Lapatinib

摘要

Lapatinib inhibits tyrosine phosphorylation of both epidermal growth factor receptor and human epidermal receptor (HER) 2, thus preventing receptor activation.Preliminary evidence suggests that clinical response to lapatinib may be linked to the extent of baseline HER2 gene expression. In a randomised, open-label, phase III trial, the median time to progression was significantly longer with lapatinib in combination with capecitabine than with capecitabine monotherapy (6.2 vs 4.3 months) in patients with locally advanced or meta-static HER2-positive breast cancer who were refractory to previous therapy.The overall response rate was also significantly higher in patients receiving lapatinib plus capecitabine than in those receiving capecitabine alone.A Most adverse events in this trial were mild to moderate in severity and of a similar nature to those seen with capecitabine monotherapy