Table 4.
Summary of pharmacokinetic parameters for LC350189 in the single ascending dose study
| Cmax (ng/mL) | Tmax (h) | AUClast (h·ng/mL) | AUCinf (h·ng/mL) | CL/F (L/h) | t1/2 (h) | Ae0–72h (mg) | CLR (L/h) | fe | |
|---|---|---|---|---|---|---|---|---|---|
| 10 mg (n=6) | 313.3 (118.4) | 2.8 (2.5–4.0) | 1,680.5 (620.5) | 1,770.0 (620.6) | 6.4 (2.8) | 5.1 (1.6) | 2.49 (0.79) | 1.5 (0.5) | 0.249 (0.079) |
| 25 mg (n=6) | 978.0 (126.2) | 2.3 (2.0–4.0) | 5,008.3 (664.9) | 5,186.4 (678.9) | 4.9 (0.6) | 8.1 (3.8) | 9.23 (3.78) | 1.8 (0.5) | 0.369 (0.151) |
| 50 mg (n=8) | 1,441.3 (287.3) | 3.0 (2.5–4.0) | 6,977.4 (1,674.4) | 7,121.3 (1,612.9) | 7.3 (1.5) | 7.1 (2.9) | 9.84 (5.02) | 1.4 (0.7) | 0.197 (0.100) |
| 100 mg (n=8) | 3,525.0 (321.8) | 3.5 (2.0–5.0) | 19,435.8 (4,432.1) | 19,574.5 (4,413.5) | 5.3 (1.2) | 6.6 (1.0) | 20.18 (9.79) | 1.0 (0.5) | 0.202 (0.098) |
| 200 mg (n=8) (fasting) | 8,767.5 (2,611.8) | 2.7 (1.0–6.0) | 43,864.5 (13,322.2) | 44,304.3 (13,234.5) | 4.8 (1.3) | 13.3 (18.1) | 54.83 (13.30) | 1.3 (0.2) | 0.274 (0.066) |
| 200 mg (n=8) (fed) | 5,400.0 (1,352.6) | 5.0 (3.0–6.0) | 43,702.1 (18,895.1) | 44,340.0 (18,642.7) | 5.0 (1.4) | 15.0 (19.7) | 51.02 (18.74) | 1.2 (0.3) | 0.255 (0.094) |
| 400 mg (n=8) | 14,731.0 (3,676.6) | 3.0 (1.5–4.0) | 91,495.5 (18,918.8) | 92,006.2 (18,705.8) | 4.5 (1.0) | 13.1 (9.3) | 90.55 (29.62) | 1.1 (0.5) | 0.226 (0.074) |
| 600 mg (n=8) | 18,207.9 (1,881.5) | 2.5 (1.5–3.5) | 98,839.8 (11,379.3) | 99,784.2 (12,253.5) | 6.1 (0.7) | 11.9 (8.0) | 168.03 (130.81) | 1.8 (1.6) | 0.280 (0.218) |
Note: All values are presented as mean ± SD, except for Tmax for which the median (range) is presented.
Abbreviations: Cmax, maximum plasma drug concentration; Tmax, time to reach peak plasma drug concentrations; AUClast, area under the plasma concentration–time curve (AUC) from 0 h to 72 h; h, hours; AUCinf, AUC from time zero to infinity; CL/F, apparent total clearance of the drug from plasma after oral administration; t1/2, elimination half-life; Ae0–72h, total amount excreted unchanged in the urine from 0 h to 72 h; CLR, renal clearance, calculated as CLR = Ae/AUC; fe, fraction of unchanged drug excreted in urine calculated as Ae/Dose; SD, standard deviation.