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British Journal of Cancer (2004) 90, 566-572.
doi:10.1038/sj.bjc.6601550

Gefitinib ('Iressa', ZD1839) and new epidermal growth factor receptor inhibitors

G Blackledge1 and S Averbuch2

1AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK

2AstraZeneca, OW3-236, 1800 Concord Pike, PO Box 15437, Wilmington, DE 19850-5437, USA



Correspondence to: G Blackledge, E-mail: george.blackledge@astrazeneca.com

Received 30 June 2003; revised 10 November 2003; accepted 11 November 2003



The epidermal growth factor receptor (EGFR) is a promising target for cancer therapy and a number of EGFR-targeted agents have been developed. Those most advanced in development are the EGFR tyrosine kinase inhibitors gefitinib ('Iressa', ZD1839) and erlotinib ('Tarceva', OSI-774), and the monoclonal antibody cetuximab ('Erbitux', IMC-C225). This review provides a clinical overview of these agents, highlighting their antitumour activities in different tumour types. Epidermal growth factor receptor-targeted agents are generally well tolerated and are not typically associated with the severe adverse events often seen with cytotoxic chemotherapy. Gefitinib is the agent with the most extensive clinical experience, particularly in non-small-cell lung cancer (NSCLC). Recently, gefitinib became the first-approved EGFR-targeted agent, for use in patients with previously treated advanced NSCLC in Japan, the USA and other countries. Further studies are required to explore the full potential of these novel agents either as monotherapy or combination therapy.

Keywords: EGFR-targeting agents; gefitinib; erlotinib; cetuximab

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