BEA-17

BEA-17 is a preclinical, first-in-class small molecule allosteric modulator and targeted protein degrader (TPD) of the LSD1/coREST complex. Developed by Beactica Therapeutics, it is primarily being investigated for the treatment of glioblastoma, where it has shown synergistic effects with standard-of-care agents and HDAC inhibitors. Unlike traditional irreversible catalytic inhibitors of LSD1, BEA-17 binds to an allosteric site, inducing a reduction in nuclear LSD1 levels without directly inhibiting its enzymatic activity. This mechanism aims to address the non-enzymatic functions of LSD1 that contribute to cancer progression. BEA-17 has demonstrated good blood-brain barrier penetration and oral bioavailability in preclinical models.