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(.pdf) dr.ssa Antonella Ferro - Progettoeventi

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Lapatinib<br />

• Binds to intracellular ATP binding site of<br />

EGFR (ErbB-1) and HER2 (ErbB-2)<br />

preventing phosphorylation and activation<br />

• Blocks downstream signaling through<br />

homodimers and heterodimers of EGFR<br />

(ErbB-1) and HER2 (ErbB-2)<br />

• Dual blockade of signaling may be more<br />

effective than the single-target inhibition<br />

provided by agents such as trastuzumab<br />

Lapatinib<br />

1+1 2+2 1+2<br />

Downstream signaling<br />

cascade<br />

Rusnak et al. Mol Cancer Ther 2001;1:85-94; Xia et al. Oncogene 2002;21:6255-6263;<br />

Konecny et al. Cancer Res. 2006;66:1630-1639

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