Daniel C P, Gaskell S J, Bishop H, Nicholson R I
J Endocrinol. 1979 Dec;83(3):401-8. doi: 10.1677/joe.0.0830401.
An assay has been established for the selective measurement of tamoxifen and its monohydroxy derivative, metabolite B, in human plasma. The assay was used to examine the concentrations of these compounds, relative to oestradiol-17 beta, in the plasma of patients undergoing tamoxifen therapy for advanced breast cancer. Oral administration of the drug (20 mg twice a day) raised the level of tamoxifen in plasma to approximately 200 ng/ml 20 days after the commencement of treatment. This level was 3000-fold higher than the corresponding concentration of oestradiol which remained within the range for post-menopausal women. Metabolite B was present in plasma at a much lower concentration than tamoxifen although in considerable excess over oestradiol. The overall results are discussed in relation to the possible mechanism of action of the drug.
已建立一种用于选择性测定人血浆中他莫昔芬及其单羟基衍生物（代谢物B）的分析方法。该分析方法用于检测晚期乳腺癌患者接受他莫昔芬治疗时，相对于雌二醇-17β，这些化合物在血浆中的浓度。口服该药物（每日两次，每次20mg），治疗开始20天后，血浆中他莫昔芬水平升至约200ng/ml。该水平比绝经后女性雌二醇的相应浓度高3000倍，而后者仍处于正常范围内。代谢物B在血浆中的浓度远低于他莫昔芬，尽管其含量仍大大超过雌二醇。结合该药物可能的作用机制对总体结果进行了讨论。
