Draper M W, Flowers D E, Neild J A, Huster W J, Zerbe R L
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA.
Pharmacology. 1995 Apr;50(4):209-17. doi: 10.1159/000139284.
This 21-day, open-label study evaluated the effects of raloxifene and tamoxifen on estrogen-induced changes in serum levels of anterior pituitary hormones (prolactin, luteinizing hormone, and follicle-stimulating hormone), sex steroids (testosterone, estradiol), and binding globulins [thyroid binding globulin (T3 resin uptake), transcortin, sex steroid binding globulin]. Seventeen healthy male volunteers completed the study after being randomized to one of three treatments: raloxifene, tamoxifen, or placebo. Six subjects received raloxifene (200 mg daily) for 10 days, 6 subjects received tamoxifen [20 mg twice a day (b.i.d.)] for 10 days, and 5 subjects received placebo for 10 days. All subjects received ethinyl estradiol (20 micrograms b.i.d.) for 7 days starting 3 days after initiation of study drug or placebo treatment. Results of the primary analysis of this study indicate that for six of the seven analyzable parameters of estrogen action (excluding luteinizing hormone) raloxifene blunted the estrogen response; this effect was significant only for T3 resin uptake. Tamoxifen administration significantly blunted or reversed the estrogen effect in all six of these parameters. Raloxifene, an effective antiestrogen in animal models, is also antiestrogenic in humans.
这项为期21天的开放标签研究评估了雷洛昔芬和他莫昔芬对雌激素诱导的垂体前叶激素（催乳素、促黄体生成素和促卵泡激素）、性类固醇（睾酮、雌二醇）以及结合球蛋白[甲状腺结合球蛋白（T3树脂摄取）、皮质素转运蛋白、性类固醇结合球蛋白]血清水平变化的影响。17名健康男性志愿者在被随机分配到三种治疗方案之一后完成了该研究：雷洛昔芬、他莫昔芬或安慰剂。6名受试者接受雷洛昔芬（每日200毫克）治疗10天，6名受试者接受他莫昔芬[每日两次，每次20毫克（bid）]治疗10天，5名受试者接受安慰剂治疗10天。所有受试者在开始研究药物或安慰剂治疗3天后开始连续7天接受乙炔雌二醇（每日两次，每次20微克）治疗。该研究的初步分析结果表明，在雌激素作用的七个可分析参数中的六个（不包括促黄体生成素）方面，雷洛昔芬减弱了雌激素反应；这种作用仅在T3树脂摄取方面显著。在所有这六个参数中，他莫昔芬的给药显著减弱或逆转了雌激素的作用。雷洛昔芬在动物模型中是一种有效的抗雌激素药物，在人体中也具有抗雌激素作用。
