{"doi":"10.1016/j.nucmedbio.2017.05.007","title":"[ 11 C]Erlotinib PET cannot detect acquired erlotinib resistance in NSCLC tumor xenografts in mice","abstract":null,"journal":"Nuclear Medicine and Biology","year":2017,"id":597151,"datarank":0.32958368660043297,"base_score":2.1972245773362196,"endowment":2.1972245773362196,"self_citation_contribution":0.32958368660043297,"citation_network_contribution":0.0,"self_endowment_contribution":0.32958368660043297,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":8,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":null,"is_data_producer":false,"deposit_databanks":null,"is_oa":false,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":null,"fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":1529773,"name":"Taraneh Beikbaghban","orcid":null,"position":1,"is_corresponding":false},{"id":1529774,"name":"Thomas Wanek","orcid":null,"position":2,"is_corresponding":false},{"id":1529775,"name":"Kushtrim Kryeziu","orcid":null,"position":3,"is_corresponding":false},{"id":1229275,"name":"Christine Pirker","orcid":"0000-0001-7104-4404","position":4,"is_corresponding":false},{"id":1529776,"name":"Severin Mairinger","orcid":null,"position":5,"is_corresponding":false},{"id":1529778,"name":"Johann Stanek","orcid":null,"position":6,"is_corresponding":false},{"id":1529780,"name":"Thomas Filip","orcid":null,"position":7,"is_corresponding":false},{"id":1529782,"name":"Michael Sauberer","orcid":null,"position":8,"is_corresponding":false},{"id":1529783,"name":"Claudia Kuntner","orcid":null,"position":9,"is_corresponding":false},{"id":25331,"name":"Walter Berger","orcid":"0000-0003-0014-1658","position":10,"is_corresponding":false},{"id":1529784,"name":"Oliver Langer","orcid":null,"position":11,"is_corresponding":false},{"id":1529772,"name":"Alexander Traxl","orcid":null,"position":0,"is_corresponding":false}],"reference_count":0,"raw_metadata":{"has_enrichment":true,"resolved":true,"title":"[ 11 C]Erlotinib PET cannot detect acquired erlotinib resistance in NSCLC tumor xenografts in mice","abstract":"<h4>Introduction</h4>[<sup>11</sup>C]Erlotinib PET has shown promise to distinguish non-small cell lung cancer (NSCLC) tumors harboring the activating epidermal growth factor receptor (EGFR) mutation delE746-A750 from tumors with wild-type EGFR. To assess the suitability of [<sup>11</sup>C]erlotinib PET to detect the emergence of acquired erlotinib resistance in initially erlotinib-responsive tumors, we performed in vitro binding and PET experiments in mice bearing tumor xenografts using a range of different cancer cells, which were erlotinib-sensitive or exhibited clinically relevant resistance mechanisms to erlotinib.<h4>Methods</h4>The following cell lines were used for in vitro binding and PET experiments: the epidermoid carcinoma cell line A-431 (erlotinib-sensitive, wild-type EGFR) and the three NSCLC cell lines HCC827 (erlotinib-sensitive, delE746-A750), HCC827<sub>EPR</sub> (erlotinib-resistant, delE746-A750 and T790M) and HCC827<sub>ERLO</sub> (erlotinib-resistant, delE746-A750 and MET amplification). BALB/c nude mice with subcutaneous tumor xenografts underwent two consecutive [<sup>11</sup>C]erlotinib PET scans, a baseline scan and a second scan in which unlabeled erlotinib (10mg/kg) was co-injected. Logan graphical analysis was used to estimate total distribution volume (V<sub>T</sub>) of [<sup>11</sup>C]erlotinib in tumors.<h4>Results</h4>In vitro experiments revealed significantly higher uptake of [<sup>11</sup>C]erlotinib (5.2-fold) in the three NSCLC cell lines as compared to A-431 cells. In all four cell lines co-incubation with unlabeled erlotinib (1μM) led to significant reductions in [<sup>11</sup>C]erlotinib uptake (-19% to -66%). In both PET scans and for all four studied cell lines there were no significant differences in tumoral [<sup>11</sup>C]erlotinib V<sub>T</sub> values. For all three NSCLC cell lines, but not for the A-431 cell line, tumoral V<sub>T</sub> was significantly reduced following co-injection of unlabeled erlotinib (-20% to -35%).<h4>Conclusions</h4>We found no significant differences in the in vitro and in vivo binding of [<sup>11</sup>C]erlotinib between erlotinib-sensitive and erlotinib-resistant NSCLC cells. Our findings suggest that [<sup>11</sup>C]erlotinib PET will not be suitable to distinguish erlotinib-sensitive NSCLC tumors from tumors with acquired resistance to erlotinib.","is_dataset_classified":null,"base_score":2.1972245773362196,"endowment":2.1972245773362196,"datacite_reuse_total":0,"file_count":0,"downloads":0,"views":0,"has_version_chain":false,"is_dataset":false,"is_oa":false,"pmid":"28575795","pmcid":null,"openalex_id":"https://openalex.org/W2619172668","authors":[],"funders":[],"total_grants":0,"fwci":0.735,"citation_percentile":0.72238402,"influential_citations":0,"citation_trend":[{"year":2017,"count":1},{"year":2018,"count":2},{"year":2019,"count":1},{"year":2022,"count":2},{"year":2025,"count":1},{"year":2026,"count":1}],"oa_status":"closed","license":"https://www.elsevier.com/tdm/userlicense/1.0/","oa_locations":[{"url":"https://api.elsevier.com/content/article/PII:S0969805117301178?httpAccept=text/xml","host_type":"publisher"},{"url":"https://api.elsevier.com/content/article/PII:S0969805117301178?httpAccept=text/plain","host_type":"publisher"},{"url":"https://doi.org/10.1016/j.nucmedbio.2017.05.007","host_type":"journal"},{"url":"https://pubmed.ncbi.nlm.nih.gov/28575795","host_type":"repository"}],"fields_of_study":["Lung Cancer Treatments and Mutations","Colorectal Cancer Treatments and Studies","HER2/EGFR in Cancer Research","Animals","Carcinoma, Non-Small-Cell Lung","Cell Line, Tumor","Cell Transformation, Neoplastic","Drug Resistance, Neoplasm","ErbB Receptors","Erlotinib Hydrochloride","Female","Gene Expression Regulation, Neoplastic","Humans","Lung Neoplasms","Mice","Positron-Emission Tomography"],"mesh_terms":["Erlotinib Hydrochloride","Animals","Carcinoma, Non-Small-Cell Lung","Cell Transformation, Neoplastic","Female","Humans","Lung Neoplasms","Gene Expression Regulation, Neoplastic","Drug Resistance, Neoplasm","Cell Line, Tumor","Positron-Emission Tomography","Mice","ErbB Receptors"],"keywords":["Erlotinib","Erlotinib Hydrochloride","Epidermal growth factor receptor","Medicine","Lung cancer","T790M","Cancer research","Pharmacology","Internal medicine","Oncology","Cancer","Gefitinib","Non-small cell lung cancer","acquired resistance","Met Amplification","[(11)C]erlotinib"],"sdg_mappings":[{"sdg_number":0,"sdg_label":"Good health and well-being"}],"linked_datasets":[],"clinical_trials":[],"software_tools":[],"database_accessions":[],"source":"live","citation_network_status":"fetched"},"created_at":"2026-07-28T12:25:18.198051Z","pmid":null,"pmcid":null,"fwci":null,"citation_percentile":null,"influential_citations":0,"oa_status":null,"license":null,"views":0,"total_file_size_bytes":0,"version_count":0,"fair_f":null,"fair_a":null,"fair_i":null,"fair_r":null,"fair_zscore":null,"fair_rationale":null,"fair_model":null,"fair_agent_version":null,"fair_fulltext_source":null,"fair_has_llm":null,"fair_computed_at":null,"clinical_trials":[],"software_tools":[],"db_accessions":[],"linked_datasets":[],"topics":[]}