Table 3.
Summary of ruxolitinib cream pharmacokinetic parameters
| Patient age, years | Affected BSA at baseline, % | Overall | ||||
|---|---|---|---|---|---|---|
| 12–15 | 16–17 | ≥ 18 | 25% to < 40% | ≥ 40% | ||
| Baseline | n = 14 | n = 7 | n = 20 | n = 28 | n = 13 | n = 41 |
| Affected BSA, % | 30.1 (4.6) | 35.1 (10.1) | 44.7 (20.4) | 29.2 (2.6) | 57.2 (17.1) | 38.1 (16.3) |
| Lesion area treated, cm2 | 5140 (925) | 6130 (1470) | 7870 (3380) | 5180 (762) | 9780 (2910) | 6640 (2760) |
| Day 1 | n = 14 | n = 7 | n = 19 | n = 27 | n = 13 | n = 40 |
| Cmax, nMa | 114 (305) | 102 (118) | 449 (883) | 51.4 (69.7) | 727 (1010) | 271 (650) |
| tmax, h | 12.0 | 4.0 | 4.0 | 12.0 | 4.0 | 4.0 |
| AUC(0–12h), h*nMb | 856 (2450) | 690 (758) | 3220 (6190) | 359 (510) | 5250 (7140) | 1950 (4610) |
| C12h, nM | 60.7 (113) | 47.4 (43.4) | 188 (332) | 39.0 (51.3) | 284 (381) | 119 (245) |
| Days 15 and 28 combined | n = 14 | n = 7 | n = 19 | n = 28 | n = 12 | n = 40 |
| Css, nM | 43.8 (67.7) | 20.2 (23.0) | 179 (438) | 30.9 (32.8) | 274 (539) | 104 (309) |
| Average application amount of API, mg | 143 (43.8) | 89.2 (64.6) | 182 (109) | 133 (51.2) | 197 (136) | 152 (89.1) |
| Bioavailability, % | 1.84 (2.31) | 1.91 (1.65) | 3.30 (4.64) | 1.49 (1.31) | 5.00 (5.60) | 2.54 (3.56) |
| Day 28 | n = 14 | n = 7 | n = 17 | n = 27 | n = 11 | n = 38 |
| Cmax, nM | 66.2 (93.3) | 24.5 (12.9) | 242 (548) | 49.2 (51.2) | 353 (669) | 137 (377) |
| Cmax/Cmin | 3.20 (2.39) | 2.90 (1.59) | 2.32 (1.66) | 2.80 (1.89) | 2.55 (2.05) | 2.72 (1.91) |
| tmax, h | 12.0 | 1.0 | 4.0 | 4.0 | 1.0 | 4.0 |
| AUC(0–12h), h*nM | 555 (863) | 196 (149) | 1970 (4230) | 427 (499) | 2830 (5170) | 1120 (2930) |
| t1/2, h |
266 (442) (n = 3) |
18.3 (7.0) (n = 2) |
51.3 (49.0) (n = 4) |
159 (305) (n = 6) |
28.0 (26.0) (n = 3) |
116 (251) (n = 9) |
| C12h, nM | 52.1 (75.0) | 16.9 (15.2) | 131 (232) | 41.3 (48.8) | 178 (284) | 80.8 (166) |
API active pharmaceutical ingredient, AUC(0–12h) area under the curve from 0 to 12 h, BSA body surface area, C12h concentration at 12 h post-application, Cmax maximum concentration, Cmin minimum concentration, Css steady-state plasma concentration, PK pharmacokinetic, SD standard deviation, t1/2 half-life, tmax time to Cmax
Data are mean (SD), except tmax, which shows the median
aMean (SD) Cmax for patients aged 12–17 years was 110 (255) nM
bMean (SD) AUC(0–12h) for patients aged 12–17 years was 801 (2020) h*nM