Division of Cancer, Department of Surgery and Oncology, Imperial College London, Hammersmith Hospital, London W12 0NN, United Kingdom.
Annu Rev Med. 2011;62:217-32. doi: 10.1146/annurev-med-052209-100305.
The identification of the link between breast cancer and estrogens has led to the development of antiestrogens, in particular tamoxifen, to inhibit the activities of estrogen receptors (ERs) in breast cancer cells. The clinical use of tamoxifen has played a major part in decreasing breast cancer mortality over the past 30 years. Though antiestrogenic in the breast, some antiestrogens have estrogen-like actions in other tissues, acting to promote bone density and protect against cardiovascular disease, thus raising the possibility of their use in counteracting the effects of estrogen loss following menopause. Moreover, antiestrogens show efficacy as chemopreventive agents in women at high risk of developing breast cancer. Thus, antiestrogens define an important and well-understood class of cancer drug, which continue to be a mainstay in breast cancer treatment.
乳腺癌与雌激素之间关联的确认，促成了抗雌激素药物，特别是他莫昔芬的发展，以抑制乳腺癌细胞中雌激素受体（ERs）的活性。在过去的 30 年中，他莫昔芬的临床应用在降低乳腺癌死亡率方面发挥了重要作用。虽然在乳腺中具有抗雌激素作用，但一些抗雌激素在其他组织中具有类雌激素作用，可促进骨密度并预防心血管疾病，从而增加了它们在对抗绝经后雌激素缺乏影响的可能性。此外，抗雌激素作为化学预防剂在有发展乳腺癌高风险的女性中显示出疗效。因此，抗雌激素药物定义了一类重要且理解透彻的癌症药物，它们仍然是乳腺癌治疗的主要药物。
