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. 2012 Oct;40(10):1883–1893. doi: 10.1124/dmd.111.043901

TABLE 1.

Pharmacokinetic parameters of genistein, G-7-G, G-4′-S, and G-7-S in WT and BCRP(−/−) mice after oral administration

Pharmacokinetic parameters in BCRP(−/−) mice were compared to WT mice at the same dose. Data are presented as means ± S.D.; n = 5.

Strain Dose Cmax ke t1/2 AUC0–t
mg/kg μM h1 h h · μM
Genistein FVB 2 0.10 ± 0.05 N.A. N.A. 0.36 ± 0.17
BCRP(−/−) 2 0.23 ± 0.17 0.27 ± 0.20 3.8 ± 2.7 0.71 ± 0.24*
FVB 20 0.65 ± 0.22 N.A. N.A. 6.05 ± 0.54
BCRP(−/−) 20 3.35 ± 0.65** N.A. N.A. 16.41 ± 4.23*
G-7-G WT 2 N.A. N.A. 0.15a
BCRP(−/−) 2 0.30 ± 0.16 N.A. N.A. 1.87 ± 0.68*
WT 20 1.07 ± 1.03 N.A. N.A. 3.49 ± 2.58
BCRP(−/−) 20 9.63 ± 5.65* 0.16 ± 0.10 5.5 ± 3.3 56.71 ± 43.87*
G-4′-G WT 2 N.A. N.A. 0.12a
BCRP(−/−) 2 0.11 ± 0.12 0.28 ± 0.23 3.7 ± 3.0 0.26 ± 0.17
WT 20 0.52 ± 0.37 0.25 ± 0.25 6.5 ± 6.5 1.56 ± 0.79
BCRP(−/−) 20 2.14 ± 1.44* 0.15 ± 0.10 6.2 ± 3.3 15.19 ± 11.16*
G-4′-S WT 2 0.04 ± 0.03 0.17 ± 0.01 4.0 ± 0.3 0.13 ± 0.04
BCRP(−/−) 2 0.14 ± 0.11 N.A. N.A. 1.37 ± 1.17*
WT 20 0.25 ± 0.22 0.32 ± 0.19 2.7 ± 1.3 1.03 ± 0.64
BCRP(−/−) 20 6.18 ± 4.14* 0.30 ± 0.10 2.4 ± 0.7 26.78 ± 13.79*
G-7-S WT 2 0.08 ± 0.02 0.27 ± 0.07 2.7 ± 0.6 0.32 ± 0.05
BCRP(−/−) 2 0.17 ± 0.05 0.21 ± 0.03 3.4 ± 0.5 1.13 ± 0.81*
WT 20 0.65 ± 0.56 0.21 ± 0.18 5.6 ± 4.5 2.49 ± 1.51
BCRP(−/−) 20 4.39 ± 2.55* 0.25 ± 0.09 2.9 ± 1.1 20.92 ± 8.86**

N.A., not available because of poor fitting value (R2 < 0.8) in the terminal phase.

*

p < 0.05.

**

p < 0.01.

a

Estimated AUC0–t.