A bispecific transmembrane antibody simultaneously targeting intra- and extracellular epitopes of the epidermal growth factor receptor inhibits receptor activation and tumor cell growth.

Epidermal growth factor receptor (EGFR) plays an important role in essential cellular processes such as proliferation, survival and migration. Aberrant activation of EGFR is frequently found in human cancers of various origins and has been implicated in cancer pathogenesis. The therapeutic antibody cetuximab (Erbitux) inhibits tumor growth by binding to the extracellular domain of EGFR, thereby preventing ligand binding and receptor activation.

Therapeutic antibodies.

Monoclonal antibodies had the lure of drugs very much since their first description. The ability to bind to a predetermined chemical structure stimulated the imagination of drug discoverers and developers. Nevertheless it took many years before a drug was registered which started to make good on the promise.