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Table 3 Primary pharmacokinetic parameters for LJM716 3–40 mg/kg QW (Cycle 1 Day 1)

From: A phase I open-label dose-escalation study of the anti-HER3 monoclonal antibody LJM716 in patients with advanced squamous cell carcinoma of the esophagus or head and neck and HER2-overexpressing breast or gastric cancer

 

3 mg/kg QW

n = 1

10 mg/kg QW

n = 5

20 mg/kg QW

n = 6

40 mg/kg QW

n = 6

40 mg/kg QW

EX, n = 30

20 mg/kg Q2W

n = 6

AUClast, h*μg/mLa

6158 (−)

21,302 (3731)

32,791 (9635)

74,637 (7182)

73,360 (18,819)

52,659 (23,302)

Cmax, μg/mL

65.2 (−)

204 (23.6)

369 (131)

839 (143)

706 (129)

408 (137)

Tmax, h

2.18 (2.18–2.18)

4.00 (2.13–4.53)

3.88 (2.08–5.33)

4.34 (2.42–8.42)

3.79 (2.05–7.5)

3.25 (2.08–4.03)

Tlast, h

168 (168–168)

170 (166–171)

167 (146–169)

167 (166–191)

166 (7.22–171)

334 (261–336)

Clast, μg/mL

21.4 (−)

80.3 (18.4)

115.0 (28.6)

296.0 (66.0)

236.0 (79.7)

82.0 (46.6)

  1. Mean values (standard deviation) provided, except for Tmax and Tlast which are median (range)
  2. AUC, area under curve, EX expansion phase, Q2W once every two weeks, QW once weekly