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HKI-272
An orally available, 6,7-disubstituted-4-anilinoquinoline-3-carbonitrile, irreversible inhibitor of the HER-2 receptor tyrosine kinase with potential antineoplastic activity. HKI-272 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. HKI-272 also inhibits the epidermal growth factor receptor (EGFR) kinase and the proliferation of EGFR-dependent cells. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)
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