Breast cancer management has become increasingly complex, requiring the integration of data not only from the patient's history and imaging modalities but also from specific tumor biomarkers and gene expression. Targeted and biologic therapies in breast cancer continue to evolve rapidly. The field of molecular targeted therapy has emerged. Its ultimate goal is to personalize and simplify treatment as well as minimize toxicity. This review aims at highlighting the current state-of-the-art in novel molecular targeted therapies for breast cancer based on multi-targeted small molecule tyrosine kinase inhibitors (TKI). The first two agents in this group entering clinic, Lapatinib (GW572016; Tykerb®) and SUNITINIB (SU11248; Sutent®) are discussed. This review article also includes relevant patents.