¹⁸F-FPRGD2 PET/CT Imaging of Integrin α_vβ₃ in Renal Carcinomas: Correlation with Histopathology

18F-FPRGD2 PET/CT imaging of musculoskeletal disorders

“…Therefore, 18 F-FPRGD 2 uptake by joints and surrounding structures might be explained by the radiopharmaceutical binding to the integrin a v b 3 of constitutive cells that form the joint and its neighboring bone, thus illustrating local cellular changes during OA development. Such hypothesis was investigated in vitro by reanalyzing integrin a v b 3 expression in OA cartilage and dedifferentiated chondrocytes using anti-integrin a v b 3 antibody LM609, already described in the oncological literature through correlations observed between RGD-based radiopharmaceutical uptake and LM609 pattern in tumor and vessels at histological level [31,46]. Whereas primary chondrocytes did not either show the presence of a v or b 3 by western blotting, nor were stained by the anti-integrin a v b 3 antibody LM609 by FACS analysis, dedifferentiated chondrocytes obtained after 14 days of culture expressed both monomers (a v and b 3 ) and the heterodimer a v b 3 .…”

“…We retrospectively reviewed 62 18 F-FPRGD 2 PET/CT images (40 males; 22 females) that were initially performed as part of a prospective protocol evaluating locally advanced rectal adenocarcinoma without distant metastases (n = 36) or renal masses (n = 26) [31]. The final histology of renal masses was a clear cell renal cell carcinoma (ccRCC, n = 15), papillary RCC (n = 6), chromophobe RCC (n = 1), oncocytoma (n = 2), breast cancer metastasis (n = 1) and angiomyolipoma (n = 1).…”

68Ga-TRAP-(RGD)3 Hybrid Imaging for the In Vivo Monitoring of αvß3-Integrin Expression as Biomarker of Anti-Angiogenic Therapy Effects in Experimental Breast Cancer

“…α v ß 3 -integrin has recently gained attention as potential imaging target for the non-invasive in vivo characterization of the tumor microenvironment, and first clinical studies investigating radiolabeled RGD compounds in humans have been published [17, 32]. In particular, the in-human use of RGD-based radiotracers proved to be safe with tumor-specific uptake profiles [6, 33].…”

“…Semiquantitative measures of tissue RGD radiotracer uptake demonstrated excellent correlations with the α v ß 3 -integrin receptor expression as quantified by ex vivo immunohistochemistry [17, 18]. The selective in vivo imaging of endothelial α v ß 3 -integrin expression as surrogate of tumor angiogenesis may be limited by α v ß 3 -integrin overexpressed on tumor cell surfaces [10, 12].…”

PET/Computed Tomography Using New Radiopharmaceuticals in Targeted Therapy

“…Different RGD peptides have been labeled with 68 Ga, 18 F, and 64 Cu and used for PET imaging. 86 Withofs and colleagues 87 showed the utility of 18 F-mini-PEG spacered RGD dimer ( 18 F-FPRGD2) for angiogenesis imaging in patients with renal cell carcinoma, but the utility was limited to non-avb3-expressing tumors. Various 68Ga-labeled tracers are now being actively evaluated.…”