ArticleEJNMMI research2015
Identifying erlotinib-sensitive non-small cell lung carcinoma tumors in mice using [(11)C]erlotinib PET.
Article in EJNMMI research, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT02717221 (An EGFR-TKIs Benefit Non-small Cell Lung Carcinoma Patients Identification Strategy and Treatment Response Using Molecular Imaging), which is not on this map. Cited by 16 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
An EGFR-TKIs Benefit Non-small Cell Lung Carcinoma Patients Identification Strategy and Treatment Response Using Molecular Imaging
Who cites it
16 citing papers in PubMed, 28 citations in OpenAlex.
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- The Development of Positron Emission Tomography Tracers for In Vivo Targeting the Kinase Domain of the Epidermal Growth Factor Receptor.Pharmaceuticals (Basel, Switzerland) · 2022Review
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- Molecular Targeting of Epidermal Growth Factor Receptor (EGFR) and Vascular Endothelial Growth Factor Receptor (VEGFR).Molecules (Basel, Switzerland) · 2021Review
- Development of a Fluorinated Analogue of Erlotinib for PET Imaging of EGFR Mutation-Positive NSCLC.Molecular imaging and biology · 2019Article
- Real-time molecular optical micro-imaging of EGFR mutations using a fluorescent erlotinib based tracer.BMC pulmonary medicine · 2019Article
- Comparison of fully-automated radiosyntheses of [EJNMMI radiopharmacy and chemistry · 2018Article
- [Current Status and Progress in Molecular Imaging of Non-small Cell Lung Cancer for Molecular Targeted EGFR-TKI Treatment Sensitivity and Treatment Tolerance Prediction].Zhongguo fei ai za zhi = Chinese journal of lung cancer · 2017Review
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- [Molecular Imaging in vivo Detection of EGFR Mutations in Non-small Cell Lung Cancer].Zhongguo fei ai za zhi = Chinese journal of lung cancer · 2017Review
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- A multi species evaluation of the radiation dosimetry of [Nuclear medicine and biology · 2017Article
- Harnessing Integrative Omics to Facilitate Molecular Imaging of the Human Epidermal Growth Factor Receptor Family for Precision Medicine.Theranostics · 2017Review
- Effects of erlotinib therapy on [(11)C]erlotinib uptake in EGFR mutated, advanced NSCLC.EJNMMI research · 2016Article
- Recent Advances in the Development and Application of Radiolabeled Kinase Inhibitors for PET Imaging.Molecules (Basel, Switzerland) · 2015Review
- Quantifying and correcting for tail vein extravasation in small animal PET scans in cancer research: is there an impact on therapy assessment?EJNMMI research · 2015Article
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundNon-small cell lung carcinoma (NSCLC) represents approximately 80% of lung cancer cases, and over 60% of these tumors express the epidermal growth factor receptor (EGFR). Activating mutations in the tyrosine kinase (TK) domain of the EGFR are detected in 10% to 30% of NSCLC patients, and evidence of their presence is a prerequisite for initiation of first-line therapy with selective TK inhibitors (TKIs), such as gefitinib and erlotinib. To date, the selection of candidate patients for first-line treatment with EGFR TKIs requires an invasive tumor biopsy to affirm the mutational status of the receptor. This study was designed to evaluate whether positron emission tomography (PET) of NSCLC tumor-bearing mice using [(11)C]erlotinib could distinguish erlotinib-sensitive from erlotinib-insensitive or erlotinib-resistant tumors.
methodsFour human NSCLC cell lines were employed, expressing either of the following forms of the EGFR: (i) the wild-type receptor (QG56 cells), (ii) a mutant with an exon 19 in-frame deletion (HCC827 cells), (iii) a mutant with the exon 21 L858R point mutation (NCI-H3255 cells), and (iv) a double mutant harboring the L858R and T790M mutations (NCI-H1975 cells). Sensitivity of each cell line to the anti-proliferative effect of erlotinib was determined in vitro. In vivo PET imaging studies following i.v. injection of [(11)C]erlotinib were carried out in nude mice bearing subcutaneous (s.c.) xenografts of the four cell lines.
resultsCells harboring activating mutations in the EGFR TK domain (HCC827 and NCI-H3255) were approximately 1,000- and 100-fold more sensitive to erlotinib treatment in vitro, respectively, compared to the other two cell lines. [(11)C]Erlotinib PET scans could differentiate erlotinib-sensitive tumors from insensitive (QG56) or resistant (NCI-H1975) tumors already at 12 min after injection. Nonetheless, the uptake in HCC827 tumors was significantly higher than that in NCI-H3255, possibly reflecting differences in ATP and erlotinib affinities between the EGFR mutants.
conclusions[(11)C]Erlotinib imaging in mice differentiates erlotinib-sensitive NSCLC tumors from erlotinib-insensitive or erlotinib-resistant ones.
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