Anti-PTK7/Exatecan Antibody-drug Conjugate LY4175408

**Semantic type:** Pharmacologic Substance

**Definition:** An antibody-drug conjugate (ADC) composed of a fully human Fc-silenced immunoglobulin G1 (IgG1) monoclonal antibody directed against human inactive tyrosine-protein kinase 7 (protein tyrosine kinase 7; PTK7) conjugated, via a polysarcosine-based hydrophilic linker, to the cytotoxic agent and DNA topoisomerase I inhibitor exatecan, with potential antineoplastic activity. Upon administration of anti-PTK7/exatecan ADC LY4175408, the anti-PTK7 antibody moiety targets and binds to PTK7 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 PTK7. In addition, LY4175408 induces a bystander effect, thereby further killing PTK7-expressing tumor cells. PTK7, a tumor-associated antigen (TAA), is overexpressed on a variety of cancer cells with limited expression in normal tissues. It is an integral player in cancer cell stemness and tumor progression.

**Synonyms:** - Anti-PTK7 ADC LY4175408 - Anti-PTK7 Antibody-drug Conjugate LY4175408 - Anti-PTK7/Exatecan ADC LY4175408 - LY 4175408 - LY-4175408 - LY4175408