Anti-EGFR/Top1i ADC ALX2004

**Semantic type:** Pharmacologic Substance

**Definition:** An antibody-drug conjugate (ADC) composed of a Fc-mediated monoclonal antibody directed against the tumor-associated antigen (TAA) epidermal growth factor receptor (EGFR) conjugated, via a cleavable linker, to a topoisomerase I inhibitor (TOP1i), with potential antineoplastic activity. Upon administration of anti-EGFR/TOP1i ADC ALX2004, the anti-EGFR monoclonal antibody moiety targets and binds to EGFR expressed on tumor cells, which inhibits EGFR-mediated signaling. Upon binding and linker cleavage, the TOP1i moiety inhibits DNA topoisomerase I activity, thereby inhibiting DNA replication which results in cell cycle arrest and tumor cell apoptosis. This inhibits the proliferation of EGFR-expressing tumor cells. ALX2004 also induces a bystander killing effect, induces immunogenic cell death (ICD) ,and induces antibody-dependent cellular cytotoxicity (ADCC) and antibody-dependent cellular phagocytosis (ADCP). EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.

**Synonyms:** - ADC ALX2004 - ALX 2004 - ALX-2004 - ALX2004 - Anti-EGFR ADC ALX2004 - Anti-EGFR Antibody-drug Conjugate ALX2004