Notiretatug Rezetecan

**Semantic type:** Pharmacologic Substance

**Definition:** An antibody-drug conjugate (ADC) composed of notiretatug, an immunoglobulin G1 (IgG1) monoclonal antibody directed against the tumor-associated antigen (TAA) nectin-4 (PVRL4) conjugated, via a cleavable linker, to rezetecan, a derivative of the topoisomerase-1 inhibitor exatecan, with potential antineoplastic activity. Upon intravenous administration of notiretatug rezetecan, the notiretatug moiety targets and binds to nectin-4 expressed on tumor cells. Upon binding, internalization and linker cleavage, topoisomerase-1 inhibitor is released and inhibits DNA topoisomerase I activity, thereby inhibiting DNA replication and resulting in cell cycle arrest and apoptosis in tumor cells expressing nectin-4. Nectin-4 is overexpressed in a variety of cancers, but has a restricted distribution in normal tissue.

**Synonyms:** - ADC SHR-A2102 - Anti-nectin-4 ADC SHR-A2102 - Anti-nectin-4 Antibody-drug Conjugate SHR-A2102 - NOTIRETATUG REZETECAN - SHR A2102 - SHR-A2102 - SHRA2102