Conjugated estrogens/bazedoxifene

A combination preparation of conjugated estrogens and the selective estrogen receptor modulator (SERM) bazedoxifene that can be used for hormone replacement purposes. The conjugated estrogens increase the diminishing levels of estrogen in menopausal and postmenopausal women by binding to and activating estrogen receptors (ERs), which, in turn, bind to estrogen response elements (EREs) in target genes; this results in the transcription of estrogen-regulated genes. Maintaining adequate estrogen levels decreases symptoms such as hot flashes, night sweats, irregular menstruation, fat redistribution, mood swings, sleep disorders, vaginal dryness and osteoporosis. Bazedoxifene specifically binds to and activates ERs in certain tissues, including liver, bone, breast, and endometrium, and also promotes the transcription of estrogen-regulated genes in these tissues. However, bazedoxifene acts as an estrogen antagonist in uterine and breast tissue, thereby blocking the proliferative effects of estrogen-binding to ER-positive cells in these tissues.

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