Lapatinib (GW2016) is a potent inhibitor of the ErbB-2 and EGFR kinases at IC50 values of 10.2 and 9.8 nM. [1] In EGFR- and ErbB-2-overexpressing tumor cell lines such asA-431, HN5, BT474, N87, and CaLu-3, Lapatinib's growth inhbiition IC50 values were
Lapatinib treatment results in differential expression of genes associated with cell cycle regulation. These genes are mostly involved with the G1S phase transitions. [3]