Management of hormone replacement therapy and selective estrogen receptor modulators (SERMs) in women with systemic hepatic, renal, or bone disease

2000 ◽  
Vol 33 (9) ◽  
pp. 645-651 ◽  
Author(s):  
M. Dören
Keyword(s):  
Estrogen Receptor ◽  
Hormone Replacement Therapy ◽  
Replacement Therapy ◽  
Bone Disease ◽  
Hormone Replacement ◽  
Selective Estrogen Receptor Modulators ◽  
Estrogen Receptor Modulators ◽  
Receptor Modulators

Selective Estrogen Receptor Modulators: Structure, Function, and Clinical Use

2000 ◽  
Vol 18 (17) ◽  
pp. 3172-3186 ◽  
Author(s):  
C. Kent Osborne ◽  
Hong (Holly) Zhao ◽  
Suzanne A. W. Fuqua
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptor ◽  
Cancer Prevention ◽  
Hormone Replacement ◽  
Metastatic Breast ◽  
Selective Estrogen Receptor Modulators ◽  
Breast Cancer Prevention ◽  
Estrogen Receptor Modulators ◽  
Prevention And Treatment ◽  
Receptor Modulators

ABSTRACT: The sex hormone estrogen is important for many physiologic processes. Prolonged stimulation of breast ductal epithelium by estrogen, however, can contribute to the development and progression of breast cancer, and treatments designed to block estrogen’s effects are important options in the clinic. Tamoxifen and other similar drugs are effective in breast cancer prevention and treatment by inhibiting the proliferative effects of estrogen that are mediated through the estrogen receptor (ER). However, these drugs also have many estrogenic effects depending on the tissue and gene, and they are more appropriately called selective estrogen receptor modulators (SERMs). SERMs bind ER, alter receptor conformation, and facilitate binding of coregulatory proteins that activate or repress transcriptional activation of estrogen target genes. Theoretically, SERMs could be synthesized that would exhibit nearly complete agonist activity on the one hand or pure antiestrogenic activity on the other. Depending on their functional activities, SERMs could then be developed for a variety of clinical uses, including prevention and treatment of osteoporosis, treatment and prevention of estrogen-regulated malignancies, and even for hormone replacement therapy. Tamoxifen is effective in patients with ER-positive metastatic breast cancer and in the adjuvant setting. The promising role for tamoxifen in ductal carcinoma-in-situ or for breast cancer prevention is evolving, and its use can be considered in certain patient groups. Other SERMs are in development, with the goal of reducing toxicity and/or improving efficacy, and future agents have the potential of providing a new paradigm for maintaining the health of women.

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