Background: The 'targeted therapy' has been defined as an innovative therapy designed to interfere with molecular targets playing a critical role in tumour growth or progression. The epidermal growth factor receptor (EGFR) is a tyrosine kinase receptor mediating the effect of growth factors both in physiological and pathological conditions; aberrations in the EGFR may result in the development of a tumour phenotype. Objective: To summarise the current state of the development of anti-EGFR drugs. Methods: Patent literature and preclinical/clinical studies about EGFR inhibitors are analysed. Conclusion: Some monoclonal antibodies and small-molecule tyrosine kinase inhibitors have been approved in several countries for the treatment of various human cancer types; moreover, more than ten EGFR-targeting agents are actually in advanced clinical development.
