Table 3.
Main PK parameters for each ETC‐206 dose level and administration conditions
| Parameters | ETC‐206 10 mg FASTED (N = 16) [SD] | ETC‐206 20 mg FASTED (N = 14) [SD] | ETC‐206 10 mg (FEDa) (N = 9) [SD] |
|---|---|---|---|
| Mean Cmax (ng/mL) | 927 [154] | 1,950 [315] | 733 [78.9] |
| Mean Tmax (hour) | 1.11 [0.37] | 1.00 [0.32] | 4.62 [1.81] |
| Mean t1/2 (hour) | 22.95 [5.63] | 25.76 [4.12] | 27.57 [5.68] |
| Mean AUC0−t (hour*ng/mL) | 21,909 [5,437] | 57,799 [12,335] | 28,746 [6,198] |
| Mean AUC0−inf (hour*ng/mL) | 24,357 [6,434] | 60,279 [12,451] | 30,047 [6,360] |
| CL/F (L/hour) | 0.44 [0.13] | 0.35 [0.07] | 0.35 [0.08] |
| Vd/F (L) | 13.86 [2.16] | 12.52 [1.52] | 13.35 [1.82] |
The panel illustrates that Cmax was reached on average 1 hour postdose in fasted condition and in about 5 hours in the fed condition, with a mean t½ ~23–28 hour. AUC0−t increased in direct proportion with the dose from 10 to 20 mg single doses in fasted condition. The CL/F was estimated at about 0.4 L/hour for the two dose levels, and the Vd/F was limited to about 13 L. Food administration delayed Tmax (3.0 hour), reduced Cmax (20%), and increased AUC0−inf (25%). No formal conclusion on food effect could be drawn due to the small sample size.
AUC0−inf, area under the concentration‐time curve from zero to infinity; AUC0−t, area under concentration‐time profiles; CL/F, apparent clearance; Cmax, peak plasma concentration; PK, pharmacokinetic; t1/2, terminal half‐life; Tmax, time of maximum plasma concentration; Vd/F, apparent volume of distribution.
a N = 9 (2 healthy volunteers (HVs) received placebo). Only 7 HVs received 10 mg in both FASTED and FED conditions.