Targeted therapies, in cancer treatment, represent a new generation of drugs that interfere with specific molecular targets (typically proteins) having critical roles to play in tumour growth or progression. The principle of targeted therapy is certainly not new: tamoxifen, a hormonal agent targeted at the estrogen receptor, has been in use for more than 30 years. However, this principle has re-gained significant emphasis with the recent development of new biological agents, such as trastuzumab, which was first approved for the treatment of advanced breast cancer (BC) in 1998. Presently, there are at least three different targeted therapies with well documented activity in advanced BC and all three are now being studied in the adjuvant setting; trastuzumab and bevacizumab are monoclonal antibodies, and lapatinib is a dual inhibitor of HER-1 and HER-2. This paper will review the increasing role of molecular targeted therapies in BC, with a particular focus on those drugs currently being tested in early BC, as well as, on future perspectives.