Trioxifene (mesylate)

Trioxifene mesylate (LY133314) is an orally active and selective estrogen receptor (ER) modulator with human ERα IC₅₀ of 203.49 nM and K_i of 20.84 nM. Trioxifene mesylate binds estradiol receptors, inhibits ERα-mediated gene expression, reduces circulating gonadotrophin levels. Trioxifene mesylate can be used for the research of advanced breast cancer and androgen-independent, metastatic prostatic adenocarcinoma^[1][2]. In Vitro:Trioxifene (0.3-10000 nM; 4 h) mesylate binds to purified human recombinant ERα with human ERα IC₅₀ of 203.49 nM and K_i of 20.84 nM^[2].
Trioxifene (0.1-10.0 μM; 24 h) mesylate weakly antagonizes ERα-mediated gene expression in PAIII rat prostatic adenocarcinoma cells but does not alter ERβ-mediated gene expression in these cells^[2].
Trioxifene (7 days) mesylate inhibits the proliferation of PAIII rat prostatic adenocarcinoma cells in vitro with an IC₅₀ of 4.6 μM^[2]. In Vivo:Trioxifene mesylate exhibits significant antitumor activity in DMBA (HY-W011845)-induced rat mammary carcinoma^[1].
Trioxifene (2.0-40.0 mg/kg; s.c.; daily; 28 days or continuously until death) mesylate significantly inhibits PAIII prostatic adenocarcinoma metastasis to lymph nodes and lungs, reduces male accessory sex organ weight, and extends mean survival to 64.44 days with continuous 40.0 mg/kg-day administration in male LW rats^[2].