In Search of Optimal Long-Term Female Hormone Replacement: The Potential of Selective Estrogen Receptor Modulators

1997 ◽  
Vol 48 (4) ◽  
pp. 155-163 ◽  
Author(s):  
Bruce H. Mitlak ◽  
Fredric J. Cohen
Keyword(s):  
Estrogen Receptor ◽  
Hormone Replacement ◽  
Selective Estrogen Receptor Modulators ◽  
Female Hormone ◽  
Estrogen Receptor Modulators ◽  
Receptor Modulators

scholarly journals Incident Type 2 Diabetes Risk of Selective Estrogen Receptor Modulators in Female Patients with Breast Cancer

2021 ◽  
Vol 14 (9) ◽  
pp. 925
Author(s):  
Yeo-Jin Choi ◽  
Keunhyeong Bak ◽  
Yoon Yeo ◽  
Yongwon Choi ◽  
Sooyoung Shin
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptor ◽  
Metastatic Cancer ◽  
Selective Estrogen Receptor Modulators ◽  
Diabetes Risk ◽  
Incident Diabetes ◽  
Estrogen Receptor Modulators ◽  
Increase Diabetes Risk ◽  
Receptor Modulators

Accumulating evidence indicates a link between diabetes and cancer. Selective estrogen receptor modulators (SERMs) may increase diabetes risk via antiestrogen effects. This study investigated incident diabetes risk of SERM treatment and its effects on metastatic cancer and death prevention in breast cancer survivors. This retrospective cohort study included female patients with early-stage breast cancer, treated with or without SERMs, between 2008 and 2020 in a tertiary care hospital in Korea. Four propensity score-matched comparison pairs were designed: SERM use versus non-use, long-term use (≥1500 days) versus non-use, tamoxifen use versus non-use, and toremifene use versus non-use; then, logistic regression analysis was performed for risk analysis. SERMs in general were not associated with an elevated risk of diabetes; however, when used for ≥1500 days, SERMs—especially toremifene—substantially increased diabetes risk in breast cancer patients (OR 1.63, p = 0.048). Meanwhile, long-term SERM treatment was effective at preventing metastatic cancer (OR 0.20, p < 0.001) and death (OR 0.13, p < 0.001). SERM treatment, albeit generally safe and effective, may increase diabetes risk with its long-term use in women with breast cancer. Further studies are required to verify the association between toremifene treatment and incident diabetes.

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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