This review aims to present the preclinical and clinical data regarding efficacy and safety of
lapatinib alone and in combination with other agents in the treatment of human
epidermal growth factor receptor-2 (HER2)-overexpressing
breast cancer.
BACKGROUND: METHODS AND RESULTS: Preclinical and clinical trials of
lapatinib have shown that it is effective in the treatment on HER2+
breast cancer. More important, studies show that it is effective in the setting of
trastuzumab resistance and in the treatment of central nervous system
metastases, both of which are current treatment challenges. Furthermore,
lapatinib is effective in conjunction with
trastuzumab in the treatment of early
breast cancer. Data regarding the safety of
lapatinib show that it is generally well tolerated; however, multiple studies have shown significant (grade 3 and 4)
diarrhea and
rash associated with
lapatinib, thereby limiting its use. Carditoxicity has not been a significant adverse event associated with the use of
lapatinib.
CONCLUSION: