TABLE 3.
Pharmacokinetic parameters of LC51-0255 after daily oral administration of 0.25, 0.5, 1, 1.5, or 2 mg of LC51-0255 for 21 days.
| PK parameter | 0.25 mg (N = 7) | 0.5 mg (N = 8) | 1 mg (N = 7) | 1.5 mg (N = 6) | 2 mg (N = 6) |
|---|---|---|---|---|---|
| Tmax,ss (h) | 4.00 (1.00–24.0) | 4.51 (4.00–10.0) | 4.00 (2.00–8.00) | 4.00 (3.05–12.0) | 4.00 (4.00–10.0) |
| Cmax,ss (μg/L) | 11.1 ± 3.28 | 23.6 ± 5.29 | 57.3 ± 3.82 | 73.5 ± 22.1 | 103 ± 12.3 |
| AUCτ,ss (h* μg/L) | 229 ± 67.2 | 478 ± 115 | 1,120 ± 125 | 1,460 ± 412 | 2060 ± 260 |
| t1/2 (h) | 95 ± 43 | 81 ± 22 | 78 ± 10 | 76 ± 12 | 79 ± 11 |
| Rac | 6.64 ± 2.13 | 6.06 ± 1.77 | 5.88 ± 0.617 | 5.17 ± 0.698 | 5.53 ± 0.84 |
| PTF (%) | 20.5 ± 17.1 | 29.4 ± 5.94 | 30.3 ± 18.3 | 33.8 ± 6.61 | 28.5 ± 5.04 |
| CLss/F (L/h) | 1.18 ± 0.334 | 1.1 ± 0.254 | 0.906 ± 0.104 | 1.09 ± 0.265 | 0.985 ± 0.13 |
| Vz/F (L) | 131 ± 30.6 | 126 ± 39.5 | 108 ± 15.3 | 112 ± 26.2 | 179 ± 123 |
Notes: All data are presented as mean ± standard deviation, except for Tmax,ss, which is presented as median (minimum–maximum). The half-life (t1/2) was calculated by computing the best fit line using Phoenix WinNonlin®. Abbreviations: Tmax,ss, the time to reach maximum plasma concentration at steady state; Cmax,ss, maximum steady-state plasma concentration of LC51-0255; AUCτ, ss, area under the plasma concentration–time curve during a dosing interval at steady state; t1/2, terminal half-life; Rac, accumulation ratio calculated from AUCτ,ss and AUCτ after single dosing; PTF, peak trough fluctuation over one dosing interval at steady state; CLss/F, apparent clearance at steady state; and Vz/F, apparent volume of distribution during the terminal phase.