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Gefitinib, the first of a new class of tyrosine kinase inhibitors, is the first drug approved by the US Food and Drug Administration (FDA) for the treatment of non-small cell lung cancer. The drug inhibits the epidermal growth factor receptor and is an inhibitor of the growth of tumors driven by it. Phase II studies have confirmed that gefitinib has significant single agent activity in patients with non-small cell lung cancer, particularly those with activating mutations of the EGFR gene. After a phase II study demonstrated that the drug had activity when administered in combination with carboplatin, a phase III trial established that gefitinib plus carboplatin was not only superior to placebo plus carboplatin but to any of the single agents in the control arm. Furthermore, gefitinib monotherapy produced a response rate (RR) of 51% in the first 16 weeks of treatment. Gefitinib has also shown activity in a subgroup of patients with lung cancer who have never smoked. The drug can be used as a single agent or in combination with a number of other chemotherapeutic agents, including paclitaxel. A number of studies have evaluated the use of gefitinib in combination with radiotherapy. The toxicity profile for the drug appears to be manageable. Two other EGFR inhibitors are in development: CI-1033 and AZD9291.The New York Times’ David Gruber has an excellent article in the paper about a 21-year-old Apple engineer, Amir Chetrit

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