Definition

An antibody-drug conjugate (ADC) comprised of a monoclonal antibody against human tissue factor (TF) conjugated via a linker to an auristatin payload, with potential antineoplastic activity. Upon administration of anti-TF ADC XB002, the anti-TF antibody moiety binds to cell surface TF and is internalized. After internalization of the agent, the auristatin moiety is released. It then binds to tubulin and inhibits its polymerization, which results in G2/M phase arrest and induces apoptosis of TF-expressing tumor cells. TF, a transmembrane protein and an initiator of the coagulation cascade, is overexpressed in many tumor cells and tumor-resident endothelial cells. Expression of TF is correlated with metastasis, angiogenesis, tumor cell growth and tumor-associated thrombosis. The anti-TF antibody in XB002 does not affect coagulation.