One-step radiosynthesis of18F-IRS: A novel radiotracer targeting mutant EGFR in NSCLC for PET/CT imaging.
EGFR (epidermal growth factor receptor) targeted therapy has shown great success in clinical comparing with chemotherapy in EGFR mutation NSCLCs. Such as, gefitinib, first generation EGFR TKI, has obviously prolonged the FPS (progression free survival) of the subgroup of patients, but to those who did not get a certain mutation in EGFR kinase domain, the outcome is poor. In view of this situation, scientists have synthesized many radiotracers for selecting the right people by PET/CT imaging to NSCLC TKI therapy. In this study, we developed a novel PET radiotracer18F-IRS in one-step with a radio yield 20% (non-corrected), radiochemistry>98.5%, specific activity>105GBq/μmol, the pharmacokinetics and capacity of the tracer binding to mutant EGFR were evaluated both in vitro and in vivo.
TOF-PET/CT/MR Center, The Fourth Hospital of Harbin Medical University, China; Molecular Imaging Research Center, Harbin Medical University, China.
Zunyu
Z
Xiao
TOF-PET/CT/MR Center, The Fourth Hospital of Harbin Medical University, China; Molecular Imaging Research Center, Harbin Medical University, China.
Yan
Y
Song
TOF-PET/CT/MR Center, The Fourth Hospital of Harbin Medical University, China; Molecular Imaging Research Center, Harbin Medical University, China.
Kai
K
Wang
TOF-PET/CT/MR Center, The Fourth Hospital of Harbin Medical University, China; Molecular Imaging Research Center, Harbin Medical University, China. Electronic address: sunxilin@aliyun.com.
Xilin
X
Sun
TOF-PET/CT/MR Center, The Fourth Hospital of Harbin Medical University, China; Molecular Imaging Research Center, Harbin Medical University, China. Electronic address: shenbzh@vip.sina.com.
Baozhong
B
Shen
D000818:Animals; D002289:Carcinoma, Non-Small-Cell Lung / Q000000981:diagnostic imaging* / Q000473:pathology; D045744:Cell Line, Tumor; D004305:Dose-Response Relationship, Drug; D066246:ErbB Receptors / Q000235:genetics* / Q000378:metabolism; D006801:Humans; D051379:Mice; D015394:Molecular Structure; D000072078:Positron Emission Tomography Computed Tomography; D011799:Quinazolines / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D011849:Radioactive Tracers; D013329:Structure-Activity Relationship; D014018:Tissue Distribution
D011799:Quinazolines; D011849:Radioactive Tracers; D066246:ErbB Receptors
(18)F-IRS; EGFR; Imaging; PET/CT; TKIs