Learning Objectives After completing this course, the reader will be able to: Identify the available systemic therapies for metastatic breast cancer patients. Define the role of taxanes and targeted therapies in metastatic breast cancer patients. Discuss the most useful endocrine therapy in patients with metastatic breast cancer. Access and take the CME test online and receive 1 AMA PRA Category 1 Credit™ at CME.TheOncologist.com Over the last decades, the introduction of several new agents into clinical practices, albeit rare, survival benefits in metastatic breast cancer (MBC). Despite these results, the choice of treatment for the majority of patients is still empirically based, since the only two predictive factors with level 1 evidence for clinical use are hormonal receptor status for endocrine therapy and HER‐2 status for trastuzumab therapy. Important improvements in the endocrine therapy of both pre‐ and postmenopausal women with hormone‐responsive disease have been achieved. For premenopausal women, ovarian function suppression with luteinizing hormone‐releasing hormone analogs combined with tamoxifen has become the standard treatment, although aromatase inhibitors plus ovarian function suppression are under evaluation. In postmenopausal patients, aromatase inhibitors have proved to be superior to standard endocrine therapies in either first‐ or second‐line treatment and a novel antiestrogen compound, fulvestrant, has been introduced in clinical practice. Chemotherapy remains the treatment of choice for hormone unresponsive or resistant patients. Anthracyclines and taxanes have been used either alone or in combination as first‐line chemotherapy, but with the more frequent use of these agents in the adjuvant setting, new standards are needed for first‐line chemotherapy, and new and more efficacious treatments are required. In the subgroup of patients with tumors that overexpress HER‐2, the use of trastuzumab alone or in combination with chemotherapy has modified the natural history of these tumors, even if only about one out of two patients obtains a clinical response. In this review we summarize the main achievements and the currently available treatment options for patients with MBC. Disclosure of potential conflicts of interest is found at the end of this article.