Gefitinib is approved by the Food and Drug Administration (FDA) to treat locally advanced or metastatic non-small cell lung cancer (NSCLC) that has not gotten better after treatment with other chemotherapy. It is available only as part of a special program called the Iressa Access Program. Gefitinib is also being studied in the treatment of other types of cancer.
Gefitinib is an anilinoquinazoline with antineoplastic activity. Gefitinib inhibits the catalytic activity of numerous tyrosine kinases including the epidermal growth factor receptor (EGFR), which may result in inhibition of tyrosine kinase-dependent tumor growth. Specifically, this agent competes with the binding of ATP to the tyrosine kinase domain of EGFR, thereby inhibiting receptor autophosphorylation and resulting in inhibition of signal transduction. Gefitinib may also induce cell cycle arrest and inhibit angiogenesis.
Mutation of a gene involved in non-small cell lung cancer (NSCLC) increases the likelihood that the drug gefitinib (Iressa™) will show a beneficial response, researchers at the Dana-Farber Cancer Institute, the National Cancer Institute (NCI) - part of the National Institutes of Health - and two other institutions announced today in the online version of Science.