A Review on Selective Estrogen Receptor Modulators

Selective estrogen receptor modulators drugs, which exert estrogenic as well as antiestrogenic actions in a tissue selective manner, are used for the treatment of osteoporosis, breast cancer and with effects on the uterus and vagina that depend on the interaction with the estrogen receptors in target tissues. Due to decline of estrogen levels after menopause, hot flashes and sweating occurred as the part of the menopausal vasomotor symptoms with the estrogen related urogenital atrophy and loss of bone density. Selective estrogen receptor modulators (SERMs) has three compounds Tamoxifen Citrate, Raloxifene, Bazedofene. Tamoxifen acts as selective estrogen receptor modulator or as a partial agonist of the estrogen receptors. It has mixed estrogenic and anti-estrogenic activity with its profile of effects deficiency by tissue. Raloxifene is used for the treatment of oestoporosis in postmenopausal women and also reduces breast density. Bazedofene has been also developed for the treatment of osteoporosis. The estrogen receptor has two subunits alpha and beta and SERMs interact either of these subunits and form this interaction, there is a certain level of target site specificity and tissue specificity of SERMs action. Tamoxifen represented agonist effects in inhibiting neutralised migration and preventing arthritis progression in ovariectomized mice. Clomiphene citrate and tamoxifen commonly used SERMs for the induction of ovulation. that Bazedoxifen enhances OPCs into functional oligodendrocytes which enhanced OPC differentiation and remyelination. Estrogen receptor alpha play a vital role in the etiology, treatment and prevention of the majority breast cancer. The SERMs raloxifene and bazedoxifen also both reportedly inhibit bone resorptive activity in postmenopausal osteoporosis patients and have been used to prevent bone fragility fractures.