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pp 1-35 | Cite as

Small Molecule Inhibitors of the Epidermal Growth Factor Receptor

  • M. Raymond V. Finlay
  • Richard A. Ward
Chapter
Part of the Topics in Medicinal Chemistry book series

Abstract

The epidermal growth factor receptor (EGFR) has emerged over the past two decades as a key target in therapeutic approaches to the treatment of non-small cell lung cancer (NSCLC). This chapter describes the evolution of the EGFR small molecule inhibitor field, from early exploratory work and growing insight into the role of EGFR activating mutations, through to the first approved therapies, gefitinib and erlotinib. Advances in understanding resistance to these initial therapies and the role of the T790M mutation are discussed, along with drug discovery efforts culminating in the discovery of a number of EGFR mutant selective inhibitors, including osimertinib (TAGRISSOTM), the first approved treatment for patients with EGFR T790M mutation-positive metastatic NSCLC.

Keywords

Irreversible inhibitor Kinase Mutant Resistance T790M 

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Copyright information

© Springer International Publishing AG 2017

Authors and Affiliations

  1. 1.IMED OncologyAstraZenecaCambridgeUK

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