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|EAI045 is an allosteric, non-ATP competitive inhibitor of mutant EGFR. In vitro studies proved that EAI045 is active and selective for T790M- harboring EGFR mutants that are in a monomer state. In vivo the combination of EAI045 and cetuximab caused a marked tumor shrinkage in a mouse model carrying the EGFR mutant with L858R/T790M/C797S. Therefore, EAI045 is the first allosteric inhibitor that targets T790M and C797S EGFR mutants but it is effective only in combination with cetuximab.
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