Due to its selectivity for ERβ, WAY-200070 is inactive in various assays of classic estrogen action, such as uterotrophic and osteopenia.[1] Moreover, WAY-200070 does not affect luteinizing hormone or follicle-stimulating hormone or inhibit ovulation, indicating that it does not suppress the hypothalamic-pituitary-gonadal axis, and as ERα and not ERβ is implicated in breast development, would not be expected to cause growth of the breasts at doses that are selective for activation of ERβ.[4] In fact, ERβ activation may actually suppress breast growth,[4] and in accordance with this, WAY-200070 was shown to augment the efficacy of tamoxifen in in vitro models of breast cancer.[5] As such, WAY-200070 and other selective ERβ agonists might prove to be safe and tolerable for medical use in both premenopausal and postmenopausal women and in individuals of either sex.
^ abcdMalamas MS, Manas ES, McDevitt RE, Gunawan I, Xu ZB, Collini MD, Miller CP, Dinh T, Henderson RA, Keith JC, Harris HA (2004). "Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands". J. Med. Chem. 47 (21): 5021–40. doi:10.1021/jm049719y. PMID15456246.
^ abcHughes ZA, Liu F, Platt BJ, Dwyer JM, Pulicicchio CM, Zhang G, Schechter LE, Rosenzweig-Lipson S, Day M (2008). "WAY-200070, a selective agonist of estrogen receptor beta as a potential novel anxiolytic/antidepressant agent". Neuropharmacology. 54 (7): 1136–42. doi:10.1016/j.neuropharm.2008.03.004. PMID18423777. S2CID30469397.
^Lattrich C, Schüler S, Häring J, Skrzypczak M, Ortmann O, Treeck O (2014). "Effects of a combined treatment with tamoxifen and estrogen receptor β agonists on human breast cancer cell lines". Arch. Gynecol. Obstet. 289 (1): 163–71. doi:10.1007/s00404-013-2977-7. PMID23907354. S2CID35636541.
