Amphiregulin, an EGF family growth factor, binds and activates the epidermal growth factor receptor (EGFR or ErbB1). Activation of the EGFR by amphiregulin can occur through autocrine, paracrine and juxtacrine mechanisms. Amphiregulin plays a role in several biological processes including nerve regeneration, blastocyst implantation, and bone formation. Amphiregulin also plays an important role in mammary duct formation as well as the outgrowth and branching of several other human tissues such as the lung, kidney and prostate. This effect is most likely due to the induction of genes involved in invasion and migration such as cytokines and matrix metalloproteases. Clinical studies have suggested that amphiregulin also plays a role in human breast cancer progression and its expression has been associated with aggressive disease. Therefore, amphiregulin may be a novel and effective target for the treatment of breast cancer and could represent an alternative to targeting the EGFR.