Fulvestrant: an oestrogen receptor antagonist with a novel mechanism of action
Top Cited Papers
Open Access
- 5 March 2004
- journal article
- review article
- Published by Springer Nature in British Journal of Cancer
- Vol. 90 (S1) , S2-S6
- https://doi.org/10.1038/sj.bjc.6601629
Abstract
Due to their favourable tolerability profiles, endocrine therapies have long been considered the treatment of choice for hormone-sensitive metastatic breast cancer. However, the oestrogen agonist effects of the available selective oestrogen receptor modulators, such as tamoxifen, and the development of cross-resistance between endocrine therapies with similar modes of action have led to the need for new treatments that act through different mechanisms. Fulvestrant (‘Faslodex’) is the first of a new type of endocrine treatment – an oestrogen receptor (ER) antagonist that downregulates the ER and has no agonist effects. This article provides an overview of the current understanding of ER signalling and illustrates the unique mode of action of fulvestrant. Preclinical and clinical study data are presented in support of the novel mechanism of action of this new type of ER antagonist.Keywords
This publication has 57 references indexed in Scilit:
- The search for the ideal SERMExpert Opinion on Pharmacotherapy, 2002
- Anastrozole alone or in combination with tamoxifen versus tamoxifen alone for adjuvant treatment of postmenopausal women with early breast cancer: first results of the ATAC randomised trialThe Lancet, 2002
- Distinct expression patterns of ER and ER in normal human mammary glandJournal of Clinical Pathology, 2002
- Estrogen receptor beta in breast cancer.Endocrine-Related Cancer, 2002
- Cloning of a novel receptor expressed in rat prostate and ovary.Proceedings of the National Academy of Sciences, 1996
- Short-term effects of pure anti-oestrogen ICI 182780 treatment on oestrogen receptor, epidermal growth factor receptor and transforming growth factor-alpha protein expression in human breast cancerEuropean Journal Of Cancer, 1996
- Effects of short-term antiestrogen treatment of primary breast cancer on estrogen receptor mRNA and protein expression and on estrogen-regulated genesBreast Cancer Research and Treatment, 1996
- Megestrol Acetate in Advanced Breast CarcinomaOncology, 1994
- Novel antioestrogens without partial agonist activityJournal of Steroid Biochemistry, 1988
- Steroid receptors study in breast carcinomaMedical and Pediatric Oncology, 1978