Table 2 Pharmacokinetic parameters of four glyco-modified pertuzumabs in ICR mice (n = 5) after a single 1 mg/kg intravenous administration.

From: Glycoengineering of pertuzumab and its impact on the pharmacokinetic/pharmacodynamic properties

 

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

  1. 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.
  2. Data are representative of three independent experiments with similar results.