A5008109921- Radiopharmaceutical Chemistry and Applications
- Prostate Cancer Treatment and Research
- Medical Imaging Techniques and Applications
- Fluorine in Organic Chemistry
- Peptidase Inhibition and Analysis
- Cerebrovascular and Carotid Artery Diseases
- Synthesis of β-Lactam Compounds
- Cancer, Hypoxia, and Metabolism
- Angiogenesis and VEGF in Cancer
- Neuroendocrine Tumor Research Advances
- Cancer, Lipids, and Metabolism
- Click Chemistry and Applications
- Chemical Synthesis and Analysis
- Boron Compounds in Chemistry
- Orthopaedic implants and arthroplasty
- Dementia and Cognitive Impairment Research
- Neuroblastoma Research and Treatments
- Cancer Immunotherapy and Biomarkers
- Nanoparticle-Based Drug Delivery
- Prostate Cancer Diagnosis and Treatment
- Carbohydrate Chemistry and Synthesis
- Ferrocene Chemistry and Applications
- Alzheimer's disease research and treatments
- Lung Cancer Treatments and Mutations
- Organometallic Complex Synthesis and Catalysis
University Hospital Cologne
2014-2025
University of Cologne
2015-2025
Forschungszentrum Jülich
2016-2025
Stadtwerke Jülich (Germany)
2021
Max Planck Institute for Metabolism Research
2014-2016
Cologne Business School
2014
Max Planck Society
2013
Gallium-68 (Ga-68)-labeled tracers for imaging expression of the prostate-specific membrane antigen (PSMA) such as [68Ga]Ga-PSMA-HBED-CC have already demonstrated high potential detection recurrent prostate cancer. However, compared to Ga-68, a labeling with fluorine-18 (F-18) would offer advantages respect availability, production amount, and image resolution. [18F]DCFPyL is promising F-18-labeled candidate PSMA-positron emission tomography (PET) that has been recently introduced. In...
Abstract Two novel methods for copper‐mediated aromatic nucleophilic radiofluorination were recently reported. Evaluation of these reveals that, although both are efficient in small‐scale experiments, they inoperative the production positron emission tomography (PET) tracers. Since high base content turned out to be responsible low radiochemical conversions, a “low base” protocol has been developed which affords 18 F‐labeled arenes from diaryliodonium salts and aryl pinacol boronates...
A novel radiofluorination procedure using only precursor and [<sup>18</sup>F]fluoride without the need for azeotropic drying, base other ingredients was developed.
<sup>18</sup>F-prostate-specific membrane antigen (PSMA)-1007 is excreted mainly through the liver. We benchmarked performance of <sup>18</sup>F-PSMA-1007 against 3 renally PSMA tracers. <b>Methods:</b> Among 668 patients, we selected 27 in whom PET/CT results obtained with <sup>68</sup>Ga-PSMA-11, <sup>18</sup>F-DCFPyL (2-(3-(1-carboxy-5-[(6-[<sup>18</sup>F]fluoro-pyridine-3-carbonyl)-amino]-pentyl)-ureido)-pentanedioic acid), or <sup>18</sup>F-JK-PSMA-7 (JK, Juelich-Koeln) were interpreted...
Prostate-specific membrane antigen (PSMA), expressed by most prostate carcinomas (PCa), is a promising target for PCa imaging. The application of PSMA-specific <sup>18</sup>F-labeled PET probes such as <sup>18</sup>F-DCFPyL and <sup>18</sup>F-PSMA-1007 considerably improved the accuracy tumor detection. However, there remains need further improvements in sensitivity specificity. aim this study was development highly selective specific PSMA with enhanced imaging properties, comparison...
Abstract Background In clinical practice, several radiopharmaceuticals are used for PSMA-PET imaging, each with distinct biodistribution patterns. This may impact treatment decisions and outcomes, as eligibility PSMA-directed radioligand therapy is usually assessed by comparing tumoral uptake to normal liver a reference. this study, we aimed compare tracer intraindividually in various reference regions including liver, parotid gland spleen well the respective tumor-to-background ratios (TBR)...
In a recent contribution of Scott et al., the substrate scope Cu-mediated nucleophilic radiofluorination with [18F]KF for preparation 18F-labeled arenes was extended to aryl- and vinylstannanes. Based on these findings, potential this reaction production clinically relevant positron emission tomography (PET) tracers investigated. To end, radiofluorodestannylation using trimethyl(phenyl)tin as model re-evaluated respect different parameters. The resulting labeling protocol applied...
Background: The radiotracer [18F]JK-PSMA-7, a prostate cancer imaging agent for positron emission tomography (PET), was previously synthesized by indirect radiofluorination using an 18F-labeled active ester as prosthetic group, which had to be isolated and purified before it could linked the pharmacologically Lys-urea-Glu motif. Although this procedure automated on two-reactor modules like GE TRACERLab FX2N (FXN) afford tracer in modest radiochemical yields (RCY) of 18-25%, is unsuitable...
The spatial extent of amyloid, tau, and neurodegeneration, derived from PET imaging, has higher diagnostic performance for cognitive impairment severity compared with standardized uptake value ratios.
Background: The exhalation of radioiodine following therapy (RIT) presents a challenge in radiation protection, though the mechanisms remain incompletely understood. Previous studies have indicated that is predominantly exhaled an organically bound form humans. Methods: This study investigates chemical composition and amounts radioiodine, as well impact thyroid-targeted pharmacological interventions, using controlled mouse model. Female Balb/c mice (25 g) were administered oral doses (0.1,...
In preclinical trials, the recently developed tracer 2-methoxy-<sup>18</sup>F-DCFPyL (<sup>18</sup>F-JK-prostate-specific membrane antigen [PSMA]-7) has shown favorable properties regarding clinical performance and radiochemical accessibility. The aim of this study was to evaluate utility <sup>18</sup>F-JK-PSMA-7 for PET/CT imaging patients with prostate cancer. <b>Methods:</b> an Institutional Review Board–approved pilot study, initial directly compared <sup>68</sup>Ga-PSMA-11 in a group 10...
We investigated the whole-body distribution and radiation dosimetry of [18F]-JK-PSMA-7, a novel 18F-labeled PSMA-ligand for PET/CT imaging prostate cancer.Ten patients with cancer biochemical recurrence or radiologic evidence metastatic diseases were examined 329-384 MBq (mean 359 ± 17 MBq) [18F]-JK-PSMA-7. Eight sequential positron emission tomography (PET) scans acquired from 20 min to 3 h after injection IRB approval. The kidneys, liver, lungs, spleen, salivary glands segmented into...
Cerebral glucose hypometabolism is a typical hallmark of Alzheimer's disease (AD), usually associated with ongoing neurodegeneration and neuronal dysfunction. However, underlying pathological processes are not fully understood reproducibility in animal models well established. The aim the present study was to investigate regional interrelation measured by [18F]FDG positron emission tomography (PET) various molecular targets AD pathophysiology using PET tracers [18F]PI-2620 for tau...
In 2022, the American Food and Drug Administration European Medicines Agency approved [177Lu]Lu-PSMA-617 (PLUVICTO™, Novartis AG, Basel, Switzerland) for radionuclide therapy with prostate-specific membrane antigen (PSMA) ligands in metastatic prostate cancer. Theranostics require appropriate patients to be identified by positron emission tomography (PET) prior therapy, usually employing [68Ga]Ga-PSMA-11. Alternatively, several 18F-labelled PSMA-PET tracers are available may increasingly...
Abstract Owing to their broad spectrum of biological activities and low toxicity, β‐lactams are attractive lead structures for the design novel molecular probes. However, synthesis positron emission tomography (PET)‐isotope‐labelled has not yet been reported. Herein, we describe simple preparation radiofluorinated by using fast Kinugasa reaction between 18 F‐labelled nitrone [ F]‐ 1 alkynes different reactivity. Additionally, fused were obtained through a cyclic 7 with 6 , b . Radiochemical...
Introduction [68Ga]PSMA-HBED-CC and [18F]DCFPyL show a high potential for the detection of recurrent prostate cancer. While 18F-based tracers have several advantages in availability image resolution, their sensitivity skeleton might be impaired by released [18F]fluoride due to its bone affinity. In turn, chemically unbound trivalent 68Ga also accumulate osseous tissue, cases occupied binding sites plasma proteins thereby influence signal. Methods A comparison average SUV was performed 17...
The application of toxic solvents and additives is inevitable for most the described protocols 18 F-labeling. Herein, a novel "green" procedure nucleophilic aromatic radiofluorination highly activated (hetero)aromatic substrates in pure EtOH described. Using this method series F-labeled (hetero)arenes have been synthesized radiochemical yields (RCYs) up to 97%.
Preliminary studies on a radioactive antibody against the neural cell adhesion molecule (NCAM) demonstrated significant accumulation of [131I]I-ERIC1 in neuroblastoma tumor cells mice. This study aims to validate therapeutic efficacy and potential adverse effects these immunoconjugates (RICs) neuroblastoma-bearing To determine highest tolerated dose, healthy SCID mice received 1 22 MBq [131I]I-ERIC1, with survival time measured. Tumor response was evaluated by administering 0.8 assessing...
Abstract A convenient method for the preparation of hitherto unknown ([ 18 F]fluorophenyl)acetylenes F]FPAs) using Seyferth–Gilbert homologation is reported. The novel building blocks were efficiently prepared from easily accessible [ F]fluorobenzaldehydes by Bestmann–Ohira reagent. High radiochemical yields and excellent purities achieved within only 20 min reaction time; 2‐ 4‐[ F]FPAs applied to prepare radiofluorinated heterocycles different cycloaddition cross‐coupling reactions....
Surface modification of nanocarriers enables selective attachment to specific molecular targets within a complex biological environment.
Abstract The short- and long-term success of intravascular stents depends on a proper re-endothelialisation after the intervention-induced endothelial denudation. aim this study was to evaluate potential in vivo molecular imaging glutamate carboxypeptidase II (GCPII; identical with prostate-specific membrane antigen PSMA) expression as marker re-endothelialisation. Fifteen Sprague Dawley rats underwent unilateral balloon angioplasty common carotid artery (CCA). Positron emission tomography...
PSMA imaging is frequently used for monitoring of androgen deprivation therapy (ADT) in prostate cancer. In a previous study, [18F]-JK-PSMA-7 exhibited favorable properties tumor localization after biochemical recurrence. this retrospective we evaluated the performance under ADT. We examined 70 patients (first cohort) with increasing or detectable PSA values ADT (PSA < 2 ng/ml 21/70 patients). further analyzed 58 independent levels ADT, who were imaged [68Ga]PSMA-11 [18F]DCFPyL (second...
The recent implementation of PET with prostate specific membrane antigen (PSMA)-specific radiotracers into the clinical practice has resulted in significant improvement accuracy detection carcinoma (PCa). PSMA-expression ganglia been regarded as an important pitfall carcinoma-PET diagnostics but not found any practical use for diagnosis or therapy. We explored this phenomenon and demonstrated applicability peripheral healthy rats surrogates small PSMA positive lesions preclinical evaluation...