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| Home > Publications database > Development of Fibroblast Activation Protein-Targeted Radiotracers with Improved Tumor Retention. > print |
| 001 | 147192 | ||
| 005 | 20240229112642.0 | ||
| 024 | 7 | _ | |2 doi |a 10.2967/jnumed.118.224469 |
| 024 | 7 | _ | |2 pmid |a pmid:30850501 |
| 024 | 7 | _ | |2 pmc |a pmc:PMC6785792 |
| 024 | 7 | _ | |2 ISSN |a 0022-3123 |
| 024 | 7 | _ | |2 ISSN |a 0097-9058 |
| 024 | 7 | _ | |2 ISSN |a 0161-5505 |
| 024 | 7 | _ | |2 ISSN |a 1535-5667 |
| 024 | 7 | _ | |2 ISSN |a 2159-662X |
| 024 | 7 | _ | |a altmetric:70354575 |2 altmetric |
| 037 | _ | _ | |a DKFZ-2019-02328 |
| 041 | _ | _ | |a eng |
| 082 | _ | _ | |a 610 |
| 100 | 1 | _ | |0 P:(DE-He78)b92647c18492ca0d83530e3e93821495 |a Loktev, Anastasia |b 0 |e First author |
| 245 | _ | _ | |a Development of Fibroblast Activation Protein-Targeted Radiotracers with Improved Tumor Retention. |
| 260 | _ | _ | |a New York, NY |b Soc. |c 2019 |
| 336 | 7 | _ | |2 DRIVER |a article |
| 336 | 7 | _ | |2 DataCite |a Output Types/Journal article |
| 336 | 7 | _ | |0 PUB:(DE-HGF)16 |2 PUB:(DE-HGF) |a Journal Article |b journal |m journal |s 1572003795_13167 |
| 336 | 7 | _ | |2 BibTeX |a ARTICLE |
| 336 | 7 | _ | |2 ORCID |a JOURNAL_ARTICLE |
| 336 | 7 | _ | |0 0 |2 EndNote |a Journal Article |
| 520 | _ | _ | |a Cancer-associated fibroblasts constitute a vital subpopulation of the tumor stroma and are present in more than 90% of epithelial carcinomas. The overexpression of the serine protease fibroblast activation protein (FAP) allows a selective targeting of a variety of tumors by inhibitor-based radiopharmaceuticals (FAPIs). Of these compounds, FAPI-04 has been recently introduced as a theranostic radiotracer and demonstrated high uptake into different FAP-positive tumors in cancer patients. To enable the delivery of higher doses, thereby improving the outcome of a therapeutic application, several FAPI variants were designed to further increase tumor uptake and retention of these tracers. Methods: Novel quinoline-based radiotracers were synthesized by organic chemistry and evaluated in radioligand binding assays using FAP-expressing HT-1080 cells. Depending on their in vitro performance, small-animal PET imaging and biodistribution studies were performed on HT-1080-FAP tumor-bearing mice. The most promising compounds were used for clinical PET imaging in 8 cancer patients. Results: Compared with FAPI-04, 11 of 15 FAPI derivatives showed improved FAP binding in vitro. Of these, 7 compounds demonstrated increased tumor uptake in tumor-bearing mice. Moreover, tumor-to-normal-organ ratios were improved for most of the compounds, resulting in images with higher contrast. Notably two of the radiotracers, FAPI-21 and -46, displayed substantially improved ratios of tumor to blood, liver, muscle, and intestinal uptake. A first diagnostic application in cancer patients revealed high intratumoral uptake of both radiotracers already 10 min after administration but a higher uptake in oral mucosa, salivary glands, and thyroid for FAPI-21. Conclusion: Chemical modification of the FAPI framework enabled enhanced FAP binding and improved pharmacokinetics in most of the derivatives, resulting in high-contrast images. Moreover, higher doses of radioactivity can be delivered while minimizing damage to healthy tissue, which may improve therapeutic outcome. |
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| 700 | 1 | _ | |a Lindner, Thomas |b 1 |
| 700 | 1 | _ | |a Burger, Eva-Maria |b 2 |
| 700 | 1 | _ | |0 P:(DE-He78)5f322a4feb2548d8312f781f80718b3c |a Altmann, Annette |b 3 |u dkfz |
| 700 | 1 | _ | |a Giesel, Frederik |b 4 |
| 700 | 1 | _ | |a Kratochwil, Clemens |b 5 |
| 700 | 1 | _ | |0 P:(DE-He78)8714da4e45acfa36ce87c291443a9218 |a Debus, Jürgen |b 6 |u dkfz |
| 700 | 1 | _ | |a Marmé, Frederik |b 7 |
| 700 | 1 | _ | |a Jäger, Dirk |b 8 |
| 700 | 1 | _ | |a Mier, Walter |b 9 |
| 700 | 1 | _ | |0 P:(DE-He78)13a0afba029f5f64dc18b25ef7499558 |a Haberkorn, Uwe |b 10 |e Last author |u dkfz |
| 773 | _ | _ | |0 PERI:(DE-600)2040222-3 |a 10.2967/jnumed.118.224469 |g Vol. 60, no. 10, p. 1421 - 1429 |n 10 |p 1421 - 1429 |t Journal of nuclear medicine |v 60 |x 2159-662X |y 2019 |
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