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Biologieal

Neratinib is an orally available, irreversible tyrosine kinase inhibitor with IC50 of 59 nM and 92 nM for HER2 and EGFR, respectively.^[1] Neratinib binds to the HER-2 receptor irreversibly, thereby reducing autophosphorylation in cells, apparently by targeting a cysteine residue in the ATP-binding pocket of the receptor. Neratinib also inhibits the epidermal growth factor receptor (EGFR) kinase and the proliferation of EGFR-dependent cells.^[2]

Reference

[1] Tsou HR et al. J Med Chem. 2005 Feb 24;48(4):1107-31.