{"doi":"10.1101/2020.07.13.20141036","title":"Preclinical and first-in-human-brain-cancer applications of [18F]poly-(ADP-ribose) polymerase inhibitor PET/MR","abstract":"Abstract We report pre-clinical and first-in-human-brain-cancer data using a targeted poly(ADP-ribose)polymerase1 (PARP1) binding PET tracer, [ 18 F]PARPi, as a diagnostic tool to differentiate between brain cancers and treatment related changes. In a pre-clinical mouse model, we illustrated that [ 18 F]PARPi crosses the blood-brain barrier and specifically binds to PARP1 overexpressed in cancer cell nuclei. In humans, we demonstrated high [ 18 F]PARPi uptake on PET/MR in active brain cancers and low uptake in treatment related changes, independent of blood brain-barrier disruption. Immunohistochemistry results confirmed higher PARP1 expression in cancers than non-cancers. Specificity was also corroborated by blocking fluorescent tracer uptake with excess of unlabeled PARP inhibitor in fresh cancer tissue derived from a patient. Although larger studies are necessary to confirm and further explore this tracer, we describe an encouraging role for the use of [ 18 F]PARPi as a diagnostic tool in evaluating patients with brain cancers and possible treatment related changes. One Sentence summary PET imaging with [ 18 F]PARPi can differentiate active brain cancer from treatment related changes with encouraging results for use during treatment follow-up.","journal":"medRxiv","year":2020,"id":119914,"datarank":0.0,"base_score":0.0,"endowment":0.0,"self_citation_contribution":0.0,"citation_network_contribution":0.0,"self_endowment_contribution":0.0,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":14,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9009,"is_data_producer":false,"deposit_databanks":null,"is_oa":true,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2020-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":280688,"name":"Paula Demétrio De Souza França","orcid":"0000-0003-4316-8834","position":1,"is_corresponding":false},{"id":280685,"name":"Giacomo Pirovano","orcid":"0000-0001-8862-3613","position":2,"is_corresponding":false},{"id":281415,"name":"Anna F. Piotrowski","orcid":"0000-0003-0058-8476","position":3,"is_corresponding":false},{"id":477325,"name":"Philip J. Nicklin","orcid":"0009-0005-0869-3598","position":4,"is_corresponding":false},{"id":268008,"name":"Christopher C. Riedl","orcid":"0000-0002-7859-6997","position":5,"is_corresponding":false},{"id":477326,"name":"Jazmin Schwartz","orcid":"0000-0001-9367-4538","position":6,"is_corresponding":false},{"id":236579,"name":"Tejus Bale","orcid":"0000-0003-3641-9287","position":7,"is_corresponding":false},{"id":328138,"name":"Patrick L. Donabedian","orcid":"0000-0003-3636-4378","position":8,"is_corresponding":false},{"id":280686,"name":"Susanne Kossatz","orcid":"0000-0002-1908-1782","position":9,"is_corresponding":false},{"id":451223,"name":"Eva Burnazi","orcid":"0000-0003-3089-0959","position":10,"is_corresponding":false},{"id":408501,"name":"Sheryl Roberts","orcid":"0000-0002-2326-9120","position":11,"is_corresponding":false},{"id":269473,"name":"Serge K. Lyashchenko","orcid":null,"position":12,"is_corresponding":false},{"id":413120,"name":"Alexandra Miller","orcid":"0000-0003-2048-579X","position":13,"is_corresponding":false},{"id":374896,"name":"Nelson S. Moss","orcid":"0000-0002-0930-1681","position":14,"is_corresponding":false},{"id":478172,"name":"Megan Fiasconaro","orcid":null,"position":15,"is_corresponding":false},{"id":281409,"name":"Zhigang Zhang","orcid":"0000-0002-1556-7945","position":16,"is_corresponding":false},{"id":291692,"name":"Audrey Mauguen","orcid":"0000-0003-3236-6093","position":17,"is_corresponding":false},{"id":245644,"name":"Thomas Reiner","orcid":"0000-0002-7819-5480","position":18,"is_corresponding":false},{"id":269961,"name":"Mark Dunphy","orcid":"0000-0002-1886-1832","position":19,"is_corresponding":false},{"id":281410,"name":"Robert J. Young","orcid":"0000-0001-7003-3017","position":0,"is_corresponding":true}],"reference_count":48,"raw_metadata":null,"created_at":"2026-07-18T23:14:13.002105Z","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":[]}