Abstract
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.
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