Lasofoxifene — Investigational Agent
Other · Phase 3 · Sermonix Pharmaceuticals
Mechanism of Action
Lasofoxifene is a third-generation oral selective estrogen receptor modulator (SERM) with tissue-selective activity — ER antagonist in breast tissue with favorable bone and endometrial effects. It retains potent antagonist activity against ESR1 ligand-binding-domain mutations (e.g., Y537S, D538G) that drive endocrine resistance, and preclinically also reduces metastatic seeding, supporting its repositioning for ESR1-mutant metastatic breast cancer.
Investigational Indications
- ER+/HER2- advanced or metastatic breast cancer with an ESR1 mutation