NCIt definition : An orally available, 6,7-disubstituted-4-anilinoquinoline-3-carbonitrile irreversible
inhibitor of the HER-2 receptor tyrosine kinase with potential antineoplastic activity.
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. Treatment of cells with this agent results in inhibition of downstream
signal transduction events and cell cycle regulatory pathways; arrest at the G1-S
(Gap 1/DNA synthesis)-phase transition of the cell division cycle; and ultimately
decreased cellular proliferation. Neratinib also inhibits the epidermal growth factor
receptor (EGFR) kinase and the proliferation of EGFR-dependent cells.;