Table 2.
Plasma pharmacokinetics of NYX‐2925: single ascending dose groups
| Parameter (units) | Group 1 & CSF cohort 50 mg (n = 12) | Group 2 150 mg (n = 6) | Elderly cohort 300 mg (n = 6) | Group 3 400 mg fasting (n = 6) | Group 3 400 mg fed (n = 6) | Group 4 800 mg (n = 6) | Group 5 1,200 mg (n = 6) |
|---|---|---|---|---|---|---|---|
| Cmax (μg/mL) | 0.8 (31.5) | 2.7 (24.3) | 5.0 (26.3) | 5.5 (25.1) | 4.9 (14.0) | 12.4 (26.3) | 20.1 (24.8) |
| Tmax (h) | 1.0 (0.5–2.8) | 1.0 (1.0–2.0) | 1.25 (1.0–2.0) | 1.5 (1.0–2.0) | 3.0 (1.5–4.0) | 1.25 (1.0–4.0) | 1.5 (1.0–3.0) |
| AUC0–last (h*μg/mL) | 4.4 (17.8) | 14.1 (11.1) | 28.5 (23.4) | 34.2 (13.7) | 35.6 (15.5) | 71.5 (7.7) | 113.7 (17.6) |
| AUC0–24 (h*μg/mL) | 4.4 (17.8) | 14.1 (11.1) | 28.5 (23.4) | 34.2 (13.7) | 35.6 (15.5) | 71.5 (7.7) | 113.7 (17.6) |
| AUC0–∞ (h*μg/mL) | 4.5 (16.7) | 14.3 (11.2) | 29.0 (23.1) | 35.1 (13.2) | 36.4 (15.6) | 72.7 (7.7) | 116.2 (17.6) |
| t1/2 (hour) | 3.9 (20.5) | 3.6 (7.8) | 4.0 (11.2) | 4.4 (23.0) | 3.9 (10.5) | 3.9 (19.7) | 4.3 (12.7) |
| CL/F (L/h) | 11.0 (16.7) | 10.5 (11.3) | 10.3 (23.1) | 11.4 (13.4) | 11.0 (15.5) | 11.0 (7.6) | 10.3 (17.8) |
| Vd/F (L) | 62.1 (31.0) | 54.1 (10.1) | 60.0 (29.1) | 71.6 (28.2) | 61.2 (15.2) | 61.9 (21.1) | 64.7 (20.1) |
AUC0–24, area under the plasma concentration‐time curve from 0–24 hours; AUC0‐∞, area under the plasma concentration‐time curve from 0 to infinity; AUC0–last, area under the plasma concentration‐time curve from 0 to last collection time after drug administration; CL/F, apparent oral clearance; Cmax, maximum plasma concentration; CSF, cerebrospinal fluid; t1/2, apparent terminal elimination half‐life; Tmax, time to maximum plasma concentration; Vd/F, apparent volume of distribution.
Data are geometric mean (% coefficient of variation), except Tmax is median (minimum‐maximum).