Table 4 Summary of pharmacokinetic parameters administered orally once daily for 6 months at 4 dose levels
From: Safety of ilunocitinib tablets (Zenrelia™) after once daily oral administration in dogs
Gp 2 (1X: 0.8 mg/kg) | Gp 3 (2X: 1.6 mg/kg) | Gp 4 (3X: 2.4 mg/kg) | Gp 5 (5X: 4.0 mg/kg) | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Day 1 | Day 182 | Day 1 | Day 182 | Day 1 | Day 182 | Day 1 | Day 182 | |||||||||
Tmax (h)* | 2 | (1–2) | 2 | (1–2) | 1.50 | (1–2) | 2 | (1–2) | 2 | (1–2) | 2 | (1–5) | 2 | (2–2) | 2 | (1–2) |
Cmax (ng/mL) | 274 | (24.2) | 310 | (20.6) | 433 | (21.0) | 540 | (13.4) | 659 | (15.1) | 972 | (33.2) | 919 | (15.6) | 1080 | (29.4) |
Cmax/D (ng/mL)** | 327 | (23.0) | 378 | (20.6) | 269 | (21.7) | 332 | (13.6) | 272 | (15.5) | 400 | (33.7) | 227 | (16.3) | 270 | (29.1) |
AUClast (h*ng/mL) | 1150 | (25.3) | 1360 | (25.1) | 1710 | (24.3) | 2440 | (21.3) | 3310 | (28.5) | 5190 | (52.4) | 4380 | (14.7) | 5420 | (22.6) |
AUClast/D (h*ng/mL)** | 1370 | (26.4) | 1660 | (25.8) | 1060 | (24.9) | 1500 | (20.5) | 1360 | (29.0) | 2130 | (52.9) | 1080 | (14.8) | 1350 | (22.3) |
AUCinf (h*ng/mL) | 1160 | (25.8) | 1370 | (25.5) | 1720 | (24.5) | 2450 | (21.0) | 3360 | (29.1) | 5140 | (59.0) | 4410 | (14.8) | 5470 | (23.1) |
AUCinf/D (h*ng/mL)** | 1380 | (26.9) | 1670 | (26.2) | 1070 | (25.0) | 1510 | (20.2) | 1380 | (29.6) | 2110 | (59.6) | 1090 | (14.8) | 1360 | (22.8) |
AUCextra (%) | 0.595 | (77.4) | 0.557 | (70.9) | 0.398 | (54.3) | 0.472 | (118) | 0.918 | (173) | 0.891 | (215) | 0.498 | (54.6) | 0.557 | (133) |
T1/2 (h) | 3.36 | (14.6) | 3.29 | (11.9) | 3.08 | (8.95) | 2.68 | (28.5) | 3.68 | (24.8) | 3.62 | (27.4) | 3.08 | (10.6) | 3.20 | (20.7) |