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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Derailed Estrogen Signaling and Breast Cancer: An Authentic Couple
Bramanandam Manavathi,Oindrilla Dey,Vijay Narsihma Reddy Gajulapalli,Raghavendra Singh Bhatia,Suresh Bugide,Rakesh Kumar +5 more
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Anti-inflammatory effect of selective estrogen receptor modulators (SERMs) in microglial cells
TL;DR: It seems that the raloxifene-induced protection in N9 microglia was connected to a decline of LPS-induced DNAbinding activity of AP-1 but not that of NF-κB transcription factors.
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Comparison of Proteomic and Genomic Analyses of the Human Breast Cancer Cell Line T47D and the Antiestrogen-resistant Derivative T47D-r
Martina Huber,Inke Bahr,Jörn Krätzschmar,Andreas Becker,Eva-Christina Müller,Peter Donner,Hans-Dieter Pohlenz,Martin R. Schneider,Anette Sommer +8 more
TL;DR: In this article, the authors analyzed differences in the gene and protein expression pattern of the human breast carcinoma cell line T47D and its derivative T 47D-r, which is resistant toward the pure antiestrogen ZM 182780 (Faslodex™, fulvestrant).
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The mechanisms and managements of hormone-therapy resistance in breast and prostate cancers
TL;DR: The potential mechanisms of antihormone-therapy resistance in breast and prostate cancers are discussed, especially focusing on the similarities and differences of these two cancers.
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Beyond the ligand-binding pocket: targeting alternate sites in nuclear receptors.
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Journal ArticleDOI
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