Anti-EGFR/c-Met Antibody-drug Conjugate GEN1286

**Semantic type:** Pharmacologic Substance

**Definition:** An antibody-drug conjugate (ADC) composed of a human bispecific immunoglobulin G1 (IgG1) antibody targeting both epidermal growth factor receptor (EGFR) and hepatocyte growth factor receptor (HGFR; c-Met) conjugated to sesutecan, a cleavable hydrophilic linker and camptothecin analog and topoisomerase 1 inhibitor exatecan-based linker-drug, with potential antineoplastic activity. Upon administration, anti-EGFR/c-Met ADC GEN1286 simultaneously targets and binds to both EGFR and c-Met expressed on cancer cells. Upon binding, internalization and linker cleavage, exatecan is released. Exatecan inhibits DNA topoisomerase I activity, thereby inhibiting DNA replication and resulting in DNA damage, cell cycle arrest and apoptosis in tumor cells overexpressing EGFR and c-Met. EGFR and c-Met, both upregulated or mutated in a variety of tumor cell types, play key roles in tumor cell proliferation.

**Synonyms:** - Anti-EGFR/Anti-c-Met Bispecific ADC GEN1286 - Anti-EGFR/c-Met ADC GEN1286 - Anti-EGFR/c-Met Antibody-Sesutecan Conjugate GEN1286 - Anti-EGFR/c-Met/Exatecan ADC GEN1286 - GEN 1286 - GEN-1286 - GEN1286 - PRO 1286 - PRO-1286 - PRO1286