Drug Overview
Iressa (gefitinib; AstraZeneca) is a selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase domain. The receptor is expressed on the cell surface of both normal and cancer cells, and plays an important role in cell growth and proliferation. EGFR-activating mutations such as exon 19 deletion (del19) or exon 21 point mutation L858R have previously been identified as contributing to the promotion of tumor cell growth and blocking apoptosis in non-small cell lung cancer. Iressa inhibits the kinase activity of del19 or exon 21 point mutation L858R mutations, preventing phosphorylation of tyrosine residues associated with the receptor, resulting in the inhibition of EGFR-dependent proliferation.
Iressa (gefitinib; AstraZeneca) is a selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase domain. The receptor is expressed on the cell surface of both normal and cancer cells, and plays an important role in cell growth and proliferation. EGFR-activating mutations such as exon 19 deletion (del19) or exon 21 point mutation L858R have previously been identified as contributing to the promotion of tumor cell growth and blocking apoptosis in non-small cell lung cancer. Iressa inhibits the kinase activity of del19 or exon 21 point mutation L858R mutations, preventing phosphorylation of tyrosine residues associated with the receptor, resulting in the inhibition of EGFR-dependent proliferation.
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