The DOI matches its Crossref record; 31 of the 31 references it cites were found in a registry or an index.
Development of Quinoline-Based Theranostic Ligands for the Targeting of Fibroblast Activation Protein
Open accessAbstract
Fibroblast activation protein (FAP) is overexpressed in cancer-associated fibroblasts and is involved in a variety of tumor-promoting activities such as matrix remodeling, angiogenesis, chemotherapy resistance, and immunosuppression. Because FAP shows low expression in most normal organs, it presents an interesting target for imaging and endoradiotherapy. In this investigation, FAP inhibitors (FAPIs) were modified and optimized for use as theranostic tracers. Methods: FAPIs based on a quinoline structure were synthesized and characterized with respect to binding, internalization, and efflux in cells expressing human and murine FAP as well as CD26. Preclinical pharmacokinetics were determined in tumor-bearing animals with biodistribution experiments and small-animal PET. Finally, a proof-of-concept approach toward imaging and therapy was chosen for 2 patients with metastasized breast cancer. Results: Of 15 synthesized FAPIs, FAPI-04 was identified as the most promising tracer for clinical application. Compared with the previously published ligand, FAPI-02, FAPI-04 showed excellent stability in human serum, higher affinity for FAP as opposed to CD26, and slower excretion in vitro. In vivo, a higher SUV was reached in tumor-bearing animals, leading to larger areas under the curve as calculated from biodistribution experiments. Finally, PET/CT scans with 68Ga-FAPI-04 in 2 patients with metastasized breast cancer revealed high tracer uptake in metastases and a reduction in pain symptoms after therapy with a considerably low dose of 90Y-FAPI-04. Conclusion: FAPI-04 represents a promising tracer for both diagnostic imaging and, possibly, targeted therapy of malignant tumors with a high content of activated fibroblasts, such as breast cancer.
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Cites
Suppression of Antitumor Immunity by Stromal Cells Expressing Fibroblast Activation Protein–α
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A Tumor-Imaging Method Targeting Cancer-Associated Fibroblasts
Loktev, A., Lindner, T., Mier, W., Debus, J., Altmann, A., Jäger, D., Giesel, F., Kratochwil, C., Barthe, P., Roumestand, C., et al. (2018) · Journal of Nuclear Medicine · doi:10.2967/jnumed.118.210435 · Cited by 777
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Carcinoma-associated fibroblasts: orchestrating the composition of malignancy
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Tumor-Promoting Desmoplasia Is Disrupted by Depleting FAP-Expressing Stromal Cells
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Cited by
Development of Fibroblast Activation Protein–Targeted Radiotracers with Improved Tumor Retention
Loktev, A., Lindner, T., Burger, E.-M., Altmann, A., Giesel, F., Kratochwil, C., Debus, J., Marmé, F., Jäger, D., Mier, W., et al. (2019) · Journal of Nuclear Medicine · doi:10.2967/jnumed.118.224469 · Cited by 554
Self-citationBaum, R. P., Schuchardt, C., Singh, A., Chantadisai, M., Robiller, F. C., Zhang, J., Mueller, D., Eismant, A., Almaguel, F., Zboralski, D., et al. (2022) · Journal of Nuclear Medicine · doi:10.2967/jnumed.120.259192 · Cited by 359
Advances in PET imaging of cancer
Schwenck, J., Sonanini, D., Cotton, J. M., Rammensee, H.-G., la Fougère, C., Zender, L., & Pichler, B. J. (2023) · Nature Reviews Cancer · doi:10.1038/s41568-023-00576-4 · Cited by 312
Comparison of 68Ga-FAPI and 18F-FDG Uptake in Gastric, Duodenal, and Colorectal Cancers
Pang, Y., Zhao, L., Luo, Z., Hao, B., Wu, H., Lin, Q., Sun, L., & Chen, H. (2021) · Radiology · doi:10.1148/radiol.2020203275 · Cited by 298
Targeting of activated fibroblasts for imaging and therapy
Lindner, T., Loktev, A., Giesel, F., Kratochwil, C., Altmann, A., & Haberkorn, U. (2019) · EJNMMI Radiopharmacy and Chemistry · doi:10.1186/s41181-019-0069-0 · Cited by 205
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Metadata
- Authors
- Lindner, T., Loktev, A., Altmann, A., Giesel, F., Kratochwil, C., Debus, J., Jäger, D., Mier, W., & Haberkorn, U.
- Venue
- Journal of Nuclear Medicine
- Publisher
- Society of Nuclear Medicine
- Published
- 2018-04-06
- Volume
- 59
- Issue
- 9
- Pages
- 1415-1422
- ISSN
- 0161-5505 (ISSN-L)
- 2159-662X
- OpenAlex
- W2796437750
- Cited by
- 935
- References
- 31
- FWCI
- 18.96
- Type
- journal article
- Language
- en
- Open access
- bronze
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