Table 4 Pharmacokinetic parameters and incidence of anti-blisibimod antibodies in patients with systemic lupus erythematosus in the phase 1b study
0.3 mg/kg SC (n = 12) | 1.0 mg/kg SC (n = 13) | 3.0 mg/kg SC (n = 12) | 6.0 mg/kg IV (n = 12) | |||||
|---|---|---|---|---|---|---|---|---|
Parameter, mean (SD) | Day 1 | Day 22 | Day 1 | Day 22 | Day 1 | Day 22 | Day 1 | Day 22 |
tmax (hr) | 47 (24–97) | 48 (24–96) | 49 (25–170) | 26 (8–73) | 47 (20–170) | 49 (0.58–170) | N/A | N/A |
Cmax or C0 (μg/hr) | 1.18 (0.498) | 2.13 (0.466) | 3.84 (1.02) | 8.21 (1.88) | 13.2 (4.49) | 34.6 (8.84) | 243 (128) | 315 (163) |
AUC0-t (hr*μg/mL) | 149 (54.7) | 657 (203) | 484 (100) | 2780 (862) | 1670 (479) | 9450 (2850) | 8100 (3740) | 35600 (15600) |
t1/2,z (day) | NC | 7.9 (1.3) | NC | 9.8 (1.6) | NC | 10 (2.4) | NC | 12 (2.4) |
CL/F or CL (mL/hr) | NC | 79.7 (38.2) | NC | 78.2 (30.4) | NC | 59.9 (16.3) | NC | 34.0 (18.6) |
AR | 2.21 (0.74) | 2.21 (0.52) | 2.76 (0.89) | 2.31 (0.34) | ||||
Antibodies, n (%) | ||||||||
Pre-dose only | 0 (0) | 1 (8) | 1 (8) | 1 (8) | ||||
Post-dose only | 7 (58) | 1 (8) | 1 (8) | 6 (50) | ||||
Pre- and post-dose | 0 (0) | 1 (8) | 1 (8) | 0 (0) | ||||
Neutralizing | 2 (17) | 1 (8) | 0 (0) | 0 (0) | ||||