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Tamoxifen是一种三苯乙烯衍生物的反式异构体,用其柠檬酸盐口服。推荐治疗乳腺癌的初始剂量是每日两次共10 mg,如无效,可在一个月内把剂量逐步加至每日两次共20～40mg。药效学研究表明,此剂在卵巢切除或未成熟动物中有抑制外源性雌激素的效果,在成熟的整体动物(大鼠和猴)试验以及用子宫组织培养的体外研究中,显示了抑制雌激素合成的作用。但在啮齿类动物中,Tamoxifen能引起不明显的雌激素作用,接受治疗量的少数妇女中也发现有些类似雌激素样的作用。Tamoxifen能抑制或逆转大鼠某些化学诱发肿瘤的生长,当与致癌物二甲基苯并蒽同时投予时,肿瘤发生率下降。用人体乳腺肿瘤细胞培养做的体外研究中,此剂加人含雌激素受体的肿瘤培养基时是抑制肿瘤细胞的增殖,但加入无雌激素受体的肿瘤培养基时,则
Tamoxifen is a trans-isomer of a tristyryl derivative that is orally administered with its citrate salt. The recommended initial dose for breast cancer treatment is 10 mg twice a day. If it is ineffective, the dose can be gradually increased to 20 to 40 mg twice a day within one month. Pharmacodynamic studies have shown that this agent has the effect of suppressing exogenous estrogen in ovariectomized or immature animals, and has been shown in mature whole animal (rat and monkey) tests and in in vitro studies using uterine tissue culture. Inhibition of estrogen synthesis. However, in rodents, tamoxifen can cause insignificant estrogen effects, and a small number of women receiving treatment also found some estrogen-like effects. Tamoxifen can inhibit or reverse the growth of some chemically-induced tumors in rats. When administered simultaneously with the carcinogen dimethylbenzopyrene, the incidence of tumors decreases. In vitro studies using human breast tumor cell cultures, this agent added tumor growth medium containing estrogen receptors to inhibit the proliferation of tumor cells, but when added to the tumor medium without estrogen receptors,