A5065878136- Radiopharmaceutical Chemistry and Applications
- Peptidase Inhibition and Analysis
- Neuroendocrine Tumor Research Advances
- Neuroblastoma Research and Treatments
- Cardiac Structural Anomalies and Repair
- Medical Imaging Techniques and Applications
- Prostate Cancer Treatment and Research
- Neuropeptides and Animal Physiology
- Lung Cancer Research Studies
- Chemical Synthesis and Analysis
- Bladder and Urothelial Cancer Treatments
- Urinary and Genital Oncology Studies
- Immunotherapy and Immune Responses
- Cancer, Stress, Anesthesia, and Immune Response
- Mesoporous Materials and Catalysis
- Lung Cancer Treatments and Mutations
- Mass Spectrometry Techniques and Applications
- Surface Chemistry and Catalysis
- Cancer Immunotherapy and Biomarkers
- Lanthanide and Transition Metal Complexes
- Medical Imaging and Pathology Studies
- Porphyrin and Phthalocyanine Chemistry
- Esophageal Cancer Research and Treatment
- Ubiquitin and proteasome pathways
- DNA and Nucleic Acid Chemistry
Deutsche Klinik für Diagnostik
2023
Johannes Gutenberg University Mainz
2013-2021
Fibroblast activation protein (FAP) is a proline selective serine protease that overexpressed in tumor stroma and lesions of many other diseases are characterized by tissue remodeling. In 2014, most potent FAP-inhibitor (referred to as UAMC1110) with low nanomolar FAP-affinity high selectivity toward related enzymes such prolyl oligopeptidase (PREP) the dipeptidyl-peptidases (DPPs): DPP4, DPP8/9 DPP2 were developed. This inhibitor has been adopted recently groups create radiopharmaceuticals...
This study aims to retrospectively assess the safety of [225Ac]Ac-PSMA-PRLT, both as monotherapy and in combination (TANDEM) with Lutetium-177, concerning tolerance after radiopharmaceutical administration long-term safety, its impact on salivary glands’ function, overall survival (OS), follow-up duration. Between December 2020 September 2024, 89 patients received a total 151 cycles [225Ac]Ac-PSMA-PRLT. Patients at least one (n = 71) were included analysis evaluate xerostomia, well...
Radiolabeled somatostatin receptor (SSTR) agonists 68Ga-DOTA-TATE and 68Ga-DOTA-TOC are widely applied for imaging of patients with neuroendocrine tumors (NETs). Preclinical preliminary clinical evidence has indicated that SSTR antagonists perform better NET imaging. In this study, we assessed the feasibility using a new hybrid chelator DATA5m ((6-pentanoic acid)-6-(amino)methyl-1,4-diazepinetriacetate))-conjugated kit-type antagonist 68Ga-DATA5m-LM4 PET evaluated safety, biodistribution,...
691 Background: Patients with muscle invasive urothelial carcinoma (MIBC) achieving pathological complete response (pCR) upon neoadjuvant chemotherapy (NACT) have improved prognosis. Previously we did show that luminal tumors respond better to NACT (Ecke et al 2022), while chemoresistant express radioligand targets CXCR4 and FAP. First-in-Human treatment of resistant T4 MIBC using two cycles Lu 177 FAP combined one cycle pembrolizumab results in durable (Baum al, submitted). The objective...
Targeting vectors bound to a chelator represent significant fraction of radiopharmaceuticals used nowadays for diagnostic and therapeutic purposes in nuclear medicine. The use squaramides as coupling units targeting vector helps circumvent the disadvantages several common methods. This review gives an overview squaric acid diesters (SADE) linking agents. It focuses on conjugation cyclic chelators, e.g., DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid), well hybrid chelators...
Radiolabeled FAPI (fibroblast activation protein inhibitors) recently gained attention as widely applicable imaging and potential therapeutic compounds targeting CAF (cancer-associated fibroblasts) or DAF (disease-associated fibroblasts in benign disorders). Moreover, the use of has distinct advantages compared to FDG (e.g., increased sensitivity regions with high glucose metabolism, no need for fasting, rapid imaging). In this study, we wanted evaluate radiochemical synthesis clinical...
Hardly any new tracers attracted more attention in nuclear medicine the last couple of years than radiolabeled fibroblast activation protein inhibitors (FAPi's). Molecules targeting cancer-associated fibroblasts (CAFs) or disease-associated benign disorders (DAFs) gave rise to a class radiopharmaceuticals widely applicable for imaging and with desired use as therapeutic compounds. Despite displaying benefits diagnostic sensitivity over FDG, most FAP-targeting compounds today's clinical...
The L-lysine urea-L-glutamate (KuE) represents a key motif in recent diagnostic and therapeutic radiopharmaceuticals targeting the prostate specific membrane antigen (PSMA). Using squaric acid moiety for coupling of KuE with radioactive label, as linker PSMA ligand seems to mimic aromatic structure naphthylalanine unit on PSMA-617. In this work, we investigate influence biological activity compound carrying three typical chelates. derivatives TRAM.SA.KuE, DOTAGA.SA.KuE NODAGA.SA.KuE were all...
We study the influence of Alizarin Red S deprotonation on molecular self-assembly at solid–liquid interface natural cleavage plane calcite immersed in aqueous solution. To elucidate adsorption details, we perform pH dependent high-resolution atomic force microscopy measurements. When is deposited onto calcite(10.4) a liquid environment an acidic 5, weakly bound, ordered islands with (3 × 3) superstructure are observed. A sharp structural transition revealed when increasing above 8. Above...
Radiolabeled somatostatin subtype 2 receptor (SST2R)-antagonists have shown advantageous profiles for cancer theranostics compared with agonists. On the other hand, newly introduced hybrid chelator (6-pentanoic acid)-6-(amino)methyl-1,4-diazepinetriacetate (DATA5m) rapidly binds Ga-68 (t1/2: 67.7 min) at much lower temperature, thus allowing quick access to "ready-for-injection" [68Ga]Ga-tracers in hospitals. We herein introduce [68Ga]Ga-DATA5m-LM4 PET/CT imaging of SST2R-positive human...
Abstract DATA (6-Amino-1,4-diazapine-triacetate) and AAZTA (6-Amino-1,4-diazapine-tetracetate) chelators represent a novel approach representing hybrid-chelates: possessing significant cyclic acyclic character. It is believed that flexibility of the part facilitates rapid complexation, whilst preorganized minimizes energy barrier to complexation inhibits decomplexation processes. So far, these have been used exclusively with 44 Sc 68 Ga only. Recent results nat Cu predict high stabilities...
(1) Background: Prostate-specific membrane antigen (PSMA) has been extensively studied in the last decade. It became a promising biological target diagnosis and therapy of PSMA-expressing cancer diseases. Although there are several radiolabeled PSMA inhibitors available, search for new compounds with improved pharmacokinetic properties simplified synthesis is still ongoing. In this study, we developed ligands two different hybrid chelators modified linker. Both have displayed profile. (2)...
Abstract Background Fibroblast activation protein (FAP) is a proline selective serine protease that overexpressed in tumor stroma and lesions of many other diseases are characterized by tissue remodeling. In 2014, most potent FAP-inhibitor (referred to as UAMC1110) with low nanomolar FAP-affinity high selectivity toward related enzymes such prolyl oligopeptidase (PREP) the dipeptidyl-peptidases (DPPs): DPP4, DPP8/9 DPP2 were developed. This inhibitor has been adopted recently groups create...
550 Background: Patients with muscle invasive urothelial carcinoma achieving pathological complete response (pCR) upon neoadjuvant chemotherapy (NACT) have improved prognosis. Previously we did show that luminal tumors respond better to NACT (Ecke et al 2022), while the radioligand targets CXCR4 and FAP are found in chemoresistant, stroma-associated tumors. The objective of this study was exploit expression & for theranostic imaging treatment selected patients by instillation into...
Ziel/Aim To assess the feasibility of using a novel kit-type SSTR antagonist 68Ga-DATA5m-LM4 for PET imaging and evaluate safety, biodistribution preliminary diagnostic efficacy it in patients with metastatic neuroendocrine tumors.
Bisphosponates are an interesting molecular class and in recent years their application has found its way into radiopharmaceutical research thus imaging. In addition to great imaging of bone metastases, bisphospnate-based tracers for also have some significant drawbacks. For example, synthesis is often difficult. Additionally, this can lead complex almost impossible purification quality control. This limited the production labeling suitable widespread use a few facilities. Our squaric...
Ziel/Aim Kürzlich konnte gezeigt werden, dass bestimmte NET nur mit Antagonisten visualisiert werden können, da hier eine erhöhte Zahl Bindungsstellen vermutet wird (1). Wir zeigen hier, der SSTR(Somatostatinrezeptor)-Antagonist [68Ga]Ga-DATA5m-LM4 hoher RCY und RCP in einem vollautomatisierten Prozess markiert kann. Außerdem stellen wir erste klinische Daten von Patienten vor, die mittels PET/CT untersucht wurden.
Ziel/Aim Das Theranostikum 3BP-3940 ist ein DOTA-Konjugat eines hochaffinen, FAP-bindenden Peptides, welches in unserem Zentrum mit versch. Radionukliden (177Lu, 90Y, 225Ac) markiert wurde. 68Ga-3BP-3940 dient dabei der molekularen Bildgebung und Selektion Patienten für die Peptid-vermittelte Radiorezeptortherapie (PRRT).
Ziel/Aim The purpose of this study was to determine the feasibility using a novel FAP-targeted cyclic peptide 3BP-3940 for targeted radionuclide therapy (PTRT) and present first-in-humans results 177Lu, 90Y 225Ac labeled in end-stage cancer patients.
Ziel/Aim Das Fibroblasten-Aktivierungs-Protein (FAP) stellt ein interessantes Zielprotein für die Diagnose und molekulare Strahlentherapie verschiedener bösartiger Erkrankungen dar. Im Gegensatz zu den zumeist eingesetzten FAP-Inhibitoren (FAPIs) ist das FAP-gerichtete Motiv in 3BP-3940 Peptidgerüst, mit verschiedenen Radionukliden Bildgebung oder PTRT markiert werden kann. In dieser Studie berichten wir über bewährte Verfahren Radiomarkierung von oben genannten Radioisotopen.
Ziel/Aim Radiomarkierte FAPis haben in letzter Zeit als breit einsetzbare, bildgebende und therapeutische Radiopharmazeutika Aufmerksamkeit gewonnen. In dieser Studie zeigen wir die automatisierte Synthese von [68Ga]Ga-DATA.SA.FAPi sowie dessen erste Anwendung bei Patienten.