The better understanding of the biology of breast cancer has allowed the identification of new targets for anticancer therapy. Trastuzumab, a monoclonal antibody binding the HER2 receptor, is used since several years in the treatment of HER2 overexpressing breast cancer, including in the adjuvant setting. Lapatinib, a tyrosine kinase inhibitor, was introduced more recently into the clinic. New treatment options under evaluation in HER2 overexpressing breast cancer include combinations of anti-HER2 treatments, drugs targeting the downstream signaling pathway and new anti-HER2 agents such as pertuzumab and T-DM1. This article also reviews other targeted treatments of interest in the field of breast cancer including antiangiogenic agents and drugs targeting the PI3K-AKT-mTOR pathway.