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SUMMARY:Inhibition of EGF receptor signalling: The Discovery of AZD9291 - 
 Ray Finlay\, Darren Cross &amp\; Richard A Ward
DTSTART:20150226T163000Z
DTEND:20150226T180000Z
UID:TALK57905@talks.cam.ac.uk
CONTACT:Claus Bendtsen
DESCRIPTION:Small molecule inhibitors of the Epidermal Growth Factor Recep
 tor (EGFR) tyrosine kinase such as gefitinib and erlotinib have been emplo
 yed successfully in the treatment of non-small cell lung cancer (NSCLC) pa
 tients harboring an activating/sensitising mutation in EGFR (“single mut
 ant”\, EGFRm +). However\, these drugs are not curative and most patient
 s will progress due to acquired resistance\, with up to two thirds of thes
 e 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 progra
 ms that led to the discovery of AZD9291\, an orally bioavailable\, irrever
 sible EGFR inhibitor of both the resistance and sensitising mutations that
  also spares the wild type form of the receptor\, inhibition of which is b
 elieved to drive the observed dose limiting toxicities (such as skin rash 
 and diarrhea) for these first generation therapies in the clinic.\n\nFirst
  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 als
 o be shared.\n\nRegistration necessary: https://www.eventbrite.co.uk/event
 /15599859600
LOCATION:Building 310 on the Cambridge Science Park
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