) | 75 mg(n = 6) |
| Cmax, ng/mL | |||||||
| Day 1 | |||||||
| Geometric mean (CV) | 9.5 (39.7) | 18.1 (42.0) | 28.0 (48.3) | 89.4 (26.9) | 72.1 (49.0) | 187 (39.2) | 203 (51.2) |
| Mean (SD) | 10.1 (4.3) | 19.4 (7.9) | 30.4 (13.1) | 92.0 (24.0) | 79.4 (43.1) | 199 (81.2) | 223 (103) |
| Day 14 | |||||||
| Geometric mean (CV) | 14.8 (30.6) | 22.0 (49.1) | 44.8 (35.7) | 102 (32.0) | 120 (41.8) | 218 (16.5) | 401 (35.3) |
| Mean (SD) | 15.4 (4.7) | 24.0 (10.7) | 46.9 (14.5) | 107 (38.9) | 128 (47.0) | 220 (33.5) | 420 (140) |
| tmax, median (range), h | |||||||
| Day 1 | 2.0 (1.5‐4.0) | 1.3 (1.0‐3.0) | 3.3 (1.0‐12.0) | 1.5 (1.0‐5.0) | 3.0 (2.0‐5.0) | 2.0 (1.0‐4.0) | 3.0 (1.0‐5.0) |
| Day 14 | 2.0 (1.0‐3.0) | 1.0 (1.0‐3.0) | 1.8 (1.0‐4.0) | 3.0 (1.5‐5.0) | 2.0 (1.5‐4.0) | 2.0 (2.0‐3.0) | 2.0 (1.0‐2.0) |
| AUC0‐24h, ng•h/mL | |||||||
| Day 1 | |||||||
| Geometric mean (CV) | 57.5 (27.3) | 104 (34.4) | 182 (25.2) | 540 (19.2) | 538 (49.4) | 899 (31.3) | 1230 (23.5) |
| Mean (SD) | 59.4 (17.5) | 108 (34.9) | 187 (47.9) | 549 (104) | 596 (347) | 931 (253) | 1260 (301) |
| Day 14 | |||||||
| Geometric mean (CV) | 116 (30.6) | 169 (49.5) | 321 (52.7) | 1050 (36.0) | 1170 (31.0) | 2220 (28.5) | 3710 (23.5) |
| Mean (SD) | 120 (38.0) | 186 (87.5) | 357 (193) | 1100 (387) | 1210 (335) | 2300 (758) | 3790 (857) |
| t½,eff, h, mean (SD) | 24.7 (7.3) | 18.0 (6.5) | 20.9 (10.7) | 23.0 (10.9) | 29.9 (18.2) | 31.3 (11.6) | 45.3 (23.2) |
| RacCmax | |||||||
| Day 14 | |||||||
| Geometric mean (CV) | 1.6 (22.4) | 1.2 (28.4) | 1.6 (49.4) | 1.2 (43.0) | 1.7 (54.2) | 1.2 (32.1) | 2.3 (41.5) |
| Mean (SD) | 1.6 (0.3) | 1.3 (0.3) | 1.8 (0.8) | 1.3 (0.5) | 1.9 (1.0) | 1.2 (0.4) | 2.4 (0.9) |
| RacAUC0‐24h | |||||||
| Day 14 | |||||||
| Geometric mean (CV) | 2.0 (20.7) | 1.6 (22.9) | 1.8 (29.4) | 1.9 (35.9) | 2.2 (49.1) | 2.5 (27.9) | 3.1 (41.2) |
| Mean (SD) | 2.1 (0.4) | 1.7 (0.4) | 1.8 (0.6) | 2.0 (0.6) | 2.4 (1.1) | 2.5 (0.7) | 3.3 (1.4) |
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.