GW-572016（Lapatinib Ditosylate；GW2016 tosylat；Tykerb ditosylate；二苯磺酸拉帕替尼；二甲苯磺酸拉帕替尼；二对甲苯磺酸拉帕替尼；甲苯磺酸拉帕替尼）是一种有效的具有口服活性的EGFR/ErbB2抑制剂，其IC₅₀值分别为10.8 nM和9.2 nM。Lapatinib Ditosylate可抑制EGF刺激的Erk1/2和AKT的磷酸化，抑制肿瘤生长。 

参考文献

[1] Rusnak DW, et al. The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther 2001, 1(2):85-94.

[2] Xia W, et al. Anti-tumor activity of GW572016: a dual tyrosine kinase inhibitor blocks EGF activation of EGFR/erbB2 and downstream Erk1/2 and AKT pathways. Oncogene 2002, 21(41):6255-6263.

[3] Konecny GE, et al. Activity of the dual kinase inhibitor lapatinib (GW572016) against HER-2-overexpressing and trastuzumab-treated breast cancer cells. Cancer Res 2006, 66(3):1630-1639.

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