Table 1.
Selected plasma AJM300 and HCA2969 pharmacokinetic parameters
| Day 1 | Day 10 | |||||
|---|---|---|---|---|---|---|
| 240 mg (n=6) | 480 mg (n=5) | 960 mg (n=6) | 240 mg (n=6) | 480 mg (n=5) | 960 mg (n=6) | |
| AJM300 | ||||||
| C trough (ng mL −1 ) | 0.49 (0.43) | 2.19 (1.10) | 2.77 (2.11) | 0.60 (0.52) | 1.49 (0.36) | 2.00 (1.57) |
| C max 24h (ng mL −1 ) | 121.90 (72.71) | 292.20 (257.31) | 527.33 (551.13) | 195.00 (40.03) | 278.20 (87.51) | 501.17 (269.59) |
| AUC 24h (ng·h mL −1 ) | 755.33 (310.80) | 1667.26 (559.66) | 3134.36 (1307.14) | 1186.95 (176.07) | 2408.00 (617.91) | 3120.62 (788.25) |
| T max 24h (h) | 10.00 (9.00, 13.00) | 10.00 (10.00, 13.00) | 6.00 (4.00, 10.00) | 10.00 (9.00, 10.00) | 9.00 (8.00, 9.00) | 10.00 (9.00, 10.00) |
| t 1/2 (h) | 1.43 (0.14)‡ | 6.01 (6.64) | 3.98 (5.87) | 1.45 (0.14)† | 24.83 (46.14) | 5.60 (8.24) |
| fe (%) | 0.0003 (0.0004) | 0.0007 (0.0002) | 0.0007 (0.0005) | 0.0005 (0.0003) | 0.0006 (0.0006) | 0.0005 (0.0005) |
| HCA2969 | ||||||
| C trough (ng mL −1 ) | 53.98 (5.98) | 103.38 (45.51) | 191.97 (115.43) | 48.52 (4.89) | 103.72 (29.33) | 168.67 (64.95) |
| C max 24h (ng mL −1 ) | 465.50 (200.11) | 1251.00 (612.71) | 1989.17 (1104.53) | 824.17 (129.86) | 1732.00 (354.43) | 2246.67 (1018.56) |
| AUC 24h (ng mL −1 ) | 4709.99 (1591.89) | 11 312.82 (3603.00) | 18 978.42 (7684.07) | 7660.10 (1916.43) | 17 457.26 (3476.98) | 19 790.21 (5600.69) |
| T max 24h (h) | 10.00 (10.00, 10.00) | 10.00 (10.00, 11.00) | 10.50 (10.00, 11.00) | 9.50 (7.00, 10.00) | 9.00 (9.00, 10.00) | 10.00 (10.00, 10.00) |
| t 1/2 (h) | 6.54 (3.08) | 8.86 (4.07) | 9.56 (4.11) | 18.32 (12.44) | 26.87 (23.96) | 14.07 (7.90) |
| fe (%) | 0.7488 (0.1978) | 0.8223 (0.3075) | 0.6315 (0.2196) | 0.9655 (0.1853) | 0.8232 (0.2319) | 0.5374 (0.1231) |
Selected pharmacokinetic parameters are presented as means (standard deviation, SD) unless otherwise stated.
Tmax is presented as median (interquartile range, IQR)
fe (%) was obtained from the data on Days 1 and 9. †n = 4, ‡n = 3.
AUC24h, area under the plasma concentration–time curve from zero to 24 h; Cmax 24h, maximum plasma concentration from zero to 24 h; Ctrough, plasma trough concentration; fe, cumulative fraction of the dose excreted unchanged into urine; t1/2, terminal half‐life; Tmax 24h; time to reach Cmax 24h from zero to 24 h.