مورد إلكتروني
Automated Radiosynthesis, Preliminary In Vitro/In Vivo Characterization of OncoFAP-Based Radiopharmaceuticals for Cancer Imaging and Therapy
| العنوان: | Automated Radiosynthesis, Preliminary In Vitro/In Vivo Characterization of OncoFAP-Based Radiopharmaceuticals for Cancer Imaging and Therapy |
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| المؤلفون: | Bartoli, F, Elsinga, P, Nazario, L, Zana, A, Galbiati, A, Millul, J, Migliorini, F, Cazzamalli, S, Neri, D, Slart, R, Erba, P, Bartoli F., Elsinga P., Nazario L. R., Zana A., Galbiati A., Millul J., Migliorini F., Cazzamalli S., Neri D., Slart R. H. J. A., Erba P. A. |
| بيانات النشر: | MDPI country:CH 2022 |
| نوع الوثيقة: | Electronic Resource |
| مستخلص: | FAP-targeted radiopharmaceuticals represent a breakthrough in cancer imaging and a viable option for therapeutic applications. OncoFAP is an ultra-high-affinity ligand of FAP with a dissociation constant of 680 pM. OncoFAP has been recently discovered and clinically validated for PET imaging procedures in patients with solid malignancies. While more and more clinical validation is becoming available, the need for scalable and robust procedures for the preparation of this new class of radiopharmaceuticals continues to increase. In this article, we present the development of automated radiolabeling procedures for the preparation of OncoFAP-based radiopharmaceuticals for cancer imaging and therapy. A new series of [68Ga]Ga-OncoFAP, [177Lu]Lu-OncoFAP and [18F]AlF-OncoFAP was produced with high radiochemical yields. Chemical and biochemical characterization after radiolabeling confirmed its excellent stability, retention of high affinity for FAP and absence of radiolysis by-products. The in vivo biodistribution of [18F]AlF-NOTA-OncoFAP, a candidate for PET imaging procedures in patients, was assessed in mice bearing FAP-positive solid tumors. The product showed rapid accumulation in solid tumors, with an average of 6.6% ID/g one hour after systemic administration and excellent tumor-to-healthy organs ratio. We have developed simple, quick, safe and robust synthetic procedures for the preparation of theranostic OncoFAP-compounds based on Gallium-68, Lutetium-177 and Fluorine-18 using the commercially available FASTlab synthesis module. |
| مصطلحات الفهرس: | 177, Lu-labeled, 68, Ga-labeled, Al[, 18, F]F-labeled, automated radiosynthesi, OncoFAP, positron emission tomography, radiopharmaceutical, theranostic, tumors imaging, info:eu-repo/semantics/article |
| URL: | info:eu-repo/semantics/altIdentifier/pmid/36015106 info:eu-repo/semantics/altIdentifier/wos/WOS:000845703300001 volume:15 issue:8 journal:PHARMACEUTICALS |
| الإتاحة: | Open access content. Open access content info:eu-repo/semantics/openAccess |
| ملاحظة: | ELETTRONICO English |
| أرقام أخرى: | ITBAO oai:boa.unimib.it:10281/414702 10.3390/ph15080958 info:eu-repo/semantics/altIdentifier/scopus/2-s2.0-85137375300 1383765680 |
| المصدر المساهم: | BICOCCA OPEN ARCH From OAIster®, provided by the OCLC Cooperative. |
| رقم الأكسشن: | edsoai.on1383765680 |
| قاعدة البيانات: | OAIster |
| الوصف غير متاح. |