Gefitinib (Iressa) blocks phosphorylation of the intracellular portion of the tyrosine kinase domain, stopping signals that lead to breast cancer proliferation, prevention of apoptosis (programmed cell death), secretion of growth factors and decreased sensitivity to chemotherapy and hormonal therapies. In two Phase II trials among women with advanced disease, oral gefitinib at 500 mg/day demonstrated antitumor activity.
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