Dose group | 0.5 mg/kg QW | 1.0 mg/kg QW | 2.0 mg/kg QW | 4.0 mg/kg QW | 6.0 mg/kg QW | 6.0 mg/kg Q2W | 8.0 mg/kg Q2W | 9.0 mg/kg QW | 12.0 mg/kg QW | 15.0 mg/kg QW |
---|---|---|---|---|---|---|---|---|---|---|
n | n = 3 | n = 3 | n = 3 | n = 3 | n = 17 | n = 3 | n = 3 | n = 3 | n = 3 | n = 3 |
AUCtau (h*µg/mL) | 280.0 (13.7) | 674.1 (43.8) | 3,788.3 (19.9) | 10,552.4 (33.0) | 23,231.0 (22.0) | 19,577.6 (15.3) | 32,545.7 (40.9) | 35,343.9 (1.9) | 55,113.3 (10.0) | 70,988.8 (9.5) |
AUC0-∞ (h*µg/mL) | 280.0 (13.8) | 675.7 (44.1) | 4,479.0 (19.5) | 18,080.2 (43.7) | 51,260.6 (33.7) | 23,931.8 (19.7) | 46,099.0 (60.2) | 80,008.9 (16.1) | 154,936.3 (47.1) | 192,598.2 (23.8) |
Accumulation index | 1.6 (7.2) | 1.3 (17.9) | 1.8 (12.1) | 2.0 (24.0) | 2.1 (13.8) | 1.3 (20.2) | 1.6 (31.0) | 1.9 (18.4) | 2.4 (5.0) | 2.4 (5.8) |
CLss (mL/h/kg) | 1.8 (13.8) | 1.5 (43.8) | 0.5 (19.9) | 0.4 (33.0) | 0.3 (22.0) | 0.3 (15.3) | 0.25 (40.9) | 0.3 (1.9) | 0.2 (10.0) | 0.2 (9.5) |
Cmax (µg/mL) | 7.7 (8.4) | 13.9 (16.6) | 39.5 (17.8) | 100.0 (16.6) | 196.4 (18.0) | 144.8 (13.1) | 204.4 (12.0) | 326.2 (2.3) | 442.0 (3.1) | 652.1 (4.9) |
Cmin (µg/mL) | 0.1 (56.7) | 0.1 (80.0) | 7.4 (26.2) | 35.6 (32.4) | 93.2 (18.1) | 18.0 (35.8) | 35.0 (48.9) | 126.3 (15.9) | 241.1 (18.5) | 311.9 (5.5) |
T1/2 (h) | 12.7 (9.2) | 18.0 (42.1) | 28.2 (3.2) | 134.2 (13.6) | 187.9 (26.6) | 138.0 (12.2) | 188.7 (41.2) | 190.1 (24.5) | 263.4 (51.9) | 244.3 (32.9) |