Journal ArticleDOI
Fulvestrant ('Faslodex')--a new treatment option for patients progressing on prior endocrine therapy.
C Morris,A Wakeling +1 more
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TLDR
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 and these new hormonal treatments expand the choice of endocrine therapy for women with advanced breast cancer.Abstract:
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.read more
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Journal ArticleDOI
Synthesis and biological evaluation of stilbene-based pure estrogen antagonists.
TL;DR: Replacement of one of the ethyl substituents in diethylstilbestrol by side chains with functional groups converted this potent estrogen into pure antiestrogens with the potential for the treatment of breast cancer.
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Estrogenic and antiestrogenic activities of 2,4-diphenylfuran-based ligands of estrogen receptors α and β
TL;DR: 3,5-Dialkyl-2,4-bis(4-hydroxyphenylfurans) were shown to act as agonists with preference for ERβ and replacement of one of the alkyl groups by the [(pentylsulfanyl)propyl]aminohexyl side chain afforded estrogen antagonists without receptor selectivity.
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Prevention of breast cancer using SERMs and aromatase inhibitors.
TL;DR: The proof-of-principle demonstrated with tamoxifen suggests that strategies inhibiting estrogen are a logical way forward in breast cancer prevention, and the data pointing to the efficacy of aromatase inhibitors in this setting are outlined.
Journal ArticleDOI
Characterization of a human breast cancer cell line, MCF-7/RU58R-1, resistant to the pure antiestrogen RU 58,668.
TL;DR: It appears as acquired resistance to RU 58,668 is not a result of loss of the ERα expression or function and it is suggested that in the presence of RU58,668, the RU58R-1 cell line probably uses other mitogenic pathways than the ER α pathway for growth and survival.
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Journal ArticleDOI
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