Current Knowledge and Future Directions of the Selective Epidermal Growth Factor Receptor Inhibitors Erlotinib (Tarceva®) and Gefitinib (Iressa®)

Oncologist - Tập 10 Số 8 - Trang 579-589 - 2005
Wandena S. Siegel-Lakhai1,2, Jos H. Beijnen3,1,2, Jan H.M. Schellens3,1,2
1Slotervaant Hospital, Amsterdam, The Netherlands
2The Netherlands Cancer Institute, Antoni van Leeuwenhoek Hospital, Amsterdam, The Netherlands
3Faculty of Pharmaceutical Sciences, Division of Drug Toxicology, Utrecht University, Utrecht, The Netherlands

Tóm tắt

AbstractThe CME activity for this article is forthcoming.Access and take the CME test online and receive 1 hour of AMA PRA category 1 credit at CME.TheOncologist.comGefitinib (Iressa®; AstraZeneca Pharmaceuticals, Wilmington, DE, http://www.astrazeneca-us.com) and erlotinib (Tarceva®; OSI Pharmaceuticals, Inc., Melville, NY, http://www.osip.com) are so-called small molecules that selectively inhibit epidermal growth factor receptor (EGFR) tyrosine kinase activity. Both drugs received registration approval by the U.S. Food and Drug Administration (FDA) for the second- and third-line treatment of non-small cell lung cancer (NSCLC), but the failure of gefitinib to show a survival advantage over placebo has resulted in a discussion about the registration of gefitinib. Recently published results have revealed that mutations in the tyrosine kinase domain of EGFR are strongly associated with increased gefitinib and erlotinib sensitivity in patients with advanced NSCLC. Here, we present the current knowledge and the future directions of the EGFR tyrosine kinase inhibitors gefitinib and erlotinib.

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