Much effort has been expended in the search for inhibitors of signalling molecules that may prove to be important therapeutically in cancer. The epidermal growth factor receptor (EGFR) family and their associated ligands has been one such area extensively investigated. The complex nature of EGFR biology allows for potential opportunities for EGFR inhibitors in a number of areas of cancer therapy, including proliferative, angiogenic, invasive, and metastatic aspects. Much positive evidence of likely benefit has already been gathered from a multiplicity of laboratory experiments. Clinical trials are now urgently required to further evaluate the advantages of such agents.