MRX-5287

MRX-5287 is an orally bioavailable, direct small-molecule inhibitor of the Myc (c-Myc) oncoprotein, currently in IND-enabling development by MycRx for the treatment of various cancers. Myc is a transcription factor that is deregulated or overexpressed in over 70% of human cancers, driving cell proliferation, survival, and other hallmarks of cancer. Historically considered 'undruggable' due to its disordered structure and lack of a traditional ligand-binding pocket, MRX-5287 is designed to directly bind to Myc, disrupting the formation of the Myc-associated factor X (MAX) heterodimer and blocking its transcriptional activity. This direct inhibition shuts down the oncogenic transcriptional program, leading to potent anti-cancer activity and induction of apoptosis in Myc-driven tumors.