2021
DOI: 10.3390/ph14030256
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A Radiobrominated Tyrosine Kinase Inhibitor for EGFR with L858R/T790M Mutations in Lung Carcinoma

Abstract: Activating double mutations L858R/T790M in the epidermal growth factor receptor (EGFR) region are often observed as the cause of resistance to tyrosine kinase inhibitors (TKIs). Third-generation EGFR-TKIs, such as osimertinib and rociletinib (CO-1686), was developed to target such resistance mutations. The detection of activating L858R/T790M mutations is necessary to select sensitive patients for therapy. Hence, we aimed to develop novel radiobromine-labeled CO-1686 as a positron emission tomography (PET) imag… Show more

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Cited by 8 publications
(8 citation statements)
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References 29 publications
(52 reference statements)
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“…As a result, [ 77 Br]­Br – is distributed to some organs, and its radioactivity is retained for a long time. 77 Br-labeled CO-1686, [ 77 Br]­BrCO1686, showed delayed blood clearance derived from its debromination . Meanwhile, in in vitro stability experiments in a buffered solution, approximately 15% of [ 125 I] 9 and [ 77 Br] 15 was decomposed to free iodine and free bromine after 24 h of incubation.…”
Section: Resultsmentioning
confidence: 99%
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“…As a result, [ 77 Br]­Br – is distributed to some organs, and its radioactivity is retained for a long time. 77 Br-labeled CO-1686, [ 77 Br]­BrCO1686, showed delayed blood clearance derived from its debromination . Meanwhile, in in vitro stability experiments in a buffered solution, approximately 15% of [ 125 I] 9 and [ 77 Br] 15 was decomposed to free iodine and free bromine after 24 h of incubation.…”
Section: Resultsmentioning
confidence: 99%
“…77 Br-labeled CO-1686, [ 77 Br]BrCO1686, showed delayed blood clearance derived from its debromination. 23 Meanwhile, in in vitro stability experiments in a buffered solution, approximately 15% of [ 125 I] 9 and [ 77 Br]15 was decomposed to free iodine and free bromine after 24 h of incubation. However, the in vivo deiodination and debromination of the tracers barely occurred as mentioned above.…”
Section: ■ Results and Discussionmentioning
confidence: 99%
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“…The H358, H2170, H3255 and H1975 cell lines were cultured with 5% CO 2 at 37 °C following the protocol of the American Type Culture Collection (ATCC). The H2170 and H358 cell lines have EGFR wild-type status, while H1975 has two EGFR tyrosine kinase domain mutations—L858R and T790M [ 26 , 27 ]. H3255 has a single EGFR tyrosine kinase domain mutation-L858R [ 27 , 28 ].…”
Section: Methodsmentioning
confidence: 99%
“…However, the radiotracers employed in the imaging of double mutations of EGFR T790M/L858R, such as [ 11 C]osimertinib, [ 11 C]rociletinib, [ 125 I]ICO1686, [ 77 Br]BrCO1686, [ 125 I]I-osimertinib, and [ 77 Br]Br-osimertinib have some limitations, such as low accumulation in the targeted tumor, which results in insufficient tumor-to-blood ratios or tumor-to-nontarget tissue ratios. 11 - 13 , 15 …”
Section: Introductionmentioning
confidence: 99%