izalontamab brengitecan

A dual-targeted antibody-drug conjugate (ADC) consisting of a bispecific antibody directed against both the epidermal growth factor receptor (EGFR; HER1; ErbB1) and the epidermal growth factor receptor 3 (HER3; ErbB3) conjugated, via a cathepsin-B cleavable linker, to the camptothecin derivative and topoisomerase 1 inhibitor Ed-04, with potential antineoplastic activity. Upon administration of izalontamab brengitecan, the bispecific antibody moiety simultaneously targets and binds to EGFR and HER3 expressed on cancer cells. Upon binding and internalization, Ed-04 is released and inhibits DNA topoisomerase I activity, thereby inhibiting DNA replication and resulting in cell cycle arrest and apoptosis in tumor cells expressing EGFR and/or HER3. EGFR and HER3, both upregulated and/or mutated in a variety of tumor cell types, play key roles in tumor cell proliferation. Simultaneously targeting both EGFR and HER3 may enhance the anti-tumor activity of izalontamab brengitecan.