Li Yuxin, Brown Powel H
Lester and Sue Smith Breast Center, Baylor College of Medicine, Houston, TX 77030, USA.
Recent Results Cancer Res. 2009;181:121-34. doi: 10.1007/978-3-540-69297-3_13.
The successful demonstration that the selective estrogen receptor modulators (SERMs) tamoxifen and raloxifene reduce the risk of breast cancer has stimulated great interest in using drugs to prevent breast cancer in high-risk women. In addition, recent results from breast cancer treatment trials suggest that aromatase inhibitors may be even more effective at preventing breast cancer than are SERMs. However, while SERMs and aromatase inhibitors do prevent the development of many estrogen-receptor (ER)-positive breast cancers, these drugs do not prevent the development of ER-negative breast cancer. Thus, there is an urgent need to identify agents that can prevent ER-negative breast cancer. We have studied the cancer preventative activity of several classes of drugs for their ability to prevent ER-negative breast cancer in preclinical models. Results from these studies demonstrate that rexinoids (analogs of retinoids that bind and activate RXR receptors), tyrosine kinase inhibitors (such as EGFR inhibitors and dual kinase inhibitors that block EGFR and HER2/neu signaling), and cyclo-oxygenase 2 (COX-2) inhibitors all prevent ER-negative breast cancer in transgenic mice that develop ER-negative breast cancer. Other promising agents now under investigation include vitamin D and vitamin D analogs, drugs that activate PPAR-gamma nuclear receptors, and statins. Many of these agents are now being tested in early phase cancer prevention clinical trials to determine whether they will show activity in breast tissue and whether they are safe for use in high-risk women without breast cancer. The current status of these studies will be reviewed. It is anticipated that in the future, drugs that effectively prevent ER-negative breast cancer will be used in combination with hormonal agents such SERMs or aromatase inhibitors to prevent all forms of breast cancer.
选择性雌激素受体调节剂(SERM)他莫昔芬和雷洛昔芬可降低乳腺癌风险,这一成功的论证激发了人们对使用药物预防高危女性乳腺癌的浓厚兴趣。此外,乳腺癌治疗试验的最新结果表明,芳香化酶抑制剂在预防乳腺癌方面可能比SERM更有效。然而,虽然SERM和芳香化酶抑制剂确实能预防许多雌激素受体(ER)阳性乳腺癌的发生,但这些药物并不能预防ER阴性乳腺癌的发生。因此,迫切需要确定能够预防ER阴性乳腺癌的药物。我们研究了几类药物在临床前模型中预防ER阴性乳腺癌的防癌活性。这些研究结果表明,视黄酸X受体激动剂(维甲酸的类似物,可结合并激活RXR受体)、酪氨酸激酶抑制剂(如阻断EGFR和HER2/neu信号传导的EGFR抑制剂和双激酶抑制剂)以及环氧化酶2(COX-2)抑制剂均可预防发生ER阴性乳腺癌的转基因小鼠发生ER阴性乳腺癌。目前正在研究的其他有前景的药物包括维生素D及其类似物、激活过氧化物酶体增殖物激活受体γ核受体的药物以及他汀类药物。目前,这些药物中的许多正在早期癌症预防临床试验中进行测试,以确定它们是否会在乳腺组织中显示活性,以及它们对无乳腺癌的高危女性使用是否安全。本文将综述这些研究的现状。预计未来,有效预防ER阴性乳腺癌的药物将与SERM或芳香化酶抑制剂等激素药物联合使用,以预防所有形式的乳腺癌。