PET imaging with [⁶⁸Ga]NOTA-RGD for prostate cancer: a comparative study with [¹⁸F]fluorodeoxyglucose and [¹⁸F]fluoroethylcholine.
The α(v)β₃ integrin is highly expressed in prostate cancer (PCa), in which it is a key player in tumour invasion, angiogenesis and metastasis formation. Therefore, α(v)β₃ integrin is considered a very promising target for molecular imaging of PCa. This study tested the potential of the novel α(v)β₃ integrin affine agent [⁶⁸Ga]NOTA-RGD in comparison with the established [¹⁸F]fluoroethylcholine (FEC) and [¹⁸F]fluorodeoxyglucose (FDG) for assessing PCa using positron emission tomography (PET). [⁶⁸Ga]NOTA-RGD showed a lower uptake in PC-3 and DU-145 cells compared with FEC and FDG. µPET imaging studies showed a good delineation of the PCa xenografts in mice. The means tumor-to-muscle and tumor-to-bone-ratio amounted 5.1 ± 1.4 and 5.2 ± 1.2 for [⁶⁸Ga]NOTA-RGD compared with 2.6 ± 0.9 and 2.9 ± 1.6 for FDG, and 2.4 ± 0.7 and 0.8 ± 0.2 for FEC, respectively. The uptake of [⁶⁸Ga]NOTA-RGD into tumor was fully inhibited by c(RGDfV), known to bind specifically to α(v)β₃ integrin, confirming the specificity of the tumor uptake in vivo. These results suggest that [⁶⁸Ga]NOTA-RGD is a promising candidate for PET imaging of α(v)β₃ integrin expression in PCa and warrant further in vivo validations to ascertain its potential as an imaging agent for clinical use. The simple and fast preparation of [⁶⁸Ga]NOTA-RGD may greatly facilitate its translation to a clinical setting.
Ina
I
Israel
Dominik
D
Richter
Jochen
J
Stritzker
Michaela
M
van Ooschot
Ulrike
U
Donat
Andreas K
AK
Buck
Department of Nuclear Medicine, University of Wurzburg, Oberdurrbacher Straße 6, D-97080 Wurzburg, Germany. Samnick_S@ukw.de.
Samuel
S
Samnick
D000345:Affinity Labels / Q000737:chemistry / Q000378:metabolism; D000818:Animals; D001692:Biological Transport / Q000187:drug effects; D045744:Cell Line, Tumor; D002794:Choline / Q000031:analogs & derivatives / Q000378:metabolism; D056831:Coordination Complexes / Q000037:antagonists & inhibitors / Q000378:metabolism; D019788:Fluorodeoxyglucose F18 / Q000378:metabolism; D005710:Gallium Radioisotopes / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D039564:Integrin alphaV / Q000737:chemistry / Q000378:metabolism*; D039661:Integrin beta3 / Q000737:chemistry / Q000378:metabolism*; D016023:Integrins / Q000037:antagonists & inhibitors / Q000378:metabolism; D007553:Isotope Labeling; D008297:Male; D008819:Mice, Nude; D009363:Neoplasm Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism; D009368:Neoplasm Transplantation; D009842:Oligopeptides / Q000037:antagonists & inhibitors / Q000378:metabolism; D010456:Peptides, Cyclic / Q000008:administration & dosage / Q000494:pharmacology; D049268:Positron-Emission Tomography; D011467:Prostate / Q000000981:diagnostic imaging* / Q000187:drug effects / Q000378:metabolism / Q000473:pathology; D011471:Prostatic Neoplasms / Q000000981:diagnostic imaging* / Q000378:metabolism / Q000473:pathology; D019275:Radiopharmaceuticals / Q000737:chemistry / Q000378:metabolism
C584295:68Ga-1,4,7-triazacyclononane-1,4-7-triacetic acid-isothiocyanatobenzyl-c(Arg-Gly-Asp-Tyr-Lys); D000345:Affinity Labels; D056831:Coordination Complexes; D005710:Gallium Radioisotopes; D039564:Integrin alphaV; D039661:Integrin beta3; D016023:Integrins; D009363:Neoplasm Proteins; D009842:Oligopeptides; D010456:Peptides, Cyclic; D019275:Radiopharmaceuticals; C092113:cyclo(arginyl-glycyl-aspartyl-phenylalanyl-valyl); D019788:Fluorodeoxyglucose F18; C448902:fluoroethylcholine; D002794:Choline