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. 2018 Nov 29;7:e37161. doi: 10.7554/eLife.37161

Table 1. Competitive inhibitors of estrogen receptor alpha.

Antiestrogen Class Approved clinical indications
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4-Hydroxytamoxifen (4-OHT)
SERM • Adjuvant treatment for ER + breast cancers (Early Breast Cancer Trialists' Collaborative Group., 1998).
• Metastatic Breast Cancer (Lipton, 1982).
• Ductal Carcinoma in Situ (Allred et al., 2012).
• Reduction in Breast Cancer Incidence in High Risk Women (Visvanathan, 2009).
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Raloxifene (RAL)
SERM • Osteoporosis in postmenopausal women (Messalli and Scaffa, 2010).
• Reduction in Breast Cancer Incidence in High Risk Women(Cauley et al., 2001).
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Fulvestrant (FULV)
SERD • First-line therapy for metastatic breast cancer (Howell et al., 2004).
• Postmenopausal women with progressive breast cancer following other antiestrogen therapy (Osborne et al., 2002; Howell et al., 2002).
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Bazedoxifene (BZA)
SERM/SERD • In combination with conjugated equine estrogens (DUAVEE) to prevent postmenopausal osteoporosis (Tikoo and Gupta, 2015).