Anti-HER3/Exatecan Antibody-drug Conjugate ENV-501

**Semantic type:** Pharmacologic Substance

**Definition:** An antibody-drug conjugate (ADC) composed of a humanized monoclonal antibody directed against human epidermal growth factor receptor 3 (HER3; ErbB3) conjugated, via a hydrophilic cleavable linker, to the cytotoxic agent and DNA topoisomerase I inhibitor exatecan, with potential antineoplastic activity. Upon administration of anti-HER3/exatecan ADC ENV-501, the anti-HER3 antibody moiety targets and binds to HER3 expressed on tumor cells. Upon binding, internalization and linker cleavage, exatecan is released and inhibits DNA topoisomerase I activity, thereby inhibiting DNA replication and resulting in DNA damage, cell cycle arrest and apoptosis in tumor cells overexpressing HER3. HER3, a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, is frequently overexpressed in tumors. The hydrophilic linker is used to overcome the hydrophobicity of conjugated exatecan.

**Synonyms:** - ADC ENV-501 - Anti-HER3 ADC ENV-501 - Anti-HER3/Exatecan ADC ENV-501 - ENV 501 - ENV-501 - ENV501 - HMBD 501 - HMBD-501 - HMBD501