Scientific advances in molecular biology and understanding of oncogenesis have lead to anticancer molecular targeted therapies. They encompass monoclonal antibodies binding to active membrane epitopes and small molecules interfering with enzymatic reactions essential to cancer cell survival (oncogene addiction). These pathways may be optimal targets. Clinical benefits achieved using these targeted agents have been outstanding both in localized and metastatic disease.We conducted a survey of literature analyzing activity and safety of targeted agents approved by FDA and/or FDA for the treatment of patients with breast cancer: anti-HER2 and antiangiogenic agents.Activity and main toxicities of these targeted agents are described according to signaling pathway targeted as well as stage of breast cancer.Availability of these targeted therapies has indeed transformed the outcome of subgroups of breast cancer to the expense of acceptable and manageable side effects, as compared to classical cytotoxics to which they are nevertheless combined.