Lapatinib is an oral small molecule dual tyrosine kinase inhibitor against epidermal growth factor receptor(EGFR) and HER-2/neu.Clinical trials showed that lapatinib is effective for patients with HER2-positive breast cancer.In recent years,the researches of lapatinib in other cancers are rmore and more.lapatinib is expected to become a potential,multi-tumors targeting therapy drugs.In this review,we summarize the interaction mechanisms,clinical studies,pharmacologic characteristics and clinical application of lapatinib.