{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,4,29]],"date-time":"2026-04-29T16:44:26Z","timestamp":1777481066900,"version":"3.51.4"},"reference-count":21,"publisher":"SAGE Publications","issue":"2","license":[{"start":{"date-parts":[[2025,3,1]],"date-time":"2025-03-01T00:00:00Z","timestamp":1740787200000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/journals.sagepub.com\/page\/policies\/text-and-data-mining-license"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Cancer Biotherapy and Radiopharmaceuticals"],"published-print":{"date-parts":[[2025,3]]},"abstract":"\n Introduction:<\/jats:title>\n \n Many studies have reported the role of P-glycoprotein (Pgp) in chemoresistance in various pathological conditions such as cancer and neurodegenerative diseases, such as Alzheimer\u2019s. In this study, we are reporting the high-performance liquid chromatography (HPLC)-based purification of fluorine-18 [\n 18<\/jats:sup>\n F]AVT-011 and its preclinical evaluation.\n <\/jats:p>\n <\/jats:sec>\n \n Methods:<\/jats:title>\n \n AVT-011 was labeled with\n 18<\/jats:sup>\n F using the nucleophilic substitution method by heating the reaction mixture at 110\u00b0C for 10 min, followed by purification using preparative HPLC and C18ec cartridge. The\n in vitro<\/jats:italic>\n cell uptake study was carried out in U87 cells with and without an inhibitor. The preclinical toxicity was carried out in CD1 mice in three groups, including control, AVT-011 treated, and [\n 18<\/jats:sup>\n F]AVT-011 treated. The biodistribution study was done in CD1 mice (\n n<\/jats:italic>\n = 12) after intravenous injection of 4\u20136 MBq [\n 18<\/jats:sup>\n F]AVT-011, and mice were sacrificed at various time intervals. A dose of 3.7 \u00b1 0.7 MBq of [\n 18<\/jats:sup>\n F]AVT-011 was injected intravenously in the healthy Swiss albino mice, and the whole-body micro-positron emission tomography was acquired at 0-, 30-, 60-, and 120-min postinjection.\n <\/jats:p>\n <\/jats:sec>\n \n Results:<\/jats:title>\n \n The radiochemical purity of [\n 18<\/jats:sup>\n F]AVT-011 was 97 \u00b1 1.5% as evaluated by radio-HPLC with a yield of 14 \u00b1 2% and was stable up to 95% under\n in vitro<\/jats:italic>\n conditions in blood and\n in vivo<\/jats:italic>\n conditions up to 4 h. The\n in vitro<\/jats:italic>\n cell uptake study showed a significant difference in control (27.4 \u00b1 2.1%) and blocked U987 cells (73.2 \u00b1 3.2%) after incubation of 120 min. The tissue distribution in mice showed the highest uptake in the liver (17.3 \u00b1 2.4%), kidneys (16.6 \u00b1 3.1%), lungs (10.4 \u00b1 2.9%), and spleen (5.6 \u00b1 0.8%) at 15 min, and the activity was washed out with time. The radioactivity cleared through the hepatorenal pathway. The animal imaging study also demonstrates a similar biodistribution pattern.\n <\/jats:p>\n <\/jats:sec>\n \n Conclusions:<\/jats:title>\n \n [\n 18<\/jats:sup>\n F]AVT-011 showed higher specific activity than the cartridge-based method but showed similar biological activity.\n <\/jats:p>\n <\/jats:sec>","DOI":"10.1089\/cbr.2024.0114","type":"journal-article","created":{"date-parts":[[2024,9,12]],"date-time":"2024-09-12T05:16:30Z","timestamp":1726118190000},"page":"96-103","source":"Crossref","is-referenced-by-count":0,"title":["Synthesis, Preclinical Toxicity, and Biodistribution of [\n 18<\/sup>\n F]AVT-011 to Assess the P-Glycoprotein Function"],"prefix":"10.1177","volume":"40","author":[{"given":"Riptee","family":"Thakur","sequence":"first","affiliation":[{"name":"Department of Neuroimaging & Interventional Radiology, National Institute of Mental Health & Neurosciences (NIMHANS), Bengaluru, India."}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Manoj","family":"Kumar","sequence":"additional","affiliation":[{"name":"Department of Neuroimaging & Interventional Radiology, National Institute of Mental Health & Neurosciences (NIMHANS), Bengaluru, India."}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Aishwarya","family":"Kumar","sequence":"additional","affiliation":[{"name":"Department of Neuroimaging & Interventional Radiology, National Institute of Mental Health & Neurosciences (NIMHANS), Bengaluru, India."}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Raman Kumar","family":"Joshi","sequence":"additional","affiliation":[{"name":"Department of Neuroimaging & Interventional Radiology, National Institute of Mental Health & Neurosciences (NIMHANS), Bengaluru, India."}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Divya","family":"Maheshwari","sequence":"additional","affiliation":[{"name":"Avaant Imaging, Lexington, Massachusetts, USA."}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Afsal Mohammed","family":"KM","sequence":"additional","affiliation":[{"name":"Esente Healthcare, Bengaluru, India."}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Manjunatha","family":"Venkataswamy","sequence":"additional","affiliation":[{"name":"Department of Neurovirology, NIMHANS, Bengaluru, India."}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Bhabani","family":"Mohanty","sequence":"additional","affiliation":[{"name":"Animal Oncology Group, Advanced Centre for Treatment, Research & Education in Cancer (ACTREC), Tata Memorial Centre, Mumbai, India."}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Pradip","family":"Chaudhari","sequence":"additional","affiliation":[{"name":"Animal Oncology Group, Advanced Centre for Treatment, Research & Education in Cancer (ACTREC), Tata Memorial Centre, Mumbai, India."}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Hosahalli K.","family":"Mohan","sequence":"additional","affiliation":[{"name":"Department of Nuclear Medicine, Sri Shankara Cancer Hospital & Research Centre, Bengaluru, India."}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-1832-798X","authenticated-orcid":false,"given":"Pardeep","family":"Kumar","sequence":"additional","affiliation":[{"name":"Department of Neuroimaging & Interventional Radiology, National Institute of Mental Health & Neurosciences (NIMHANS), Bengaluru, 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