The DOI matches its Crossref record; 32 of the 32 references it cites were found in a registry or an index.
68Ga- and 177Lu-Labeled PSMA I&T: Optimization of a PSMA-Targeted Theranostic Concept and First Proof-of-Concept Human Studies
Open accessAbstract
UNLABELLED: On the basis of the high and consistent expression of prostate-specific membrane antigen (PSMA) in metastatic prostate cancer (PC), the goal of this study was the development, preclinical evaluation, and first proof-of-concept investigation of a PSMA inhibitor for imaging and therapy (PSMA I&T) for (68)Ga-based PET and (177)Lu-based endoradiotherapeutic treatment in patients with metastatic and castration-resistant disease. METHODS: PSMA I&T was synthesized in a combined solid phase and solution chemistry strategy. The PSMA affinity of (nat)Ga-/(nat)Lu-PSMA I&T was determined in a competitive binding assay using LNCaP cells. Internalization kinetics of (68)Ga- and (177)Lu-PSMA I&T were investigated using the same cell line, and biodistribution studies were performed in LNCaP tumor-bearing CD-1 nu/nu mice. Initial human PET imaging studies using (68)Ga-PSMA I&T, as well as endoradiotherapeutic treatment of 2 patients with metastatic PC using (177)Lu-PSMA I&T, were performed. RESULTS: PSMA I&T and its cold gallium and lutetium analog revealed nanomolar affinity toward PSMA. The DOTAGA (1,4,7,10-tetraazacyclododecane-1-(glutamic acid)-4,7,10-triacetic acid) conjugate PSMA I&T allowed fast and high-yield labeling with (68)Ga(III) and (177)Lu(III). Uptake of (68)Ga-/(177)Lu-PSMA I&T in LNCaP tumor cells is highly efficient and PSMA-specific, as demonstrated by competition studies both in vitro and in vivo. Tumor targeting and tracer kinetics in vivo were fast, with the highest uptake in tumor xenografts and kidneys (both PSMA-specific). First-in-human (68)Ga-PSMA I&T PET imaging allowed high-contrast detection of bone lesions, lymph node, and liver metastases. Endoradiotherapy with (177)Lu-PSMA I&T in 2 patients was found to be effective and safe with no detectable side effects. CONCLUSION: (68)Ga-PSMA I&T shows potential for high-contrast PET imaging of metastatic PC, whereas its (177)Lu-labeled counterpart exhibits suitable targeting and retention characteristics for successful endoradiotherapeutic treatment. Prospective studies on larger cohorts of patients are warranted and planned.
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Alpha Emitter Radium-223 and Survival in Metastatic Prostate Cancer
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前立腺癌のEAUガイドライン。パート1:臨床的限局性疾患のスクリーニング,診断および治療
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Cited by
68Ga-PSMA PET/CT: Joint EANM and SNMMI procedure guideline for prostate cancer imaging: version 1.0
Fendler, W. P., Eiber, M., Beheshti, M., Bomanji, J., Ceci, F., Cho, S., Giesel, F., Haberkorn, U., Hope, T. A., Kopka, K., et al. (2017) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-017-3670-z · Cited by 750
Self-citationHooijman, E. L., Chalashkan, Y., Ling, S. W., Kahyargil, F. F., Segbers, M., Bruchertseifer, F., Morgenstern, A., Seimbille, Y., Koolen, S. L. W., Brabander, T., et al. (2021) · Pharmaceutics · doi:10.3390/pharmaceutics13050715 · Cited by 59
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
- Weineisen, M., Schottelius, M., Simecek, J., Baum, R. P., Yildiz, A., Beykan, S., Kulkarni, H. R., Lassmann, M., Klette, I., Eiber, M., Schwaiger, M., & Wester, H.-J.
- Venue
- Journal of Nuclear Medicine
- Publisher
- Society of Nuclear Medicine
- Published
- 2015-06-18
- Volume
- 56
- Issue
- 8
- Pages
- 1169-1176
- ISSN
- 0161-5505 (ISSN-L)
- 2159-662X
- OpenAlex
- W2175765437
- Cited by
- 532
- References
- 32
- FWCI
- 37.20
- Type
- journal article
- Language
- en
- Open access
- bronze
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- Weineisen, M., Schottelius, M., Simecek, J., Baum, R. P., Yildiz, A., Beykan, S., Kulkarni, H. R., Lassmann, M., Klette, I., Eiber, M., Schwaiger, M., & Wester, H.-J. (2015). 68Ga- and 177Lu-Labeled PSMA I&T: Optimization of a PSMA-Targeted Theranostic Concept and First Proof-of-Concept Human Studies. Journal of Nuclear Medicine. https://doi.org/10.2967/jnumed.115.158550
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