Morris C, Wakeling A
AstraZeneca, Wilmington, Delaware 19850, USA.
Endocr Relat Cancer. 2002 Dec;9(4):267-76. doi: 10.1677/erc.0.0090267.
Since its introduction more than 30 years ago, tamoxifen has been the most widely used endocrine therapy for the treatment of women with advanced breast cancer. More recently, a number of alternative endocrine treatments have been developed, including several selective estrogen receptor modulators (SERMs), aromatase inhibitors (AIs) and, most recently, fulvestrant ('Faslodex'). Fulvestrant is an estrogen receptor (ER) antagonist, which, unlike the SERMs, has no known agonist (estrogenic) effect and downregulates the ER protein. Tamoxifen is effective and well tolerated, although the non-steroidal AIs, anastrozole and letrozole, are more effective treatments for advanced disease than tamoxifen. Fulvestrant has recently gained US Food and Drug Administration approval for the treatment of hormone receptor-positive metastatic breast cancer in postmenopausal women with disease progression following antiestrogen therapy. In two global phase III clinical trials fulvestrant was at least as effective and as equally well tolerated as anastrozole for the treatment of postmenopausal women with advanced and metastatic breast cancer. In a retrospective analysis of the combined data from these trials, mean duration of response was significantly greater for fulvestrant compared with anastrozole. These new hormonal treatments expand the choice of endocrine therapy for women with advanced breast cancer and offer new options for sequencing and combining treatments.
自30多年前问世以来,他莫昔芬一直是治疗晚期乳腺癌女性最广泛使用的内分泌疗法。最近,已开发出多种替代内分泌疗法,包括几种选择性雌激素受体调节剂(SERM)、芳香化酶抑制剂(AI),以及最近的氟维司群(“芙仕得”)。氟维司群是一种雌激素受体(ER)拮抗剂,与SERM不同,它没有已知的激动剂(雌激素)作用,并且能下调ER蛋白。他莫昔芬疗效显著且耐受性良好,尽管非甾体AI阿那曲唑和来曲唑对晚期疾病的治疗比他莫昔芬更有效。氟维司群最近已获得美国食品药品监督管理局批准,用于治疗抗雌激素治疗后疾病进展的绝经后激素受体阳性转移性乳腺癌女性。在两项全球III期临床试验中,氟维司群在治疗绝经后晚期和转移性乳腺癌女性方面至少与阿那曲唑一样有效,且耐受性相当。在对这些试验合并数据的回顾性分析中,氟维司群的平均缓解持续时间明显长于阿那曲唑。这些新的激素疗法为晚期乳腺癌女性扩大了内分泌治疗的选择范围,并为治疗的排序和联合提供了新的选择。
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