Table 2.
RN317 | Bococizumab | |||||||||
---|---|---|---|---|---|---|---|---|---|---|
s.c. | s.c. | s.c. | s.c. | i.v. | i.v. | i.v. | s.c. | s.c. | i.v. | |
0.3 mg/kg | 1 mg/kg | 3 mg/kg | 6 mg/kg | 1 mg/kg | 3 mg/kg | 6 mg/kg | 1 mg/kg | 3 mg/kg | 1 mg/kg | |
(n = 6) | (n = 12) | (n = 16) | (n = 6) | (n = 11) | (n = 6) | (n = 6) | (n = 12) | (n = 16) | (n = 6) | |
n * | 6 | 12 | 16 | 6 | 11 | 6 | 6 | 12 | 16 | 6 |
Cmax, μg/ml | 1.172 | 3.099 | 11.09 | 23.02 | 35.7 | 86.01 | 157.8 | 1.824 | 11.85 | 35.89 |
(20) | (33) | (35) | (28) | (195) | (12) | (9) | (65) | (66) | (12) | |
Tmax, h | 253 | 253 | 120 | 72 | 2.0 | 2.51 | 2.00 | 156 | 72.0 | 1.50 |
(143–339) | (72–504) | (24–672) | (72–337) | (0.967–4.00) | (1.00–4.00) | (1.00–3.00) | (48.0–171) | (4.00–168) | (1.00–4.00) | |
N* | 2 | 8 | 16 | 6 | 11 | 6 | 6 | 1 | 10 | 6 |
AUCinf, μg.h/ml | NR | 3,103 | 7,995 | 18,100 | 6,705 | 19,420 | 29,220 | NR | 3,721 | 3,451 |
(30) | (32) | (30) | (22) | (13) | (6) | (47) | (13) | |||
t1/2, days | NR | 20.88 ± 4.33 | 19.40 ± 5.40 | 18.58 ± 4.1 | 19.49 ± 6.43 | 17.52 ± 2.9 | 14.63 ± 4.68 | NR | 8.378 ± 2.656 | 3.400 ± 0.692 |
Data shown are geometric mean (coefficient of variation; %CV) for all parameters except for Tmax where median (min, max) is shown, and t1/2 where arithmetic mean ± SD is shown.
*n is the number of subjects in the treatment group and contributing to the mean; N is the number of subjects with a well‐characterized terminal phase. AUCinf, area under the plasma concentration–time curve from time zero to infinity; Cmax, maximum concentration; NR, not reported where <3 subjects had reportable parameter values; SD, standard deviation; t1/2, terminal half‐life; Tmax, time to reach maximum concentration.