Journal Article PET probe detecting non-small cell lung cancer susceptible to epidermal growth factor receptor tyrosine kinase inhibitor therapy

Makino, Akira  ,  Miyazaki, Anna  ,  Tomoike, Ayaka  ,  Kimura, Hiroyuki  ,  Arimitsu, Kenji  ,  Hirata, Masahiko  ,  Ohmomo, Yoshiro  ,  Nishii, Ryuichi  ,  Okazawa, Hidehiko  ,  Kiyono, Yasushi  ,  Ono, Masahiro  ,  Saji, Hideo

26 ( 8 )  , pp.1609 - 1613 , 2018-02 , ELSEVIER
AbstractTyrosine kinase inhibitors for epidermal growth factor receptor (EGFR-TKIs) are used as molecular targeted therapy for non-small cell lung cancer (NSCLC) patients. The therapy is applied to the patients having EGFR-primary L858R mutation, but drug tolerance caused by EGFR-secondary mutation is occurred within one and half years. For the non-invasive detection of the EGFR-TKIs treatment positive patients by positron emission tomograpy (PET) imagaing, fluorine-18 labeled thienopyrimidine derivative, [18F]FTP2 was newly synthesized. EGFR inhibition assay, cell uptake study, and blocking study indicated [18F]FTP2 binds with high and selective affinity for EGFR with L858R mutation, and not with L858R/T790M dual mutations. On animal PET study using tumor bearing mice, H3255 cells expressing L858R mutated EGFR was more clearly visualized than H1975 cells expressing L858R/T790M dual mutated EGFR. [18F]FTP2 has potential for detecting NSCLC which is susceptible to EGFR-TKI treatment.

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