Anti-PTK7/Exatecan Antibody-drug Conjugate DAY301

**Semantic type:** Pharmacologic Substance

**Definition:** An antibody-drug conjugate (ADC) composed of Ab13, an antibody directed against human inactive tyrosine-protein kinase 7 (protein tyrosine kinase 7; PTK7) conjugated, via the hydrophilic self-immolative moiety T1000, to the cytotoxic agent and DNA topoisomerase I inhibitor exatecan, with potential antineoplastic activity. Upon administration of anti-PTK7/exatecan ADC DAY301, the anti-PTK7 antibody Ab13 targets and binds to PTK7 expressed on tumor cells. Upon binding, internalization and 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, this may cause 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. The hydrophilic moiety T1000 is used to overcome the hydrophobicity of conjugated exatecan.

**Synonyms:** - Anti-PTK7 ADC DAY301 - Anti-PTK7 Antibody-drug Conjugate DAY301 - Anti-PTK7/Exatecan ADC DAY301 - DAY 301 - DAY-301 - DAY301 - MTX 13 - MTX-13 - MTX13