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Identifying nonsmall‐cell lung tumours bearing the T790M EGFR TKI resistance mutation using PET imaging
Author(s) -
Goggi Julian L.,
Haslop Anna,
Ramasamy Boominathan,
Cheng Peter,
Jiang Lingfan,
Soh Vanessa,
Robins Edward G.
Publication year - 2019
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3771
Subject(s) - t790m , cancer research , mutation , tyrosine kinase inhibitor , in vivo , tyrosine kinase , lung cancer , chemistry , in vitro , epidermal growth factor receptor , biodistribution , cancer , oncology , medicine , gefitinib , signal transduction , biology , biochemistry , gene , genetics
Specific mutations significantly affect response to epidermal growth factor tyrosine kinase inhibitor (EGFR‐TKI) treatment in lung cancer patients. Identifying patients with these mutations remains a major clinical challenge. EGFR T790M mutation, which conveys resistance to in the present study, [ 18 F]FEWZ was assessed in vitro to determine efficacy relative to the starting compound and in vivo to measure the biodistribution and specificity of binding to EGFR wild‐type, L858R and T790M bearing tumours. [ 18 F]FEWZ is the first evidence of a radiolabeled third generation anilinopyrimidine‐derived tyrosine kinase inhibitor targeting T790M mutation bearing tumours in vivo.

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