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Inhibition of EGF receptor signalling: The Discovery of AZD9291

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If you have a question about this talk, please contact Claus Bendtsen.

Small molecule inhibitors of the Epidermal Growth Factor Receptor (EGFR) tyrosine kinase such as gefitinib and erlotinib have been employed successfully in the treatment of non-small cell lung cancer (NSCLC) patients harboring an activating/sensitising mutation in EGFR (“single mutant”, EGF Rm +). However, these drugs are not curative and most patients will progress due to acquired resistance, with up to two thirds of these patients progressing due to acquisition of a second EGFR T790M mutation. This presentation will describe the background disease biology, and some key aspects of the pre-clinical bioscience and medicinal chemistry programs that led to the discovery of AZD9291 , an orally bioavailable, irreversible EGFR inhibitor of both the resistance and sensitising mutations that also spares the wild type form of the receptor, inhibition of which is believed to drive the observed dose limiting toxicities (such as skin rash and diarrhea) for these first generation therapies in the clinic.

First dose in man was achieved with AZD9291 in March 2013 and clinical findings to date have been very exciting, and some current clinical data will also be shared.

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