Table 2.
Plasma pharmacokinetic parameters of single-dose peficitinib in Japanese and Caucasian subjects
| Parameter | Japanese | Caucasian | ||||
|---|---|---|---|---|---|---|
| Peficitinib dose | ||||||
| 20 mg (n = 6) | 60 mg (n = 6) | 200 mg (n = 6) | 20 mg (n = 6) | 60 mg (n = 6) | 200 mg (n = 6) | |
| tmax (h) | ||||||
| Median | 1.0 | 1.3 | 2.0 | 1.0 | 1.0 | 1.8 |
| Range | 1.0–3.0 | 1.0–1.5 | 1.0–2.0 | 1.0–1.5 | 1.0–1.5 | 1.5–3.0 |
| Cmax (ng/mL) | ||||||
| Mean (SD) | 76.9 (24.2) | 241.1 (74.7) | 648.7 (55.5) | 48.9 (16.9) | 130.9 (19.4) | 381.2 (114.4) |
| %CV | 31.5 | 31.0 | 8.6 | 34.6 | 14.8 | 30.0 |
| AUCinf (ng∙h/mL) | ||||||
| Mean (SD) | 259.5 (42.9) | 782.8 (158.6) | 2524.9 (234.5) | 196.3 (54.6) | 528.6 (118.0) | 1520.3 (186.5) |
| %CV | 16.5 | 20.3 | 9.3 | 27.8 | 22.3 | 12.3 |
| AUClast (ng∙h/mL) | ||||||
| Mean (SD) | 256.2 (44.1) | 775.6 (155.9) | 2512.2 (232.3) | 191.1 (55.3) | 523.6 (117.4) | 1507.2 (192.4) |
| %CV | 17.2 | 20.1 | 9.2 | 28.9 | 22.4 | 12.8 |
| t½ (h) | ||||||
| Mean (SD) | 3.7 (0.7) | 4.0 (1.0) | 7.5 (4.9) | 7.3 (10.0) | 10.0 (5.0) | 6.9 (3.2) |
| %CV | 18.8 | 24.4 | 65.0 | 137.1 | 49.8 | 46.3 |
| CL/F (L/h) | ||||||
| Mean (SD) | 78.9 (13.5) | 79.8 (19.2) | 79.8 (8.2) | 108.5 (30.0) | 117.8 (23.6) | 133.1 (15.0) |
| %CV | 17.1 | 24.1 | 10.3 | 27.6 | 20.0 | 11.2 |
| Aelast (mg) | ||||||
| Mean (SD) | 3.4 (0.8) | 8.9 (1.7) | 25.1 (5.4) | 2.9 (0.7) | 6.4 (2.2) | 19.8 (2.4) |
| %CV | 24.6 | 19.0 | 21.6 | 25.3 | 33.9 | 11.8 |
| Aelast% (%dose) | ||||||
| Mean (SD) | 16.8 (4.1) | 14.8 (2.8) | 12.5 (2.7) | 14.2 (3.6) | 10.6 (3.6) | 9.9 (1.2) |
| %CV | 24.6 | 19.0 | 21.6 | 25.3 | 33.9 | 11.8 |
Aelast cumulative amount of unchanged drug excreted into the urine from the time of dosing to the last measurable concentration, Aelast% fraction of the drug dose excreted unchanged into the urine from the time of dosing to the last measurable concentration, AUCinf area under the plasma concentration–time curve from the time of dosing extrapolated to infinity, AUClast area under the plasma concentration–time curve from the time of dosing to the last measurable concentration, Cmax maximum plasma concentration, CL/F apparent total clearance of the drug from plasma after oral administration, CV coefficient of variation, SD standard deviation, t½, terminal elimination half-life, tmax time to maximum plasma concentration