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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)
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BMC Pharmacology and Toxicology

ISSN: 2050-6511

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