gw 2016

Lapatinib (GW572016) is an inhibitor of ErbB2 and EGFR (IC50=9.2 10.8 nM) with oral activity. Lapatinib has antitumor activity and can be used to treat advanced or metastatic breast cancer with HER2 overexpression.

Lapatinib tosylate (GW572016), a robust and orally administered inhibitor specifically targeting the tyrosine kinase domains of ErbB-2 and EGFR, exhibits inhibitory concentration 50 (IC50) values of 10.2 nM and 9.8 nM against purified EGFR and ErbB-2, respectively.