TABLE 5.
PK parameters of EC5026 in phase Ia SAD study.
| Parameter (unit) | EC5026 | |||
|---|---|---|---|---|
| 2 mg (N = 4) | 8 mg (N = 6) | 16 mg (N = 6) | 24 mg (N = 6) | |
| C max (ng/mL) | 4.69 (45.8) | 82.7 (11.1) | 220 (16.2) | 301 (14.6) |
| T max (h) | 1.25 (1.25, 1.30) | 1.25 (1.25, 1.30) | 1.25 (1.25, 1.25) | 1.25 (1.25, 1.25) |
| AUC0–t (ng•h/mL) | 258 (145.4) | 3450 (28.4) | 6780 (23.1) | 9030 (22.1) |
| AUC0–inf (ng•h/mL) | NC | 3690 (26.3) | 6960 (22.1) | 9310 (21.1) |
| AUC0‐48 (ng•h/mL) | 119 (59.7) | 1870 (7.9) | 4450 (14.7) | 6130 (13.4) |
| t ½ (h) | 143 (44.3) a | 59.1 (32.2) | 44.8 (31.3) | 41.8 (34.9) |
| CL/F (L/h) | NC | 2.23 (25.2) | 2.35 (22.2) | 2.62 (20.8) |
| Vz/F (L) | NC | 178 (11.8) | 146 (23.6) | 153 (6.3) |
Note: Data are presented as geometric mean (geometric CV) except for t ½, CL/F and Vz/F, which are arithmetic mean (arithmetic CV). For T max, the median (minimum, maximum) values are presented. Subjects were excluded from the PK population when there were fewer than 3 quantifiable plasma samples. All concentrations were below the limit of quantification for the EC5026 0.5 mg dose group. Values for AUC0–inf, CL/F, and Vz/F were excluded from summary statistics when %AUCextrap was >20%.
Abbreviation: NC, not calculated.
a
n = 3; given that plasma concentrations for the 2 mg dose group were near the limit of quantification, the estimates for t½ should be viewed with caution.