THE FUTURE OF NEW PURE ANTIESTROGENS IN CLINICAL BREAST-CANCER
THE FUTURE OF NEW PURE ANTIESTROGENS IN CLINICAL BREAST-CANCER
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DOI：
10.1007/bf00662395
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发表时间：
1993-01-01
影响因子：
3.8
通讯作者：
WAKELING, AE
中科院分区：
文献类型：
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作者：
WAKELING, AE
寻求鉴定新的纯抗雌激素的基本原理是基于这样的认识：以他莫昔芬为代表的现有抗雌激素均具有部分激动剂（雌激素）活性。从概念上讲，纯抗雌激素在消除雌激素对乳腺肿瘤生长的促有丝分裂作用方面应该比他莫昔芬更有效。描述了纯抗雌激素 ICI 164,384 和 ICI 182,780 的发现和特性，并与他莫昔芬进行了对比。描述了这些化合物的关键特征，这些特征可能与其在乳腺癌治疗中的治疗应用特别相关。其中包括预测在他莫昔芬治疗期间疾病复发的患者的疗效的实验数据，以及纯抗雌激素在晚期乳腺癌一线治疗中比他莫昔芬更有效的潜力。数据表明，疗效的提高可能会随着肿瘤缓解更快、更完全或更持久而出现。 ICI 182,780 的临床试验将揭示这些预测中的一项或多项是否正确。
The rationale for seeking to identify new pure antiestrogens was based on the recognition that existing antiestrogens, exemplified by tamoxifen, all possess partial agonist (estrogenic) activity. Conceptually, pure antiestrogens should be more effective than tamoxifen in ablating the mitogenic action of estrogens on breast tumor growth. The discovery and properties of the pure antiestrogens ICI 164,384 and ICI 182,780 are described and contrasted with those of tamoxifen. Key characteristics of these compounds which may be of particular relevance to their therapeutic application in the treatment of breast cancer are described. These include experimental data which predict efficacy in patients whose disease recurs during tamoxifen treatment, and the potential for pure antiestrogens to demonstrate greater efficacy than tamoxifen in first-line treatment of advanced breast cancer. The data imply that gains in efficacy could emerge as more rapid, more complete, or longer-lasting tumor remissions. Clinical trials with ICI 182,780 will reveal whether one or more of these predictions is correct.