Table 1.
Pharmacokinetic Parameters for Functional Garetosmab in Healthy Women Administered a Single Intravenous Dose
| Intravenous Garetosmab 0.3 mg/kg (n = 6) | Intravenous Garetosmab 1 mg/kg (n = 6) | Intravenous Garetosmab 3 mg/kg (n = 6) | Intravenous Garetosmab 10 mg/kg (n = 6) | |
|---|---|---|---|---|
| Cmax, mg/L | ||||
| Mean (SD) | 8.10 (0.929) | 29.6 (5.01) | 86.5 (9.74) | 378 (39.7) |
| Median (Min‐Max) | 8.08 (6.96‐9.44) | 32.2 (22.4‐33.6) | 84.9 (73.0‐98.0) | 382 (327‐421) |
| CV% | 11.5 | 16.9 | 11.3 | 10.5 |
| Cmax/dose, kg/L | ||||
| Mean (SD) | 27.0 (3.10) | 29.6 (5.01) | 28.8 (3.25) | 37.8 (3.97) |
| Median (Min‐Max) | 26.9 (23.2‐31.5) | 32.2 (22.4‐33.6) | 28.3 (24.3‐32.7) | 38.2 (32.7‐42.1) |
| CV% | 11.5 | 16.9 | 11.3 | 10.5 |
| tmax, days | ||||
| Median (Min‐Max) | 0.10 (0.04‐1.04) | 0.08 (0.04‐0.21) | 0.08 (0.04‐0.21) | 0.06 (0.04‐0.38) |
| AUCinf, mg · day/L | ||||
| Mean (SD) | 72.2 (15.4) | 379 (50.3) | 1597 (176) | 7520 (809) |
| Median | 75.8 (46.8‐91.8) | 387 (301‐439) | 1581 (1408‐1905) | 7464 (6319‐8417) |
| CV% | 21.3 | 13.3 | 11.0 | 10.8 |
| AUCinf/dose, mg · day/L | ||||
| Mean (SD) | 241 (51.2) | 379 (50.3) | 532 (58.6) | 752 (80.9) |
| Median (Min‐Max) | 253 (156‐306) | 387 (301‐439) | 527 (469‐635) | 746 (632‐842) |
| CV% | 21.3 | 13.3 | 11.0 | 10.8 |
| CL, mL/day/kg | ||||
| Mean (SD) | 4.35 (1.11) | 2.68 (0.382) | 1.90 (0.196) | 1.34 (0.149) |
| Median (Min‐Max) | 3.96 (3.27‐6.41) | 2.59 (2.28‐3.32) | 1.90 (1.57‐2.13) | 1.34 (1.19‐1.58) |
| CV% | 25.5 | 14.3 | 10.3 | 11.1 |
| Vss, mL/kg | ||||
| Mean (SD) | 41.4 (4.66) | 47.8 (4.70) | 45.3 (4.86) | 46.6 (5.40) |
| Median (Min‐Max) | 42.1 (32.9‐46.0) | 47.9 (41.3‐53.7) | 44.3 (39.4‐51.8) | 45.5 (40.8‐54.6) |
| CV% | 11.2 | 9.83 | 10.7 | 11.6 |
AUCinf, area under the concentration‐time curve from time zero extrapolated to infinity; CL, clearance; CL/F, apparent clearance; Cmax, peak concentration; CV, coefficient of variation; SD, standard deviation; tmax, time to peak concentration; Vss, volume of distribution at steady state.