Bundred Nigel, Howell Anthony
Academic Department of Surgery, University Hospital of South Manchester, Research and Teaching, Nell Lane, Manchester, M20 2LR, UK.
Expert Rev Anticancer Ther. 2002 Apr;2(2):151-60. doi: 10.1586/14737140.2.2.151.
Fulvestrant (Faslodex, formerly ICI 182,780) is a potent steroidal antiestrogen that mediates its effects by estrogen receptor downregulation. It appears to act as a pure antiestrogen and exhibits none of the negative side effects associated with the partial agonist activity of tamoxifen. It has been shown to be as effective as the oral aromatase inhibitor anastrozole in postmenopausal women with advanced breast cancer who have progressed on prior endocrine therapy, principally tamoxifen. It therefore provides the clinician with an alternative therapeutic strategy following the development of tamoxifen resistance. Fulvestrant might also have potential as a follow-on therapy after tamoxifen in an adjuvant setting and help alleviate some of the concerns surrounding long-term (up to 5 years) tamoxifen therapy.
氟维司群(芙仕得,原ICI 182,780)是一种强效甾体类抗雌激素药物,通过下调雌激素受体发挥作用。它似乎作为一种纯粹的抗雌激素起作用,没有表现出与他莫昔芬部分激动剂活性相关的负面副作用。在先前接受内分泌治疗(主要是他莫昔芬)后病情进展的绝经后晚期乳腺癌女性中,已证明它与口服芳香化酶抑制剂阿那曲唑一样有效。因此,在他莫昔芬耐药后,它为临床医生提供了一种替代治疗策略。氟维司群在辅助治疗中作为他莫昔芬之后的后续治疗可能也有潜力,并有助于减轻围绕他莫昔芬长期(长达5年)治疗的一些担忧。