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Initial evaluation of <scp>PET</scp> / <scp>CT</scp> with <sup>18</sup> F‐ <scp>FSU</scp> ‐880 targeting prostate‐specific membrane antigen in prostate cancer patients
摘要： This first-in-man study was carried out to evaluate the safety, whole-body distribution, dose estimation, and lesion accumulation of 18F-FSU-880, a newly developed probe targeting prostate-specific membrane antigen. Six prostate cancer patients with known metastatic lesions underwent serial whole-body PET/computed tomography (CT) with 18F-FSU-880. Blood and urine were analyzed before and after PET/CT. Accumulation of 18F-FSU-880 in organs and metastatic lesions in serial PET images were evaluated by measuring the standardized uptake values. From the biodistribution data, the organ doses and whole-body effective dose were calculated using OLINDA/EXM software. 18F-FSU-880 PET/CT could be carried out without significant adverse effects. High physiological uptake was observed in the salivary/lachrymal glands and kidneys. The effective dose was calculated to be 0.921 × 10?2 mSv/MBq. Known metastatic lesions were clearly visualized with high image contrast that increased with time, except in 1 patient, whose bone metastases were well-controlled and inactive. The PET/CT with 18F-FSU-880 could be carried out safely and could clearly visualize active metastatic lesions. The present results warrant further clinical studies with a larger number of cases to verify the clinical utility of 18F-FSU-880 PET/CT in the management of prostate cancer patients.
关键词： dosimetry,prostate cancer,prostate-specific membrane antigen,positron emission tomography/computed tomography,fluorine-18
更新于2025-09-23 15:23:52
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Eficacia de la imagen precoz con 68Ga-PSMA-I&T para la discriminación de lesiones en los pacientes con cáncer de próstata
摘要： Objective: 68Ga-PSMA-uptake shows accumulation in the malignant lesions of prostate cancer patients as early as 5 min p.i. Studies indicate the value of adding an early image of the pelvis to the imaging protocol of 68Ga-PSMA-11 PET/CT scan showed contradictory results. In this study we planned to assess the significance of an additional early imaging in 68Ga-PSMA-I&T PET/CT imaging in prostate cancer patients. Materials and methods: A total of 35 prostate cancer patients referred to 68Ga-PSMA-I&T PET/CT imaging for restaging of the disease due to suspicion of relapse after definitive therapy were enrolled. First an early static pelvic image was obtained at a maximum of 300 s following injection of the radiotracer. Sixty minutes postinjection a whole-body PET/CT scan was conducted with an emission time of 3 min per bed position. The lesions which were categorized as local recurrence, bone lesion and lymph node metastasis in the early images, were compared with the late images in terms of number of lesions detected and SUVmax values. Results: 68Ga-PSMA-I&T PET/CT was positive in 23 of 35 patients (65.7%). A pathological uptake was observed in the prostatic bed site, in the pelvic lymph nodes, and in the bones in 17 patients (48.5%), 12 patients (34.2%), and 13 patients (37.1%), respectively. In one patient, focal pathological increased uptake in the prostatic bed with a SUVmax value of 5.8 was detected but this lesion disappeared in the late images. The average SUVmax values of the lesions in the prostatic bed were 13.7 ± 12.1 versus 26.3 ± 23.8 in the 5 min and 60 min studies respectively (p < 0.001). In one patient, the pathological uptake in the lymph node in the early study cleared in the late study, whereas in another accumulation of activity was detected in a pelvic lymph node in the late study, while there was no lymph node detected in the early study. The average SUVmax values of the lymph nodes were 12.1 ± 8.8 versus 26.3 ± 22.6 in the 5 min and 60 min studies respectively (p < 0.001). The average SUVmax values of the bone lesions were 11.4 ± 6.9 versus 15 ± 10.7 in the 5 min and 60 min studies respectively. Conclusion: Our study is the first in the literature to evaluate the impact of adding an early static pelvic image to the 68Ga-PSMA-I&T scan, in the detection rate of the lesions. Although there was no marked discordance between the 2 sets of images, the addition of an early image to the imaging protocol of 68Ga-PSMA-I&T scan would increase the efficacy of detection of malignant lesions in the pelvis, which might show rapid clearance and has the risk of being masked by the urinary system activity.
关键词： Prostate-specific membrane antigen,68Ga-PSMA-I&T,PET/CT,Lymph node metastases,Prostate cancer
更新于2025-09-23 15:22:29
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Modular medical imaging agents based on azidea??alkyne Huisgen cycloadditions: Synthesis and prea??clinical evaluation of 18Fa??labeled PSMAa??tracers for prostate cancer imaging.
摘要： The seminal contribution of Rolf Huisgen to develop the [3+2]-cycloaddition of 1,3-dipolar compounds, its azide-alkyne variant has established itself as the key step in numerous organic syntheses and bioorthogonal processes in materials science and chemical biology. In the present study, the copper(I)-catalyzed azide-alkyne cycloaddition was applied for the development of a modular molecular platform for medical imaging of the prostate specific membrane antigen (PSMA), using positron emission tomography. This process is shown from molecular design, through synthesis automation and in vitro studies, all the way to preclinical in vivo evaluation of fluorine-18– labeled PSMA-targeting ‘F-PSMA-MIC’ radiotracers (t? = 109.7 min). Preclinical data indicate that the modular PSMA-scaffold has similar binding affinity and imaging properties to the clinically used [68Ga]PSMA-11. Furthermore, we demonstrated that targeting the arene-binding in PSMA, facilitated through the [3+2]-cycloaddition, can improve binding affinity, which was rationalized by molecular modeling. The here presented PSMA-binding scaffold potentially facilitates easy coupling to other medical imaging moieties, enabling future developments of new modular imaging agents.
关键词： prostate specific membrane antigen,positron emission tomography,fluorine-18,azide-alkyne Huisgen cycloaddition,modular imaging agents
更新于2025-09-23 15:19:57
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Metal-labeled Aptamers as Novel nanoprobes for Imaging Mass Cytometry Analysis
摘要： Imaging mass cytometry (IMC) is an emerging imaging technology that exploits the multiplexed analysis capabilities of the CyTOF mass cytometer to make spatially resolved measurements for tissue sections. In a comprehensive view of tissue composition and marker distribution, recent developments of IMC require highly sensitive, multiplexed assays. Approaching the sensitivity of the IMC technique, we designed a novel type of biocompatible metal-labeled aptamer nanoprobe (MAP), named 167Er-A10-3.2. The small molecular probe was synthesized by conjugating 167Er-polymeric pentetic acid (167Er-DTPA) with an RNA aptamer A10-3.2. For demonstration, 167Er-A10-3.2 was applied for observing protein spatial distribution on prostatic epithelium cell of paraffin embedded Prostatic adenocarcinoma (PaC) tissue sections by IMC technology. The 167Er-A10-3.2 capitalizes on the ability of aptamer to specifically bind target cancer cells, as well as the small size of 167Er-A10-3.2 can accommodate multiple aptamer binding antigen labeled at high density. The detection signal of 167Er-A10-3.2 probe was 3-fold higher than that of PSMA antibody probe for a targeted cell under lower temperature epitope retrieval (37°C) of PaC tissue. Furthermore, we successfully demonstrated the simultaneously staining ability of aptamer probes in IMC analysis. The successful imaging acquisition using aptamers probes in IMC technology may offer opportunity for the diagnosis of malignancies in the future.
关键词： imaging mass cytometry,prostate specific membrane antigen,molecular probe,metal labeled aptamer
更新于2025-09-23 15:19:57
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Integration of PSMA-targeted PET imaging into the armamentarium for detecting clinically significant prostate cancer
摘要： To explore the current state of using prostate-specific membrane antigen (PSMA)-targeted PET imaging to aid in the diagnosis of clinically significant prostate cancer. Prostate-specific antigen screening remains controversial, as it is associated with the underdetection of clinically significant prostate cancer as well as the overdetection and subsequent overtreatment of clinically insignificant disease. A diagnostic test that can accurately assess the presence of clinically significant prostate cancer and avoid detection of low-risk tumors is needed. Multiparametric magnetic resonance imaging (mpMRI) can aid in the detection of clinically significant prostate cancer and can be used with fusion-based biopsy platforms to target biopsies to specific lesions. However, there are several limitations of mpMRI including a modest negative predictive value for high-grade cancer. PSMA-targeted PET imaging has shown promise as a noninvasive test to aid in the detection of clinically significant prostate cancer while providing anatomical information to guide targeted biopsies. PSMA-targeted PET in combination with mpMRI offers a higher degree of diagnostic accuracy for imaging localized prostate cancer than either modality alone. PSMA-targeted PET imaging can aid in the identification of men with clinically significant prostate cancer. Further research is needed to determine the full potential of PSMA-targeted imaging in both the detection and treatment of localized prostate cancer.
关键词： focal therapy,MRI/ultrasound fusion,prostate-specific membrane antigen,prostate cancer,targeted biopsy
更新于2025-09-10 09:29:36
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Past and Present of Imaging Modalities Used for Prostate Cancer Diagnosis: Androgen Receptor Targeted Imaging of Prostate Cancer as a Future Modality for Early, Rapid and Efficient Diagnosis
摘要： Background: Prostate cancer is the second most prevailing cancer among men worldwide. In the most cases, prostate cancer is slowly progressing, whereas, in some cases, it is a rapidly progressing disease leading to the significantly high mortality rate. Thus, there is still demand for prostate-specific imaging in order to provide image-guided early diagnosis and for the provision of patient-specific therapy. Discussion: Besides discussing traditional diagnostic approaches, this review illustrates a perspective on prostate cancer imaging summarizing current imaging approaches with a special focus on Prostate Specific Membrane Antigen (PSMA), Bombesin (BN) and Androgen Receptor (AR) targeted imaging using Positron Emission Tomography (PET) and Single Positron Emission Computed Tomography (SPECT) based on 99mTc and other radiotracers. Here, the prostate biology is reconsidered for nuclear imaging as future modality for early, rapid and efficient diagnosis of prostate cancer. Conclusion: Future direction in prostate cancer imaging involves the development of androgen receptor based imaging using nonsteroidal antiandrogen agent for early diagnosis of prostate cancer.
关键词： single photon emission computed tomography,Prostate cancer,patient-specific therapy,radiotracer,positron-emission tomography,prostate-specific membrane antigen
更新于2025-09-09 09:28:46
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Assessment of 68Ga-PSMA-11 PET positivity predictive factors in prostate cancer
摘要： Purpose: Positron emission tomography (PET) studies with 68Ga-PSMA-11 (68Ga-HBED-CC-PSMA) have earned the attention of researchers, due to overexpression of PSMA in the tumoral tissues of prostate cancer. Our aim was to analyze the potential benefit of this radiotracer in the biochemical relapse of prostate cancer. Material and methods: This retrospective analysis included 53 studies, performed on 50 male prostate cancer patients referred due to biochemical recurrence. In all cases, previous imaging techniques were negative or inconclusive. Results: Of the 53 studies, 36 (68%) were positive. Significant differences were found between the positive and negative PET groups in Gleason’s scale, PSA levels, PSAdt, late acquisition and the administration of androgen deprivation therapy during treatment (p < .05). Regarding PSA levels, 10 (48%) of the 21 patients with PSA < 1 ng/ml, obtained a pathological PET result. When the PSAdt was below six months, 86.7% of the patients obtained an abnormal PET. In the multivariate analysis, only Gleason’s scale was associated independently with an abnormal PET result. Conclusions: 68Ga-PSMA-11 PET shows a high disease detection rate in patients where other techniques showed negative or doubtful images. Almost 50% of patients with prostate cancer biochemical recurrence and low PSA levels (<1 ng/ml) have active disease on 68Ga-PSMA-11 PET, precisely where other radiotracers lack sensitivity.
关键词： Prostate-specific membrane antigen,68Ga-PSMA-11,Prostate cancer,Positron emission tomography
更新于2025-09-09 09:28:46
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SERS-Based Quantification of PSMA in Tissue Microarrays Allows Effective Stratification of Patients with Prostate Cancer
摘要： Prostate specific membrane antigen (PSMA), a type II membrane protein, is an attractive biomarker that has been validated clinically for the diagnosis of prostate cancer. In this study, we developed surface-enhanced Raman scattering (SERS) nanoprobes for PSMA detection and quantification at the single-cell level on prostate cancer cells. The cells were targeted employing SERS nanoprobes that consisted of gold nanostars functionalized with PSMA aptamer molecules. We were able to quantify picomolar concentrations of soluble PSMA protein and used the resulting calibration curve to estimate the expression of PSMA on the surface of the prostate cancer cell, LNCaP, at the single-cell level. Importantly, we employed these SERS tags to stratify prostate cancer patients by assessing PSMA expression in tissues contained in a prostate tissue microarray. The stratification results clearly correlated PSMA expression to recommended therapy groups, rendering the described method as an effective tool to aid in designing personalized therapeutic protocols. Benchmarking detection sensitivity against immunofluorescence staining and comparing stratification results obtained with the two methods allowed us to validate our novel approach against standard practices. On the basis of these results, we confirm the validity of PSMA as an effective biomarker for prostate cancer patient evaluation and propose SERS-based diagnostic techniques as integrative methods for the assessment of disease stage and the identification of effective therapeutic protocols.
关键词： aptamer,tissue microarray,surface-enhanced Raman scattering,PSMA,Prostate specific membrane antigen,SERS,nanoprobes,prostate cancer,biomarker,gold nanostars
更新于2025-09-04 15:30:14