1A3-monomethyl auristatin E

1A3-monomethyl auristatin E is an experimental antibody-drug conjugate (ADC) designed to target Amphiregulin (AREG), a ligand for the Epidermal Growth Factor Receptor (EGFR) that is frequently overexpressed in breast cancer and other malignancies. The ADC consists of the monoclonal antibody 1A3, which specifically recognizes the C-terminal transmembrane stalk of AREG that remains on the cell surface after its extracellular domain is proteolytically cleaved by TACE/ADAM17. Upon binding to this stalk, the ADC is rapidly internalized, delivering the cytotoxic payload monomethyl auristatin E (MMAE) into the cell. MMAE is a potent antimitotic agent that inhibits tubulin polymerization, leading to cell cycle arrest at the G2/M phase and subsequent apoptosis. This therapeutic strategy leverages the specific internalization of the AREG stalk to selectively eliminate cancer cells while minimizing off-target toxicity.

Other names

Anti-AREG ADC1A3-vcMMAE