Dacomitinib Case

Satisfactory Essays

IC50: 6, 45.7, and 73.7 nM for EGFR, Her2 and her4, respectively

Dacomitinib (PF299804, PF299) is an irreversible Pan-ERBB Inhibitor.

The epidermal growth factor receptor (EGFR) is the cell-surface receptor for extracellular protein ligands. EGFR family has four closely related receptor tyrosine kinases: EGFR (ErbB-1), HER2/c-neu, Her 3 and Her 4. Mutations affecting EGFR expression or activity could lead to cancer.

In vitro: Dacomitinib could reduce the phosphorylation of EGFR, HER2, and HER4 in various sensitive cancer cell lines through a combined G0–G1 arrest and an induction of apoptosis. In addition, dacomitinib inhibited growth in several HER2-amplified lines with resistance to trastuzumab. Moreover, dacomitinib
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