[68Ga]Ga-PSMA-11 in prostate cancer: a comprehensive review (original) (raw)
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Gallium-68–Labeled Prostate-Specific Membrane Antigen–11 PET/CT of Prostate and Nonprostate Cancers
American Journal of Roentgenology, 2019
OBJECTIVE.-The purpose of this study is to provide a concise summary of the current experience with 68 Ga-labeled prostate-specific membrane antigen (PSMA)-11 imaging of prostate and nonprostate malignancies and benign conditions. CONCLUSION.-PSMA is overexpressed in prostate cancer and in the neovasculature of many other malignancies. The relevance of PSMA as a biologic target, coupled with advances in the design, synthesis, and evaluation of PSMA-based radionuclides for imaging and therapy, is anticipated to play a major role in patient care.
68Ga-PSMA PET/CT and PET/MRI in high-risk prostate cancer patients
Nuclear Medicine Communications, 2018
Treatment of high-risk prostate cancer (HRPCa) is challenging. Local staging and metastatic evaluation are important for the patient management. Recently, prostatespecific membrane antigen (PSMA)-based imaging modalities such as PSMA PET/CT and PET/MRI have received significant attention for detection of recurrent prostate cancer sites with elevated prostate-specific antigen levels, after therapy. Current evidence suggests that these imaging modalities may also have a role for the management of patients with HRPCa. In this review, we discuss PSMA-based imaging modalities in the management of patients with HRPCa. Nucl Med Commun
Clinical perspectives of PSMA PET/MRI for prostate cancer
Clinics (Sao Paulo, Brazil), 2018
Prostate cancer imaging has become an important diagnostic modality for tumor evaluation. Prostate-specific membrane antigen (PSMA) positron emission tomography (PET) has been extensively studied, and the results are robust and promising. The advent of the PET/magnetic resonance imaging (MRI) has added morphofunctional information from the standard of reference MRI to highly accurate molecular information from PET. Different PSMA ligands have been used for this purpose including 68gallium and 18fluorine-labeled PET probes, which have particular features including spatial resolution, imaging quality and tracer biodistribution. The use of PSMA PET imaging is well established for evaluating biochemical recurrence, even at low prostate-specific antigen (PSA) levels, but has also shown interesting applications for tumor detection, primary staging, assessment of therapeutic responses and treatment planning. This review will outline the potential role of PSMA PET/MRI for the clinical asses...
Diagnostic Challenges in Prostate Cancer and 68Ga-PSMA PET Imaging: A Game Changer?
Asian Pacific journal of cancer prevention : APJCP, 2017
Prostate cancer (PC) is the most frequent solid tumor in men and the third most common cause of cancer mortality among men in developed countries. Current imaging modalities like ultrasound (US), computerized tomography (CT), magnetic resonance imaging (MRI) and choline based positron emission (PET) tracing have disappointing sensitivity for detection of nodal metastasis and small tumor recurrence. This poses a diagnostic challenge in staging of intermediate to high risk PC and restaging of patients with biochemical recurrence (PSA >0.2 ng/ml). Gallium-68 labeled prostate specific membrane antigen (68Ga-PSMA) PET imaging has now emerged with a higher diagnostic yield. 68Ga-PSMA PET/CT or PET/MRI can be expected to offer a one-stop-shop for staging and restaging of PC. PSMA ligands labeled with alpha and beta emitters have also shown promising therapeutic efficacy for nodal, bone and visceral metastasis. Therefore a PSMA based theranostics approach for detection, staging, treatmen...
Journal of Nuclear Medicine, 2016
In recent years, several radiotracers targeting the prostate-specific membrane antigen (PSMA) have been introduced. Some of them have had a high clinical impact on the treatment of patients with prostate cancer. However, the number of 18 F-labeled tracers addressing PSMA is still limited. Therefore, we aimed to develop a radiofluorinated molecule resembling the structure of therapeutic PSMA-617. Methods: The nonradioactive reference compound PSMA-1007 and the precursor were produced by solid-phase chemistry. The radioligand 18 F-PSMA-1007 was produced by a 2-step procedure with the prosthetic group 6-18 F-fluoronicotinic acid 2,3,5,6-tetrafluorophenyl ester. The binding affinity of the ligand for PSMA and its internalization properties were evaluated in vitro with PSMA-positive LNCaP (lymph node carcinoma of the prostate) cells. Further, organ distribution studies were performed with mice bearing LNCaP and PC-3 (prostate cancer cell line; PSMA-negative) tumors. Finally, small-animal PET imaging of an LNCaP tumorbearing mouse was performed. Results: The identified ligand had a binding affinity of 6.7 6 1.7 nM for PSMA and an exceptionally high internalization ratio (67% 6 13%) in vitro. In organ distribution studies, high and specific tumor uptake (8.0 6 2.4 percentage injected dose per gram) in LNCaP tumor-bearing mice was observed. In the small-animal PET experiments, LNCaP tumors were clearly visualized. Conclusion: The radiofluorinated PSMA ligand showed promising characteristics in its preclinical evaluation, and the feasibility of prostate cancer imaging was demonstrated by small-animal PET studies. Therefore, we recommend clinical transfer of the radioligand 18 F-PSMA-1007 for use as a diagnostic PET tracer in prestaging and monitoring of prostate cancer.
Cancers
Prostate cancer is the second most common cancer type in men globally. Although the prognosis for localized prostate cancer is good, no curative treatments are available for metastatic disease. Better diagnostic methods could help target therapies and improve the outcome. Prostate-specific membrane antigen (PSMA) is a transmembrane glycoprotein that is overexpressed on malignant prostate tumor cells and correlates with the aggressiveness of the disease. PSMA is a clinically validated target for positron emission tomography (PET) imaging-based diagnostics in prostate cancer, and during recent years several therapeutics have been developed based on PSMA expression and activity. The expression of PSMA in prostate cancer can be very heterogeneous and some metastases are negative for PSMA. Determinants that dictate clinical responses to PSMA-targeting therapeutics are not well known. Moreover, it is not clear how to manipulate PSMA expression for therapeutic purposes and develop rational...
World journal of nuclear medicine
The (68)Ga-prostate-specific membrane antigen ( (68)Ga-PSMA) has been recently developed to be used, as a ligand, in positron emission tomography/computed tomography (PET/CT) prostate cancer imaging, to detect prostate disease. The main objective of this review was to collect data and findings from other studies and articles to assess, theoretically, if (68)GA-PSMA PET/CT is a more appropriate prostate cancer diagnostic technique in comparison with others available such as CT, (18)F-fluoro-2-deoxyglucose PET/CT, or (18)F-fluoromethylcholine ( (18)F-choline) PET/CT. For that purpose, PubMed, the online scientific articles' database, was consulted where the keywords "PSMA" and "PET" were used to find relevant articles. The clinicaltrials.gov, clinical…
Molecules
The aim of this work is to compare [68Ga]Ga-PSMA-11 and [18F]PSMA-1007 PET/CT as imaging agents in patients with prostate cancer (PCa). Comparisons were made by evaluating times and costs of the radiolabeling process, imaging features including pharmacokinetics, and impact on patient management. The analysis of advantages and drawbacks of both radioligands might help to make a better choice based on firm data. For [68Ga]Ga-PSMA-11, the radiochemical yield (RCY) using a low starting activity (L, average activity of 596.55 ± 37.97 MBq) was of 80.98 ± 0.05%, while using a high one (H, average activity of 1436.27 ± 68.68 MBq), the RCY was 71.48 ± 0.04%. Thus, increased starting activities of [68Ga]-chloride negatively influenced the RCY. A similar scenario occurred for [18F]PSMA-1007. The rate of detection of PCa lesions by Positron Emission Tomography/Computed Tomography (PET/CT) was similar for both radioligands, while their distribution in normal organs significantly differed. Furthe...
68Ga-Labeled Inhibitors of Prostate-Specific Membrane Antigen (PSMA) for Imaging Prostate Cancer
Journal of Medicinal Chemistry, 2010
Gallium-68 is a generator-produced radionuclide for positron emission tomography (PET) that is being increasingly used for radiolabeling of tumor-targeting peptides. Compounds [ 68 Ga]3 and [ 68 Ga]6 are high-affinity, urea-based inhibitors of the prostate-specific membrane antigen (PSMA) that were synthesized in decay-uncorrected yields ranging from 60-70% and radiochemical purities of more than 99%. Compound [ 68 Ga]3 demonstrated 3.78 ± 0.90 percent injected dose per gram of tissue (%ID/g) within PSMA+ PIP tumor at 30 min post-injection, while [ 68 Ga]6 showed a two hour PSMA+ PIP tumor uptake value of 3.29 ± 0.77%ID/g. Target (PSMA+ PIP) to nontarget (PSMA− flu) ratios were 4.6 and 18.3, respectively, at those time points. Both compounds delineated tumor clearly by small animal PET. The urea series of imaging agents for PSMA can be radiolabeled with 68 Ga, a cyclotron-free isotope useful for clinical PET studies, with maintenance of target specificity.