Namer M, Lalanne C, Baulieu E E
Cancer Res. 1980 May;40(5):1750-2.
In 25 cases of postmenopausal breast cancer, estradiol receptor (ER) and progesterone receptor (PR) were measured in cutaneous metastatic nodules before and after administration of 30 mg of tamoxifen per day for 1 week. No response was recorded in ER-poor cases. However, in tumors containing greater than 10 fmol ER per mg cytosol protein, 6 of 14 cases showed an increase in PR of greater than 30 fmol/mg cytosol protein. The presence or absence of PR before administration of tamoxifen did not discriminate systematically between hormone-responsive and nonresponsive tumors. These findings demonstrate in vivo that biochemical changes brought about by an agent binding to ER can be observed only in ER-positive cases. In addition they suggest that, in these ER-positive cases responding to tamoxifen by increase of PR, the simultaneous or sequential administration of both antiestrogen (rescuing PR) and progestagen (decreasing PR) may allow better hormonal control of the disease.
在25例绝经后乳腺癌患者中,于每天服用30毫克他莫昔芬,持续1周前后,对皮肤转移结节中的雌二醇受体(ER)和孕酮受体(PR)进行了测量。ER水平低的病例未记录到反应。然而,在每毫克胞浆蛋白中ER含量大于10 fmol的肿瘤中,14例中有6例显示PR增加大于30 fmol/mg胞浆蛋白。在服用他莫昔芬之前PR的有无并不能系统地区分激素反应性肿瘤和无反应性肿瘤。这些发现表明,在体内,只有在ER阳性病例中才能观察到与ER结合的药物引起的生化变化。此外,它们还提示,在这些通过PR增加对他莫昔芬有反应的ER阳性病例中,同时或序贯给予抗雌激素(挽救PR)和孕激素(降低PR)可能会更好地实现对该疾病的激素控制。