Journal ArticleDOI
Fulvestrant ('Faslodex')--a new treatment option for patients progressing on prior endocrine therapy.
C Morris,A Wakeling +1 more
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
Citations
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Journal ArticleDOI
Targeting Toll-like receptor 4 with CLI-095 (TAK-242) enhances the antimetastatic effect of the estrogen receptor antagonist fulvestrant on non-small cell lung cancer
TL;DR: It is suggested that CLI-095 enhances the antimetastatic effect of fulvestrant on NSCLC and provided support for further investigation of the antitumor activity of combined therapy with antiestrogen and anti-TLR4 agents in the clinic.
Book ChapterDOI
Estrogen receptors and anti-estrogen therapies.
TL;DR: There is considerable headway to be made in further elucidating estrogen receptor function, in particular in identifying the mechanisms underlying endocrine resistance, and it is hoped that this will lead to the development of novel therapies aimed at overcomingendocrine resistance.
Dissertation
Effect of estrogen on host-pathogen interactions in ex vivo and in vitro models of the inflammatory phase of age-related impaired healing
TL;DR: Estrogen may promote the resolution of wound bacterial infections during youth but this protection is lost as estrogen levels decline with increasing age, resulting in increased propensity and progression of wound infections in the elderly.
Journal ArticleDOI
An Efficient Regioselective Preparation of Fulvestrant
TL;DR: Fulvestrant (Figure 1) belongs to an important class of antiestrogens and is completely free of the partial agonist estrogen-like activity associated with such currently available anti-estrogens.
References
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Journal ArticleDOI
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Journal ArticleDOI
Superior Efficacy of Letrozole Versus Tamoxifen as First-Line Therapy for Postmenopausal Women With Advanced Breast Cancer: Results of a Phase III Study of the International Letrozole Breast Cancer Group
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