Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor.

doi:10.1021/jm500973a

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Article

Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor.

Journal of medicinal chemistry - 23 Oct 2014

Finlay M Raymond V, Anderton Mark, Ashton Susan, Ballard Peter, Bethel Paul A, Box Matthew R, Bradbury Robert H, Brown Simon J, Butterworth Sam, Campbell Andrew, Chorley Christopher, Colclough Nicola, Cross Darren A E, Currie Gordon S, Grist Matthew, Hassall Lorraine, Hill George B, James Daniel, James Michael, Kemmitt Paul, Klinowska Teresa, Lamont Gillian, Lamont Scott G, Martin Nathaniel, McFarland Heather L, Mellor Martine J, Orme Jonathon P, Perkins David, Perkins Paula, Richmond Graham, Smith Peter, Ward Richard A, Waring Michael J, Whittaker David, Wells Stuart, Wrigley Gail L

Abstract excerpt

Epidermal growth factor receptor (EGFR) inhibitors have been used clinically in the treatment of non-small-cell lung cancer (NSCLC) patients harboring sensitizing (or activating) mutations for a number of years. Despite encouraging clinical efficacy with these agents, in many patients resistance develops leading to disease progression. In most cases, this resistance is in the form of the T790M mutation. In...

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PMID: 25271963
DOI: 10.1021/jm500973a

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EGFR

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