Review
Chemistry, Medicinal
Lexi Gower-Fry, Travis Kronemann, Andreas Dorian, Yinglan Pu, Carolin Jaworski, Carmen Waengler, Peter Bartenstein, Leonie Beyer, Simon Lindner, Klaus Jurkschat, Bjoern Waengler, Justin J. Bailey, Ralf Schirrmacher
Summary: Incorporation of silicon fluoride acceptor (SiFA) moieties into various molecules has enhanced the generation of F-18 radiopharmaceuticals for medical imaging. The efficient isotopic exchange radiofluorination process, along with the enhanced in vivo stability of [F-18]SiFA, makes it a suitable strategy for fluorine-18 incorporation. This review emphasizes the clinical applicability of [F-18]SiFA-labeled compounds and discusses significant radiotracers currently in clinical use.
Review
Chemistry, Multidisciplinary
Kaiqiang Zhang, Wanru Feng, Zhaobiao Mou, Jiayin Chen, Xiaoqun Tang, Zijing Li
Summary: This review provides an overview of F-18 labeling methods in aqueous media, focusing on reaction mechanisms, the effect of water, and applications in the development of F-18 radiopharmaceuticals.
CHEMISTRY-A EUROPEAN JOURNAL
(2023)
Article
Chemistry, Medicinal
Nils Walter, Jan Bertram, Birte Drewes, Victor Bahutski, Marco Timmer, Markus B. Schuetz, Felicia Kraemer, Felix Neumaier, Heike Endepols, Bernd Neumaier, Boris D. Zlatopolskiy
Summary: A protocol for radiolabeling of aryl fluorosulfates using ultrafast isotopic exchange has been developed and optimized. This method allows for efficient labeling of low nanomolar amounts of aryl fluorosulfates without the need for azeotropic drying, base addition, and HPLC purification. The labeled compounds demonstrated sufficient stability in vivo and showed promise as tracers for visualizing specific molecular expressions.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Justin J. Bailey, Melinda Wuest, Michael Wagner, Atul Bhardwaj, Carmen Waengler, Bjoern Waengler, John F. Valliant, Ralf Schirrmacher, Frank Wuest
Summary: PET imaging using Ga-68 and F-18 radiotracers targeting PSMA has gained significant interest, with novel F-18-labeled SiFA-bearing PSMA inhibitors being synthesized and tested for their in vitro binding. Among the compounds, [F-18]SiFA-Asp2-PEG3-PSMA showed the highest tumor uptake in LNCaP tumors. Increased molar activity led to a significant increase in tumor uptake, and the SiFA-isotopic exchange chemistry offers a promising method for clinical translation.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Radiology, Nuclear Medicine & Medical Imaging
Kailin Qiao, Xueting Qin, Shuai Fu, Jiazhong Ren, Jing Jia, Xinying Hu, Yuanyuan Tao, Shuanghu Yuan, Yuchun Wei
Summary: The uptake of [F-18]AlF-NOTA-FAPI-04 and [F-18]FDG imaging tracers varies in malignant and inflammatory lung lesions, with lower uptake observed in inflammatory lesions. This difference in uptake can be valuable for distinguishing between malignancy and various inflammatory findings.
EUROPEAN RADIOLOGY
(2023)
Article
Neurosciences
Xiang Kong, Song Luo, Yun Fei Wang, Gui Fen Yang, Guang Ming Lu, Long Jiang Zhang
Summary: Neuroinflammation is a key factor in the pathogenesis of hepatic encephalopathy, with TSPO upregulation providing a molecular target for imaging. The study using BDL rats found that both [18F]PBR146 and [18F]DPA-714 can quantitatively evaluate neuroinflammation in hepatic encephalopathy models, with specific brain regions showing abnormal uptake and correlating with behavioral alterations.
FRONTIERS IN NEUROSCIENCE
(2021)
Article
Clinical Neurology
Alessandro Dinoto, Marta Cheli, Milos Ajcevic, Franca Dore, Carmelo Crisafulli, Maja Ukmar, Arianna Sartori, Paolo Manganotti
Summary: In this study, two patients with LE underwent 18F-FDG-PET and ASL MRI scans for comparison. The results showed that ASL imaging was able to detect the two main 18F-FDG-PET patterns of altered metabolism, demonstrating strong concordance between the two techniques in LE patients.
NEUROLOGICAL SCIENCES
(2021)
Article
Clinical Neurology
Hiroshi Yamauchi, Shinya Kagawa, Kuninori Kusano, Miki Ito, Chio Okuyama
Summary: This pilot study with a small sample size suggests that cerebral hypoperfusion may be associated with increased tau deposition in patients with atherosclerotic internal carotid artery or middle cerebral artery disease.
Article
Multidisciplinary Sciences
Ksenia Lisova, Jia Wang, Tibor Jacob Hajagos, Yingqing Lu, Alexander Hsiao, Arkadij Elizarov, R. Michael van Dam
Summary: This study presents a simple and efficient method for synthesizing clinically-relevant batches of [F-18]FET and [F-18]FBB using a microfluidic radiosynthesizer, with the potential for batch-on-demand synthesis of F-18-labeled radiopharmaceuticals for human use. The method demonstrated high production efficiency and suitability for human use, with quality control testing passed for all batches.
SCIENTIFIC REPORTS
(2021)
Article
Chemistry, Medicinal
Ayoung Pyo, Misun Yun, Boreum Song, Seong-Young Kwon, Jung-Joon Min, Dong-Yeon Kim
Summary: In this study, 18F-labeled procainamide (PCA) was synthesized and evaluated for its potential as a PET imaging agent for melanoma detection. The results showed that 18F-PCA exhibited high melanoma uptake and could be a promising tool for direct melanoma detection using PET imaging.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2023)
Article
Anesthesiology
Christina Mueller, Yu-Hua D. Fang, Chloe Jones, Jonathan E. Mcconathy, Fabio Raman, Suzanne E. Lapi, Jarred W. Younger
Summary: This study found increased binding of the translocator protein radioligand in several brain regions among fibromyalgia patients. The results suggest that individuals with fibromyalgia may have higher levels of neuroinflammation than healthy controls. Additionally, the study found higher binding levels in multiple brain regions among high-affinity binders in the fibromyalgia group. The differences in the right parietal gray matter were associated with decreased quality of life, higher pain severity and interference, and cognitive problems.
Article
Biochemistry & Molecular Biology
Guolong Huang, Xiaolei Lu, Yifan Qiu, Lei Bi, Peizhen Ye, Min Yang, Yanfang Shen, Hongjun Jin, Junbin Han
Summary: A novel P2X7R targeting radiotracer was synthesized and proved to stably retain and target P2X7R in vivo without defluorination in major organs. It shows potential as a promising PET radioligand for clinical translation.
BIOORGANIC & MEDICINAL CHEMISTRY
(2022)
Article
Multidisciplinary Sciences
Ou Yamaguchi, Kyoichi Kaira, Ichiro Naruse, Yukihiro Umeda, Takeshi Honda, Satoshi Watanabe, Kosuke Ichikawa, Kazunari Tateishi, Norimitsu Kasahara, Tetsuya Higuchi, Kosuke Hashimoto, Shun Shinomiya, Yu Miura, Ayako Shiono, Atsuto Mouri, Hisao Imai, Kunihiko Iizuka, Tamotsu Ishizuka, Koichi Minato, Satoshi Suda, Hiroshi Kagamu, Keita Mori, Ichiei Kuji, Nobuhiko Seki
Summary: This study aimed to investigate the clinical relevance of F-18-FDG PET/CT compared to CT in predicting the response to PD-1 blockade in the early phase. The results showed that metabolic assessment by MTV or TLG was superior to morphological changes on CT for predicting the therapeutic response and survival.
SCIENTIFIC REPORTS
(2022)
Article
Oncology
Xinfeng Lin, Yingjie Li, Shuailiang Wang, Yan Zhang, Xuetao Chen, Maomao Wei, Hua Zhu, Aiwen Wu, Zhi Yang, Xuejuan Wang
Summary: This study compared the diagnostic performance of [Ga-68]Ga-FAPI-04 PET/CT and [F-18]F-FDG PET/CT in primary and metastatic colorectal cancer lesions, and found that [Ga-68]Ga-FAPI-04 showed potential as a novel PET/CT tracer. The use of this tracer improved the staging of colorectal cancer and led to optimization or adjustment of treatment decisions.
FRONTIERS IN ONCOLOGY
(2023)
Article
Medicine, General & Internal
Cecile Tissot, Joseph Therriault, Peter Kunach, Andrea L. Benedet, Tharick A. Pascoal, Nicholas J. Ashton, Thomas K. Karikari, Stijn Servaes, Firoza Z. Lussier, Mira Chamoun, Dana L. Tudorascu, Jenna Stevenson, Nesrine Rahmouni, Nina Margherita Poltronetti, Vanessa Pallen, Gleb Bezgin, Min Su Kang, Sulantha S. Mathotaarachchi, Yi-Ting Wang, Jaime Fernandez Arias, Pamela Cristina Lukasewicz Ferreira, Joao Pedro Ferrari-Souza, Eugeen Vanmechelen, Kaj Blennow, Henrik Zetterberg, Serge Gauthier, Pedro Rosa-Neto
Summary: This study investigated the agreement between [F-18]MK6240 tau-PET, plasma pTau181, and pTau231 in Alzheimer's disease. The findings suggest that these biomarkers reflect different stages of tau progression and can be useful in diagnosing and evaluating the disease stage.
Article
Cardiac & Cardiovascular Systems
Mathias Johannes Zacherl, Andrei Todica, Carmen Wngler, Ralf Schirrmacher, Mohammad Ali Hajebrahimi, Joachim Pircher, Xiang Li, Simon Lindner, Matthias Brendel, Peter Bartenstein, Steffen Massberg, Stefan Brunner, Sebastian Lehner, Marcus Hacker, Bruno C. Huber
Summary: The study shows the feasibility of noninvasive molecular imaging of cardiac CXCR4 expression using a novel, murine-based, and specific (68)Ga-mCXCL12 tracer both ex vivo and in vivo, with consistent results.
JOURNAL OF NUCLEAR CARDIOLOGY
(2021)
Review
Chemistry, Medicinal
Lexi Gower-Fry, Travis Kronemann, Andreas Dorian, Yinglan Pu, Carolin Jaworski, Carmen Waengler, Peter Bartenstein, Leonie Beyer, Simon Lindner, Klaus Jurkschat, Bjoern Waengler, Justin J. Bailey, Ralf Schirrmacher
Summary: Incorporation of silicon fluoride acceptor (SiFA) moieties into various molecules has enhanced the generation of F-18 radiopharmaceuticals for medical imaging. The efficient isotopic exchange radiofluorination process, along with the enhanced in vivo stability of [F-18]SiFA, makes it a suitable strategy for fluorine-18 incorporation. This review emphasizes the clinical applicability of [F-18]SiFA-labeled compounds and discusses significant radiotracers currently in clinical use.
Article
Chemistry, Medicinal
Marco Maspero, Clelia Dallanoce, Bjoern Waengler, Carmen Waengler, Ralph Huebner
Summary: In this study, we describe and explain the aberrant behavior in receptor binding profile of a fluorescein-based multimodal imaging agent for gastrin releasing peptide receptor (GRPR) visualization by elucidating a chelating mechanism on sodium ions of its fluorescent dye moiety.
Article
Chemistry, Medicinal
Justin J. Bailey, Melinda Wuest, Michael Wagner, Atul Bhardwaj, Carmen Waengler, Bjoern Waengler, John F. Valliant, Ralf Schirrmacher, Frank Wuest
Summary: PET imaging using Ga-68 and F-18 radiotracers targeting PSMA has gained significant interest, with novel F-18-labeled SiFA-bearing PSMA inhibitors being synthesized and tested for their in vitro binding. Among the compounds, [F-18]SiFA-Asp2-PEG3-PSMA showed the highest tumor uptake in LNCaP tumors. Increased molar activity led to a significant increase in tumor uptake, and the SiFA-isotopic exchange chemistry offers a promising method for clinical translation.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Benedikt Judmann, Diana Braun, Ralf Schirrmacher, Bjoern Wangler, Carmen Wangler, Gert Fricker
Summary: The study suggests that GE11-based monovalent and small homomultivalent radiotracers have limited affinity for EGFR and are not promising for further development as radioligands.
Article
Chemistry, Medicinal
Helen Damerow, Bjoern Waengler, Ralf Schirrmacher, Gert Fricker, Carmen Waengler
Summary: Different chelators can be used to introduce [Ga-68]Ga3+ into receptor-specific peptidic carriers for radiotracer imaging, and the choice of chelating agent significantly affects the in vivo pharmacokinetics of the radiopeptides. A backbone-functionalized variant of the chelator CB-DO2A, CB-DO2A-GA, was developed as a valuable alternative to established chelating agents for Ga-68-radiolabeling of peptides. It was found that CB-DO2A-GA required harsher reaction conditions for Ga-68-incorporation compared to DOTA, NODA-GA, and DOTA-GA.
Article
Pharmacology & Pharmacy
Helen Damerow, Xia Cheng, Valeska von Kiedrowski, Ralf Schirrmacher, Bjoern Waengler, Gert Fricker, Carmen Waengler
Summary: Zr-89 is a highly favorable positron emitter for immuno-PET imaging. Complexation of the Zr-89(4+) ion with desferrioxamine B is commonly used to introduce the ion into antibodies, but the complexes have limited kinetic inertness. Therefore, new chelators, such as DFO* and 3,4,3-(LI-1,2-HOPO), have been developed. Comparisons between these chelators have shown that DFO* is the most suitable candidate for stable Zr-89 labeling of antibodies for clinical translation.
Article
Chemistry, Medicinal
Benedikt Judmann, Bjorn Waengler, Ralf Schirrmacher, Gert Fricker, Carmen Waengler
Summary: This study investigated whether certain peptidic radiotracers can specifically target EGFR-positive tumors. The results showed that these radiotracers failed to demonstrate the ability to specifically target EGFR-positive tumors, suggesting the need for further exploration of alternative radiotracers.
Review
Chemistry, Medicinal
Carolin Jaworski, Petar Iliev, Carmen Waengler, Bjoern Waengler, Brent Page, Ralf Schirrmacher, Justin J. Bailey
Summary: Trk inhibitors are significant in personalized medicine as they target specific genetic alterations, leading to improved treatment outcomes for cancer patients. Efforts are being made to enhance efficacy and reduce toxicity.
EXPERT OPINION ON THERAPEUTIC PATENTS
(2023)
Article
Radiology, Nuclear Medicine & Medical Imaging
Ali Asgar Attarwala, Deni Hardiansyah, Chiara Romano, Luis David Jimenez-Franco, Mareike Roscher, Bjoern Waengler, Gerhard Glatting
Summary: The performance characteristics of the SPECT sub-system S102 of the ALBIRA II PET/SPECT/CT for the 80 mm field of view were analyzed, showing favorable sensitivity and spatial resolution for small animal imaging.
ANNALS OF NUCLEAR MEDICINE
(2021)
