RGN6024

RGN6024 is an orally bioavailable, brain-penetrant small-molecule tubulin destabilizer being developed by Reglagene for the treatment of high-grade gliomas such as glioblastoma and brain metastases from systemic cancers. It selectively binds the colchicine-binding site on β-tubulin, inhibits microtubule polymerization, and induces G2–M cell-cycle arrest, leading to apoptotic death of tumor cells, including temozolomide-resistant glioblastoma models.[1][3][6][11] Preclinical studies in mice and rats show low nanomolar in vitro potency, excellent blood–brain barrier penetration with high brain drug concentrations, robust antitumor activity and survival benefit in xenograft and orthotopic glioblastoma models, and a favorable safety profile, which has supported FDA orphan drug designation for glioblastoma and advancement toward first-in-human clinical trials.[2][3][5][6][9][10]