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Table 2 Effect of hormonal status on the TAM pharmacokinetics and its metabolites END, 4-HTAM and NDTAM in the investigated TAM-treated breast cancer patients (n = 40). Data are reported as the geometric mean (95% CI)

From: Hormonal status affects plasma exposure of tamoxifen and its main metabolites in tamoxifen-treated breast cancer patients

 

Premenopausal (n = 20)

Postmenopausal (n = 20)

 

AUCτ (ng*h/mL)

Geometric Mean

95% CI

Geometric Mean

95% CI

P-value

TAM

2806.78

2128.19

3701.75

4829.41

4244.20

5495.30

<  0.001

NDTAM

11,643.86

8132.88

16,670.55

20,253.09

17,886.43

22,932.88

<  0.010

4-HTAM

61.67

44.15

86.15

112.23

98.75

127.55

<  0.001

END

192.14

111.75

330.35

452.77

355.65

576.40

0.013

Css (ng/mL)

 TAM

116.95

88.67

154.24

201.23

176.84

228.97

<  0.001

 NDTAM

485.16

338.87

694.61

843.88

745.27

955.54

<  0.010

 4-HTAM

2.57

1.84

3.59

4.68

4.11

5.31

<  0.001

 END

8.01

4.66

13.76

18.87

14.82

24.02

0.013

Metabolic Ratios

 TAM/NDTAM

0.20

0.15

0.26

0.21

0.19

0.23

0.523

 TAM/4-HTAM

46.27

36.67

58.39

38.12

31.79

45.70

0.177

 NDTAM/END

68.98

46.26

102.86

44.35

32.78

60.01

0.230

 4-HTAM/END

0.30

0.20

0.44

0.24

0.19

0.31

0.275

Apparent clearance (L/h)

 TAM

7.13

5.40

9.40

4.14

3.64

4.71

0.015

  1. Tamoxifen (TAM), endoxifen (END), 4-hydroxytamoxifen (4-HTAM) and N-desmethyl tamoxifen (NDTAM)