Jordan V C
Comprehensive Cancer Center, Northwestern University Medical School, Chicago, IL 60611-3008, USA.
Lancet Oncol. 2000 Sep;1(1):43-9. doi: 10.1016/S1470-2045(00)00009-7.
Tamoxifen, originally described as an anti-oestrogen and antifertility agent in the rat, is now a pioneering medicine for the treatment and prevention of breast cancer. Its success is the result of an effective collaboration between laboratory research and clinical trial processes. However, this drug is more than just an anti-oestrogen to treat breast cancer. Laboratory and clinical research defined the concept of selective oestrogen receptor modulation in the 1980s. Non-steroidal anti-oestrogens show oestrogen-like activity in bones and lower cholesterol, but block oestrogen action in the breast and uterus. This realisation led to the development of chemical cousins, known as selective oestrogen receptor modulators. One of these compounds, raloxifene, is used for the prevention of osteoporosis, but is currently being tested as a preventive for breast cancer.
他莫昔芬最初在大鼠中被描述为一种抗雌激素和抗生育药物,现在是治疗和预防乳腺癌的开创性药物。它的成功是实验室研究与临床试验过程有效合作的结果。然而,这种药物不仅仅是一种治疗乳腺癌的抗雌激素药物。实验室和临床研究在20世纪80年代定义了选择性雌激素受体调节的概念。非甾体类抗雌激素在骨骼中表现出雌激素样活性并降低胆固醇,但会阻断雌激素在乳腺和子宫中的作用。这一认识促使了化学类似物的开发,即选择性雌激素受体调节剂。其中一种化合物雷洛昔芬用于预防骨质疏松症,但目前正在作为乳腺癌预防药物进行测试。