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Pharmacological Research 117 (2017) 406–415

Targeting EGFR T790M mutation in NSCLC:

From biology to evaluation and treatment

Osimertinib (AstraZeneca ) is a potent, irreversible EGFR tyrosine kinase inhibitor

that is selective for EGFR tyrosine kinase inhibitor–sensitizing mutations and the

T790M resistance mutation with an excellent therapeutic index because its activity

is poor towards the wild-type EGFR

Olmutinib (HM 61713)(Boehringer Ingelheim) is an irreversible tyrosine-kinase

inhibitor, selective for mutant EGFR. Its molecule structure contains a Michael

acceptor that covalently binds a cysteine residue near the kinase domain of mutant

EGFR