Definition

A proprietary antibody-drug conjugate (ADC) composed of a monoclonal antibody against human epidermal growth factor receptor 2 (HER2) site-specifically linked, via a protease cleavable linker, to an analog of dolastatin 10, Auristatin-0101, with potential antineoplastic activity. Upon administration, anti-HER2-vc0101 ADC PF-06804103 targets HER2 expressed on tumor cells. Upon binding, internalization and cleavage, Auristatin-0101 binds to tubulin and inhibits its polymerization, resulting in G2/M phase arrest and apoptosis of HER2-expressing tumor cells. HER2, a tumor-associated antigen (TAA), is overexpressed on a variety of cancer cells.