CDAC targeting EGFR mutant BG-60366

An orally bioavailable chimeric degradation activation compound (CDAC) targeting mutant epidermal growth factor receptor (EGFR) comprised of an E3 ubiquitin ligase ligand conjugated to an EGFR mutant-binding ligand, with potential antineoplastic activity. Upon oral administration, CDAC targeting EGFR mutant BG-60366 specifically targets and binds, with its mutant EGFR-targeting moiety, to mutant EGFR and the E3 ubiquitin ligase ligand moiety binds to E3 ubiquitin ligase. This catalyzes ubiquitination and proteasome-mediated degradation of mutant EGFR and prevents the activation of the EGFR-mediated signaling pathway. This leads to an inhibition of the growth of EGFR mutant-expressing tumor cells. EGFR is overexpressed or mutated in a variety of cancer cells.