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Droloxifene is an anti-estrogen triphenylthylene selective estrogen receptor modulator (SERM); it is an analog of tamoxifen. Droloxifene acts as an estrogen receptor agonist in bone and as an estrogen receptor antagonist in breast tissue. As a result of these actions, this compound exhibits anticancer chemotherapeutic, chemopreventive, anti-osteoporotic, and anti-resorptive benefits. In breast cancer cells, droloxifene decreases production of NO and increases levels of pro-apoptotic TGF-β. Droloxifene increases apoptosis in luteal cells in vivo, increasing levels of c-myc and increasing the Bax/Bcl-2 ratio. In ovariectomized rats that act as a post-menopausal animal model, droloxifene inhibits bone resorption and turnover as well as estrogen-related bone loss. This compound also decreases levels of E-selectin and increases levels if vascular cellular adhesion molecule 1 (VCAM-1) in clinical settings.

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