Table 1 Comparison of plasma and brain concentrations, and pharmacokinetic parameters between epertinib and lapatinib after single oral administration at 20 mg/kg in mice implanted intracranially with MDA-MB-361 cells.

From: Distribution analysis of epertinib in brain metastasis of HER2-positive breast cancer by imaging mass spectrometry and prospect for antitumor activity

Time (h)

Epertinib

Lapatinib

Plasma

Brain

Plasma

Brain

(ng/mL)

(ng/g)

(ng/mL)

(ng/g)

0.5

99.8

10.2

984.5

11.8

1

112.9

12.8

762.8

15.7

2

145.0

23.0

413.4

10.0

4

114.8

36.3

461.1

17.0

8

54.7

23.8

99.6

5.8

24

2.1

1.7

5.4

0.4

Cmax (ng/mL or ng/g)

145

36

985

17

Tmax (h)

2.0

4.0

0.5

4.0

AUC0–24 h (ng·h/mL or ng·h/g)

1261

409

4107

144

  1. Concentration data represents the mean of five mice except for 24 h data of lapatinib. (n  =  4 for the 24 h data of lapatinib).
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