Table 1 Noncompartmental pharmacokinetic parameters for hFcRn mouse and monkey studies.

From: An Fc variant with two mutations confers prolonged serum half-life and enhanced effector functions on IgG antibodies

Speciesa

Parameter

t1/2 (day)

Cmax (μg mL−1)

AUCinf (μg mL−1 day)

AUC%Extrap

CL (mL day−1)

hFcRn transgenic mouse1

Trastuzumab

7.03 ± 1.16

71.14 ± 3.95

247.08 ± 18.60

0.6 ± 0.25

0.41 ± 0.03

Trastuzumab-PFc29

14.07 ± 2.70

79.30 ± 9.48

528.82 ± 101.78

7.7 ± 3.9

0.21 ± 0.04

Trastuzumab-PFc41

10.90 ± 2.54

67.91 ± 7.60

480.90 ± 60.65

7.0 ± 0.5

0.22 ± 0.02

hFcRn transgenic mouse2

Aflibercept

0.41 ± 0.02

30.55 ± 8.50

15.63 ± 4.06

0.41 ± 0.11

6.40 ± 0.13

Aflibercept-PFc29

2.10 ± 0.63

45.26 ± 4.42

33.66 ± 4.56

0.40 ± 0.35

2.97 ± 0.09

Aflibercept-PFc41

1.01 ± 0.03

39.95 ± 5.32

30.33 ± 2.33

0.78 ± 0.14

3.30 ± 1.18

Cyno

Trastuzumab

7.17 ± 0.14

120.38 ± 1.29

881.49 ± 35.68

2.879 ± 0.38

13.64 ± 0.55

Trastuzumab-YTE

8.84 ± 2.81

130.56 ± 17.43

1001.44 ± 154.20

6.17 ± 4.79

12.27 ± 1.89

Trastuzumab-LS

8.88 ± 1.17

177.20 ± 10.32

1263.26 ± 42.53

6.05 ± 2.63

9.51 ± 0.32

Trastuzumab-PFc29

14.34 ± 2.75

228.52 ± 39.46

1966.32 ± 286.39

16.89 ± 5.60

6.24 ± 0.91

  1. t1/2 terminal half-life (β-phase), Cmax maximal concentration, AUCinf area under the curve from administration to infinity, AUC%Extrap percentage of the extrapolated area under the curve to the total area under the curve, CL clearance.
  2. ahFcRn transgenic mouse and Cyno refer to Tg276 mouse (B6.Cg-Fcgrttm1Dcr Tg(CAG-FCGRT)276Dcr/DcrJ homozygous) and in cynomolgus monkey, respectively. Dose levels and routes: single i.v. bolus at 5 mg/kg (n = 5) for hFcRn transgenic mouse1; single i.v. bolus at 4 mg/kg (n = 5) for hFcRn transgenic mouse2; single i.v. infusion at 6 mg/kg (n = 2) for Cyno.
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