Table 1.
Mean ± SD Peak Plasma Concentrations of Tamoxifen Metabolites in Rats after Oral Dosing of Tamoxifen and Endoxifen Once Daily for Three Days (n=5)
Drug | Dose (mg/kg) | Tamoxifen (nM) | Endoxifen (nM) | 4-OH-Tamoxifen (nM) | N-Desmethyl-Tamoxifen (nM) |
---|---|---|---|---|---|
Tamoxifena | 20 | 924 ± 111 | 69 ± 9 | 135 ± 18 | 682 ± 104 |
200 | 8380 ± 1530 | 129 ± 43 | 768 ± 106 | 4920 ± 730 | |
Endoxifen* | 5 | --- | 168 ± 102 | --- | --- |
80 | --- | 8050 ± 1080 | --- | --- | |
200 | --- | 9620 ± 1740 | --- | --- |
Tamoxifen, t = 2 hrs after dosing on Day 3; Endoxifen, t = 4 hrs after dosing on Day 3