Table 2. Pharmacokinetic parameters of four glyco-modified pertuzumabs in ICR mice (n = 5) after a single 1 mg/kg intravenous administration.
| Species | Route | Doses (mg/kg) | AUC (hr*μg/mL) | CL (mL/day/kg) | V1 (mL/kg) | Vss (mL/kg) | Alpha_HL (day) | Beta_HL (day) | |
|---|---|---|---|---|---|---|---|---|---|
| PertuzumabFuc+SA+ | ICR | IV bolus | 1 | 1327 ± 314.6 | 18.1 ± 4.3 | 57.3 ± 5.7 | 372.1 ± 50.4 | 0.08 ± 0.016 | 14.7 ± 4.8 |
| PertuzumabFuc−SA+ | ICR | IV bolus | 1 | 1305.3 ± 321 | 18.4 ± 4.5 | 69.8 ± 7.1 | 406.1 ± 54.1 | 0.09 ± 0.019 | 15.7 ± 5.2 |
| PertuzumabFuc+SA− | ICR | IV bolus | 1 | 1202.2 ± 355.6 | 19.9 ± 5.9 | 55.1 ± 9.8 | 367.4 ± 62.3 | 0.05 ± 0.016 | 13.1 ± 5.2 |
| PertuzumabFuc−SA− | ICR | IV bolus | 1 | 1155.1 ± 251.4 | 20.7 ± 4.5 | 20.8 ± 9.4 | 313.5 ± 37.4 | 0.01 ± 0.0032 | 10.6 ± 2.9 |
| ASF + PertuzumabFuc+SA− | ICR | IV bolus | 100, 1 | 1569.1 ± 335.5 | 15.3 ± 3.3 | 44.7 ± 3.7 | 338.8 ± 38.6 | 0.07 ± 0.01 | 15.8 ± 4.5 |
| ASF + PertuzumabFuc−SA− | ICR | IV bolus | 100, 1 | 1624.5 ± 267.8 | 14.7 ± 2.4 | 54.1 ± 5.1 | 325.9 ± 27.1 | 0.05 ± 0.008 | 15.5 ± 3.3 |
Fuc: fucose, SA: Sialic acid, ASF: Asialofetuin, AUC: Area under the concentration–time curve from time zero extrapolated to infinity, CL: clearance, HL: half-life, V1: volume of distribution of the central compartment, Vss: steady state volume of distribution, IV: Intravenous. Data are presented as mean values ± SD.
Data are representative of three independent experiments with similar results.