Table 3 Pharmacokinetic parameters and incidence of anti-blisibimod antibodies in patients with systemic lupus erythematosus in the phase 1a study
mg/kg SC | mg/kg IV | ||||||
|---|---|---|---|---|---|---|---|
0.1 (n = 6) | 0.3 (n = 6) | 1.0 (n = 9) | 3.0 (n = 6) | 1.0 (n = 6) | 3.0 (n = 1) | 6.0 (n = 6) | |
Parameter, mean (SD) | |||||||
tmax (hr) | 48 (2.2–72) | 48 (47–70) | 48 (24–72) | 47 (23–73) | 0.61 ( 0.083–1.1) | 0.083 | 0.42 (0.17–0.67) |
Cmax or C0 (μg/hr) | 0.273 (0.0817) | 0.916 (0.397) | 4.14 (1.54) | 9.32 (2.57) | 21.2 (4.11) | 80.9 | 190 |
AUC0-t (hr*μg/mL) | 50.0 (15.9) | 252 (123) | 1140 (384) | 2770 (459) | 1460 (543) | 6610 | 9440 (1980) |
t1/2,z (day) | 4.0 (1.1) | 6.5 (2.9) | 9.8 (2.5) | 8.4 (2.1) | 7.9 (2.8) | 8.4 | 8.7 (2.0) |
CL/F or CL (mL/hr) | 179 (62.2) | 112 (49.4) | 72.0 (26.9) | 77.8 (24.7) | 51.9 (6.96) | 48.6 | 47.5 (7.54) |
Antibodies, n (%) | |||||||
Pre-dose only | 0 (0) | 3 (50) | 0 (0) | 0 (0) | 1 (17) | 0 (0) | 0 (0) |
Post-dose only | 4 (67) | 1 (17) | 3 (33) | 1 (17) | 0 (0) | 1 (17) | 0 (0) |
Pre- and post-dose | 0 (0) | 0 (0) | 0 (0) | 2 (33) | 0 (0) | 2 (33) | 1 (100) |