TAS-108

TAS-108 is a synthetic steroidal selective estrogen receptor modulator (SERM) with antiestrogenic properties primarily targeting estrogen receptor alpha (ERα). It acts as a pure antagonist on ERα, which is mainly expressed in the mammary gland and uterus and upregulated in estrogen-dependent tumors such as breast cancer. By blocking ERα, TAS-108 inhibits the binding and effects of estrogen, leading to suppression of estrogen-dependent cancer cell proliferation. Additionally, TAS-108 functions as a partial agonist on estrogen receptor beta (ERβ), which is expressed in various tissues including the central nervous system, urogenital tract, bone, and cardiovascular system; this partial agonism may exert beneficial effects on these tissues. TAS-108 also activates the co-repressor Silencing Mediator for Retinoid and Thyroid hormone receptor (SMRT), which inhibits activities of estrogen receptors contributing to its antitumor activity. The drug has been investigated primarily for treatment of hormone-responsive breast cancer including cases resistant to tamoxifen[1][2][3][5].

Other names

TAS-108 citrateTAS108 citrateTAS 108 citrate