EGFR, highly expressed in a variety of human malignancies, is correlated with poor tumour differentiation, high tumour growth and metastatic rate. EGF and several other ligands, such as transforming growth factor-alpha, amphiregulin, heparin-binding EGF, and betacellulin, activate Ras/Raf mitogen-activated protein kinases (MAPKs) and phosphatidyl inositol 3'-kinase (PI3K)/Akt signalling pathways. Therefore, EGFR can regulate multiple processes, i.e., gene expression, cellular proliferation, angiogenesis, and inhibition of apoptosis, which contribute to the development of malignancy. In this review, we discuss the inhibition of EGFR by the specific tyrosine kinase inhibitor Iressa (ZD1839) focusing on its effects in prostate cancer.