International Journal of Endocrinology / 2017 / Article / Tab 2

Review Article

The Tissue-Selective Estrogen Complex (Bazedoxifene/Conjugated Estrogens) for the Treatment of Menopause

Table 2

Preclinical studies on breast tissue.

ModelResults

Song et al. [23]MCF-7 breast cancer cells(i) BZA blocked CE-induced stimulation, including DNA synthesis, reduction of apoptosis, expression of cMyc, pS2, and WNT1-inducible signaling pathway protein 2
Wardell et al. [24]MCF-7 breast cancer cells(i) BZA showed inverse agonist activity on many genes regulated by estradiol
Chang et al. [25]MCF-7 breast cancer cells and microarrays(i) BZA, RLZ, and LAS inhibited the proliferation of breast cancer cells induced by CE, with the following antagonist power: BZA > RLX > LAS
(ii) BZA inhibited a group of genes regulated by CE; this profile is different from those of RLX and LAS
Peano et al. [26]Ovariectomized mice(i) The stimulating effects of CE on the expression of amphiregulin (a marker of ductal proliferation) were antagonized by BZA > RLX > LAS
(ii) BZA was more effective than RLX and LAS in reducing ductal growth
Song et al. [23]Ovariectomized mice(i) BZA blocked gene expression induced by CE and the growth of mammary terminal ducts and acini
(ii) BZA blocked tumor growth and gene expression in mice with MCF-7 xenografts
Ethun et al. [27]Ovariectomized cynomolgus macaques(i) 6-month treatment with BZA/CE significantly reduced the increase in epithelial density, the growth, and the ductal proliferation induced by CE (all )
(ii) BZA/CE treatment reduced ER protein expression and activity markers

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