Anti-VEGF Antibody-drug Conjugate YL242

**Semantic type:** Pharmacologic Substance

**Definition:** An antibody-drug conjugate (ADC) composed of a monoclonal antibody directed against the human vascular endothelial growth factor (VEGF) conjugated, via a protease-cleavable tripeptide linker, to the camptothecin-based topoisomerase-1 inhibitor (TOP1i) C24, with potential anti-angiogenic and antineoplastic activities. Upon administration of anti-VEGF ADC YL242, the anti-VEGF antibody moiety targets and binds to VEGF-expressing tumor cells. Upon binding and linker cleavage, C24 is released, and inhibits DNA topoisomerase-1 activity, thereby inhibiting DNA replication and resulting in cell cycle arrest and tumor cell apoptosis. This inhibits the proliferation of VEGF-expressing tumor cells. In addition, the binding of YL242 to VEGF prevents the binding of VEGF to its receptor VEGFR and abrogates VEGF/VEGFR-mediated signaling, which may lead to the inhibition of vascular endothelial cell proliferation. The inhibition of tumor angiogenesis may further decrease tumor cell proliferation and prevent metastasis. VEGF is overexpressed in a variety of cancers and is associated with increased invasiveness and decreased survival.

**Synonyms:** - Anti-VEGF ADC YL242 - Anti-VEGF/C24 ADC YL242 - Anti-VEGF/TOP1i ADC YL242 - YL 242 - YL-242 - YL242