Haynes B, Dowsett M
Department of Academic Biochemistry, Royal Marsden Hospital, London, England.
Drugs Aging. 1999 May;14(5):323-36. doi: 10.2165/00002512-199914050-00001.
Observations of the pharmacology of tamoxifen and related compounds have lead to the concept of selective estrogen receptor modulators (SERMs). This new class of drug displays estrogen agonist or antagonist effects in a tissue-dependent manner and appears to offer an alternative to hormone replacement therapy for the prevention and treatment of osteoporosis and cardiovascular disease in postmenopausal women. Moreover, the estrogen antagonist actions of SERMs on breast tissue may also provide a protective effect against breast cancer. Although tamoxifen therapy reduces plasma cholesterol levels and maintains bone density, it is also associated with an increased risk of endometrial cancer, pulmonary embolism and deep vein thrombosis. This has lead to the development of newer SERMs which will hopefully lack these adverse effects of tamoxifen. These compounds promise a new era of disease prevention in the aging woman and their therapeutic potential is currently being evaluated in large-scale clinical trials.
对他莫昔芬及相关化合物药理学的观察催生了选择性雌激素受体调节剂（SERM）的概念。这类新型药物以组织依赖的方式表现出雌激素激动剂或拮抗剂的作用，似乎为绝经后女性预防和治疗骨质疏松症及心血管疾病提供了激素替代疗法之外的另一种选择。此外，SERM对乳腺组织的雌激素拮抗作用也可能对乳腺癌起到保护作用。尽管他莫昔芬治疗可降低血浆胆固醇水平并维持骨密度，但它也与子宫内膜癌、肺栓塞和深静脉血栓形成的风险增加有关。这促使了更新型SERM的研发，有望避免他莫昔芬的这些不良反应。这些化合物有望开创老年女性疾病预防的新时代，其治疗潜力目前正在大规模临床试验中进行评估。
