Lapatinib, an orally available dual inhibitor targeting the tyrosine-kinase domain of both epidermal growth factor receptor-1 and 2, has been introduced for the treatment of advanced/metastatic HER2+ breast cancer in combination with capacitabine after chemotherapy regimens containing anthracycline, taxanes and trastuzumab. Moreover, lapatinib is under investigation in combination with anthracycline and taxanes in neoadjuvant and adjuvant settings. Another potential field of investigation for this drug is related to its ability to restore hormonal sensitivity of HER2-, hormone-receptor positive breast cancer cells. This paper reviews the current use of lapatinib in breast cancer and its future perspectives.
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