bromo-ormeloxifene

Bromo-ormeloxifene (Br-ORM) is a novel brominated analogue of ormeloxifene, a non-steroidal selective estrogen receptor modulator (SERM). It is being investigated as a targeted therapy for cervical cancer. Br-ORM inhibits the epithelial-mesenchymal transition (EMT) by targeting the β-catenin signaling pathway. Mechanistically, it binds to the active site of β-catenin, preventing its translocation into the nucleus and subsequently repressing β-catenin/TCF-4 transcriptional activity. This leads to the downregulation of EMT-associated proteins such as N-cadherin, slug, snail, and matrix metalloproteinases (MMP2 and MMP3). Furthermore, Br-ORM treatment restores the expression of miR-200a, a microRNA that directly targets β-catenin. In preclinical studies, Br-ORM has demonstrated potent anti-proliferative, anti-invasive, and pro-apoptotic effects in cervical cancer cell lines and has shown significant tumor regression in orthotopic xenograft mouse models.

Other names

bromo-ormeloxifene