Table 8.
Summary of pharmacokinetics parameters for apitegromab by treatment: part A, single ascending dose
| Noncompartmental PK parameter | Cohort 1 | Cohort 2 | Cohort 3 | Cohort 4 | Cohort 5 |
|---|---|---|---|---|---|
| 1 mg/kg (n = 6) |
3 mg/kg (n = 6) |
10 mg/kg (n = 6) |
20 mg/kg (n = 6) |
30 mg/kg (n = 6) |
|
| Mean Cmax, µg/mL (CV%) | 25.07 (19.5) | 82.95 (8.7) | 277.50 (7.7) | 555.00 (16.9) | 744.00 (13.2) |
| Dose normalized Cmax, [µg/mL]/[mg/kg] | 25.07 | 27.65 | 27.75 | 27.75 | 24.8 |
| Median t1/2, h (min, max) | 738.8 (617, 1078) | 599.1 (533, 758) | 580.4 (273, 702) | 585.3 (384, 726) | 622.9 (499, 723) |
| Mean CL, mL/h (CV%) | 6.049 (10.7) | 7.688 (17.9) | 7.299 (26.7) | 7.062 (30.0) | 6.628 (14.1) |
| Mean Vz, L (CV%) | 6.804 (20.1) | 6.852 (13.7) | 5.395 (18.8) | 5.688 (10.4) | 5.919 (16.1) |
Cohort 1 (1 mg/kg) anchored start times on the infusion when all other cohorts are based on post end of infusion. One subject in the 10 mg/kg group discontinued the study prior to day 14
CL total body clearance, Cmax maximum serum drug concentration, CV coefficient of variation, max maximum, min minimum, PK pharmacokinetics, t1/2 terminal elimination half-life, Vz volume of distribution