TABLE 2.
Pharmacodynamic parameters of LC51-0255 after daily oral administration of 0.25, 0.5, 1, 1.5, 2 mg of LC51-0255 or placebo for 21 days.
| PD parameter | Period | 0.25 mg (N = 7) | 0.5 mg (N = 8) | 1 mg (N = 7) | 1.5 mg (N = 6) | 2 mg (N = 6) | Placebo (N = 10) |
|---|---|---|---|---|---|---|---|
| TEmax (h) | Baseline | 1.00 (0.00–23.92) | 1.00 (0.00–8.00) | 4.00 (0.00–8.00) | 2.00 (0.00–2.00) | 2.00 (0.00–23.58) | 6.00 (0.00–23.83) |
| Day 1 | 6.01 (2.00–8.02) | 6.00 (6.00–23.85) | 6.00 (6.00–12.00) | 6.00 (6.00–6.00) | 6.00 (6.00–6.05) | 6.00 (2.00–12.02) | |
| Day 21 | 6.00 (2.00–12.00) | 6.00 (0.00–8.00) | 6.00 (0.00–8.00) | 6.00 (2.00–24.02) | 6.00 (0.00–6.00) | 6.00 (0.00–8.00) | |
| Emax (/μL) | Baseline | 1,656 ± 324 | 1,655 ± 287 | 1,506 ± 262 | 1,447 ± 381 | 1,619 ± 415 | 1,412 ± 195 |
| Day 1 | 1,556 ± 258 | 1,305 ± 353 | 1,037 ± 290 | 791 ± 135 | 764 ± 226 | 1,440 ± 275 | |
| Day 21 | 744 ± 283 | 491 ± 225 | 420 ± 142 | 253 ± 41 | 247 ± 74 | 1,382 ± 241 | |
| AUECτ (h/μL) | Baseline | 48,419 ± 10,211 | 49,678 ± 12,859 | 49,147 ± 8,844 | 43,062 ± 12,080 | 47,060 ± 11,272 | 41,718 ± 4,632 |
| Day 1 | 45,941 ± 8,852 | 41,566 ± 10,409 | 33,736 ± 6,260 | 26,531 ± 5,607 | 28,450 ± 9,624 | 39,356 ± 7,704 | |
| Day 21 | 24,612 ± 6,663 | 17,304 ± 5,609 | 14,311 ± 4,190 | 9,622 ± 2,388 | 10,815 ± 2,923 | 42,563 ± 5,859 | |
| ΔEmax (/μL) | Day 1 | -461 ± 260 | -765 ± 212 | -1,011 ± 194 | -1,003 ± 432 | -1,197 ± 322 | -298 ± 179 |
| Day 21 | -1,274 ± 476 | -1,579 ± 361 | -1,628 ± 446 | -1,541 ± 528 | -1714 ± 424 | -357 ± 176 | |
| ΔAUECτ (h/μL) | Day 1 | -2,133 ± 3,859 | -7,750 ± 3,343 | -15067 ± 3,232 | -16197 ± 8,252 | -18351 ± 3,582 | -7 ± 2,271 |
| Day 21 | -23846 ± 10,577 | -32381 ± 8,284 | -34836 ± 11,766 | -33479 ± 13,130 | -36250 ± 9,042 | 843 ± 5,068 | |
| CFBmax (%) | -61.84 ± 14.70 | -76.70 ± 5.60 | -82.12 ± 3.68 | -85.30 ± 6.41 | -87.98 ± 3.50 | -31.57 ± 11.17 |
Notes: All data are presented as mean ± standard deviation, except for TEmax, which is presented as median (minimum–maximum). Abbreviations: PD, pharmacodynamic; TEmax, time to maximum effect; Emax, maximum effect; AUECτ, area under the ALC–time curve during a dosing interval; ΔEmax, change of Emax from the baseline; ΔAUECτ change of AUECτ from the baseline; and CFBmax, maximum change of ALC from the baseline.