The DOI matches its Crossref record; 27 of the 27 references it cites were found in a registry or an index.
Feasibility, Biodistribution, and Preliminary Dosimetry in Peptide-Targeted Radionuclide Therapy of Diverse Adenocarcinomas Using 177Lu-FAP-2286: First-in-Humans Results
Open accessAbstract
Fibroblast activation protein (FAP) is a promising target for diagnosis and therapy of numerous malignant tumors. FAP-2286 is the conjugate of a FAP-binding peptide, which can be labeled with radionuclides for theranostic applications. We present the first-in-human results using 177Lu-FAP-2286 for peptide-targeted radionuclide therapy (PTRT). Methods: PTRT using 177Lu-FAP-2286 was performed in 11 patients with advanced adenocarcinomas of pancreas, breast, rectum and ovary after prior confirmation of uptake on 68Ga-FAP-2286/-FAPI-04- PET/CT. Results: Administration of 177Lu-FAP-2286 (5.8 ± 2.0 GBq; range, 2.4–9.9 GBq) was well tolerated, with no adverse symptoms or clinically detectable pharmacologic effects being noticed or reported in any of the patients. The whole-body effective doses were 0.07 ± 0.02 Gy/GBq (range 0.04 – 0.1). The mean absorbed doses for kidneys and red marrow were 1.0 ± 0.6 Gy/GBq (range 0.4 – 2.0) and 0.05 ± 0.02 Gy/GBq (range 0.03 – 0.09), respectively. Significant uptake and long tumor retention of 177Lu-FAP-2286 resulted in high absorbed tumor doses, e.g., 3.0 ± 2.7 Gy/GBq (range 0.5 – 10.6) in bone metastases. No grade (G) 4 adverse events were observed. G3 events occurred in 3 patients – 1 pancytopenia, 1 leukocytopenia and 1 pain flare-up; 3 patients reported pain-response. Conclusion:177Lu-FAP-2286 PTRT, applied in a broad spectrum of cancers, was relatively well-tolerated with acceptable side effects and demonstrated long retention of the radiopeptide. Prospective clinical studies are warranted.
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Phase 3 Trial of 177 Lu-Dotatate for Midgut Neuroendocrine Tumors
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Cited by
Imaging-guided targeted radionuclide tumor therapy: From concept to clinical translation
Sun, J., Huangfu, Z., Yang, J., Wang, G., Hu, K., Gao, M., & Zhong, Z. (2022) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2022.114538 · Cited by 57
Metadata
- Authors
- Baum, R. P., Schuchardt, C., Singh, A., Chantadisai, M., Robiller, F. C., Zhang, J., Mueller, D., Eismant, A., Almaguel, F., Zboralski, D., Osterkamp, F., Hoehne, A., Reineke, U., Smerling, C., & Kulkarni, H. R.
- Venue
- Journal of Nuclear Medicine
- Publisher
- Society of Nuclear Medicine
- Published
- 2021-06-24
- Volume
- 63
- Issue
- 3
- Pages
- 415-423
- ISSN
- 0161-5505 (ISSN-L)
- 2159-662X
- OpenAlex
- W3173923097
- Cited by
- 359
- References
- 27
- FWCI
- 22.96
- Type
- journal article
- Language
- en
- Open access
- hybrid
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- Baum, R. P., Schuchardt, C., Singh, A., Chantadisai, M., Robiller, F. C., Zhang, J., Mueller, D., Eismant, A., Almaguel, F., Zboralski, D., Osterkamp, F., Hoehne, A., Reineke, U., Smerling, C., & Kulkarni, H. R. (2022). Feasibility, Biodistribution, and Preliminary Dosimetry in Peptide-Targeted Radionuclide Therapy of Diverse Adenocarcinomas Using 177Lu-FAP-2286: First-in-Humans Results. Journal of Nuclear Medicine. https://doi.org/10.2967/jnumed.120.259192
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