Objective: To highlight the potential role of pharmacists in facilitating use of everolimus in breast cancer and increase practitioner knowledge of everolimus therapy to enhance patient outcomes. Data Sources: A PubMed (1966 to May 2013) search included the terms everolimus, breast cancer, adverse events (AEs), pharmacist, and pharmacy. Abstracts presented at the American Society of Clinical Oncology 2012 Annual Meeting were also reviewed. Study Selection and Data Extraction: Articles published in English and directly related to everolimus clinical trials in breast cancer and other cancers were included, as were general pharmacy practice articles. Data Synthesis: Phase 3 clinical trials are currently exploring the efficacy of everolimus in combination therapy for breast cancer and the pharmacotherapeutical implications of the drug’s mechanism of action in relation to the PI3K/Akt pathway. Everolimus treatment–related topics relevant for pharmacists include drug administration, AE profile, potential drug interactions, dose adjustments, and comorbidity management. This comprehensive literature review of all components of everolimus treatment reveals the complexity of this treatment approach and the need for increased pharmacist involvement. Conclusions: Research based on the current treatment landscape and health care delivery system shows that pharmacists can greatly enhance patient care by providing teaching as part of a comprehensive cancer treatment approach. Because of their advanced knowledge of pharmacotherapy, pharmacists can directly support safe and effective use of everolimus while promoting optimal patient outcomes through a multidisciplinary approach that addresses comorbid conditions; they can also provide effective counseling and patient teaching in an ever-changing health care delivery system.