SS1020

SS1020 is a novel triphenylethylene selective estrogen receptor modulator (SERM) and selective estrogen receptor degrader (SERD) developed by Stony Brook University and Meijo University. Designed as a safer alternative to tamoxifen, SS1020 incorporates a chlorine atom to diminish genotoxicity and an acrylate side-chain to reduce endometrial activity. In preclinical models, SS1020 demonstrated potent anti-breast cancer activity against human MCF-7 breast cancer xenografts and DMBA-induced mammary tumors in rats, with efficacy superior to tamoxifen and raloxifene. Crucially, SS1020 lacks the genotoxic and estrogenic actions associated with tamoxifen, showing no detectable uterotrophic activity or hepatic DNA adduct formation in rats, and exhibits significantly higher oral bioavailability than raloxifene.

Other names

2E-3-{4-[(E)-4-chloro-1-(4-hydroxyphenyl)-2-phenylbut-1-enyl]-phenyl} acrylic acidE-3-{4-[(E)-4-chloro-1-(4-hydroxyphenyl)-2-phenylbut-1-enyl]-phenyl} acrylic acid