{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,26]],"date-time":"2026-09-26T06:02:11Z","timestamp":1790402531912,"version":"4.1.0"},"reference-count":0,"publisher":"MDPI AG","issue":"7","license":[{"start":{"date-parts":[[2024,6,25]],"date-time":"2024-06-25T00:00:00Z","timestamp":1719273600000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"Michigan Pioneer Fellows at the University of Michigan (Jason Witek)","award":["R01EB021155"],"award-info":[{"award-number":["R01EB021155"]}]},{"name":"Michigan Pioneer Fellows at the University of Michigan (Jason Witek)","award":["1159892"],"award-info":[{"award-number":["1159892"]}]},{"name":"NIH","award":["R01EB021155"],"award-info":[{"award-number":["R01EB021155"]}]},{"name":"NIH","award":["1159892"],"award-info":[{"award-number":["1159892"]}]},{"name":"Neuroendocrine Tumor Foundation 2023 NETRF Investigator Award","award":["R01EB021155"],"award-info":[{"award-number":["R01EB021155"]}]},{"name":"Neuroendocrine Tumor Foundation 2023 NETRF Investigator Award","award":["1159892"],"award-info":[{"award-number":["1159892"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Pharmaceuticals"],"abstract":"<jats:p>Background: Cancer-associated fibroblasts have become a new target for therapy. Fibroblasts present within malignancies express the fibroblast activation protein (FAP). Inhibitors to FAP (FAPI) are small molecules recently developed as a theranostic agents for imaging and radiotherapy. All currently used FAPI rely on a linker\u2013chelator complex attached to the \u2018inhibitor\u2019. We describe a new automated method of the direct attachment of the radioisotope to the inhibitor, resulting in a &gt;50% MW reduction with the hope of an improved tumor-to-background ratio and tumor uptake. Methods: [18F]FluroFAPI was developed from a Sn precursor. This allowed for subsequent automated radioflourination. We obtained the biodistribution of [18F]FluroFAPI in rats, performed estimated human radiation dosimetry, and performed a 100\u00d7 expected single dose toxicology analysis for eventual first-in-human experiments. Results: The synthesis of the Sn precursor for FluorFAPI and the automated synthesis of [18F]FluroFAPI was demonstrated. [18F]FluroFAPI had favorable estimated human radiation dosimetry, and demonstrated no adverse effects when injected at a dose of 100\u00d7 that planned for [18F]FluroFAPI. Conclusions: With the successful development of an automated synthesis of [18F]FluroFAPI, first-in-human testing can be planned with the hope of an improved tumor-to-background performance compared to other FAPI agents.<\/jats:p>","DOI":"10.3390\/ph17070833","type":"journal-article","created":{"date-parts":[[2024,6,28]],"date-time":"2024-06-28T03:42:30Z","timestamp":1719546150000},"page":"833","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":5,"title":["Automated Radiosynthesis of [18F]FluoFAPI and Its Dosimetry and Single Acute Dose Toxicological Evaluation"],"prefix":"10.3390","volume":"17","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-7271-6567","authenticated-orcid":false,"given":"Jason A.","family":"Witek","sequence":"first","affiliation":[{"name":"Department of Radiology, University of Michigan Medical School, Ann Arbor, MI 48109, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Allen F.","family":"Brooks","sequence":"additional","affiliation":[{"name":"Department of Radiology, University of Michigan Medical School, Ann Arbor, MI 48109, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sahil M.","family":"Kapila","sequence":"additional","affiliation":[{"name":"Department of Chemistry, University of Michigan, Ann Arbor, MI 48109, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Wade P.","family":"Winton","sequence":"additional","affiliation":[{"name":"Department of Radiology, University of Michigan Medical School, Ann Arbor, MI 48109, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jenelle R.","family":"Stauff","sequence":"additional","affiliation":[{"name":"Department of Radiology, University of Michigan Medical School, Ann Arbor, MI 48109, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-6505-0450","authenticated-orcid":false,"given":"Peter J. H.","family":"Scott","sequence":"additional","affiliation":[{"name":"Department of Radiology, University of Michigan Medical School, Ann Arbor, MI 48109, USA"},{"name":"The Interdepartmental Program in Medicinal Chemistry, University of Michigan College of Pharmacy, Ann Arbor, MI 48109, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-8471-4988","authenticated-orcid":false,"given":"Benjamin L.","family":"Viglianti","sequence":"additional","affiliation":[{"name":"Department of Radiology, University of Michigan Medical School, Ann Arbor, MI 48109, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2024,6,25]]},"container-title":["Pharmaceuticals"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/www.mdpi.com\/1424-8247\/17\/7\/833\/pdf","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2025,10,10]],"date-time":"2025-10-10T15:04:10Z","timestamp":1760108650000},"score":1,"resource":{"primary":{"URL":"https:\/\/www.mdpi.com\/1424-8247\/17\/7\/833"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2024,6,25]]},"references-count":0,"journal-issue":{"issue":"7","published-online":{"date-parts":[[2024,7]]}},"alternative-id":["ph17070833"],"URL":"https:\/\/doi.org\/10.3390\/ph17070833","relation":{},"ISSN":["1424-8247"],"issn-type":[{"value":"1424-8247","type":"electronic"}],"subject":[],"published":{"date-parts":[[2024,6,25]]}}}