Editorial Material
Radiology, Nuclear Medicine & Medical Imaging
Inki Lee, Ilhan Lim, Kyo Chul Lee, Hye Jin Kang, Sang Moo Lim
Summary: Cu-64-DOTA-rituximab PET/CT was performed on two patients with B-cell non-Hodgkin lymphoma, and it was found to be more sensitive in detecting lesions compared to F-18-FDG PET/CT. It was confirmed that there was no discernible Cu-64-DOTA-rituximab uptake in the tumor other than lymphoma. Cu-64-DOTA-rituximab PET/CT could be a powerful tool for the diagnosis and monitoring treatment response of lymphoma due to its ability to image CD20 expression.
CLINICAL NUCLEAR MEDICINE
(2023)
Article
Radiology, Nuclear Medicine & Medical Imaging
Avik Chakraborty, Arpit Mitra, Sudeep Sahu, Megha Tawate, Sangita Lad, Sutapa Kamaldeep, Sutapa Rakshit, Trupti Upadhye Bannore, Sujay Gaikwad, Geetanjali Dhotre, Mukti Kanta Ray, Archana Damle, Sandip Basu, Sharmila Banerjee
Summary: The development of humanized monoclonal antibodies (MAbs) with Lutetium-177 ([Lu-177]Lu3+) has revolutionized targeted therapy for various cancers. [Lu-177]Lu-DOTA-Rituximab and [Lu-177]Lu-DOTA-Trastuzumab have shown improved efficacy in lymphoma and breast cancer treatment. This study optimized a single protocol for the formulation of clinical doses, achieving high radiochemical yields and purities for [Lu-177]Lu-DOTA-Rituximab and [Lu-177]Lu-DOTA-Trastuzumab.
MOLECULAR IMAGING AND BIOLOGY
(2023)
Article
Radiology, Nuclear Medicine & Medical Imaging
Cuicui Li, Jun Liu, Xu Yang, Qi Yang, Wenpeng Huang, Mingyu Zhang, Dandan Zhou, Rong Wang, Jianhua Gong, Qingfang Miao, Lei Kang, Jigang Yang
Summary: This study developed Cu-64/Lu-177-labeled anti-Trop2 monoclonal antibody for PET imaging and RIT application in pancreatic cancer tumor models. The results showed that Cu-64-labeled antibody had good accumulation ability in tumor models, and Lu-177-labeled antibody could inhibit the growth of Trop2-overexpressed tumors.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
(2022)
Article
Medicine, Research & Experimental
Jingyun Ren, Mengxin Xu, Junyi Chen, Jie Ding, Peipei Wang, Li Huo, Fang Li, Zhibo Liu
Summary: Development of a highly tumor-selective αPD-L1 antibody through PET imaging screening and Lu-177 radiolabeling for PD-L1-targeted radioimmunotherapy and radiation-synergized immunotherapy resulted in significantly better therapeutic effect than immunotherapy or RIT alone in upregulating anti-tumor immunity in the tumor microenvironment. The strategy showed a strong synergistic effect with αPD-L1 checkpoint blockade therapy without observed side effects in the mouse model.
Article
Radiology, Nuclear Medicine & Medical Imaging
Frederik A. Verburg, Erik de Blois, Stijn Koolen, Mark W. Konijnenberg
Summary: This study investigated the dosimetric effect of substituting Lu-177 with Tb-161 in targeted radionuclide therapy (TRT) using the registered tracers DOTA-TATE and PSMA-617. The results showed that substituting Lu-177 with Tb-161 increased the delivered dose to tumor tissue, but activity conversion was necessary to ensure non-target dose limits were not exceeded.
Article
Chemistry, Multidisciplinary
Lei Kang, Cuicui Li, Zachary T. Rosenkrans, Nan Huo, Zhao Chen, Emily B. Ehlerding, Yan Huo, Carolina A. Ferreira, Todd E. Barnhart, Jonathan W. Engle, Rongfu Wang, Dawei Jiang, Xiaojie Xu, Weibo Cai
Summary: CD38 is identified as a specific marker for lymphoma, and Zr-89/Lu-177-labeled daratumumab shows potential in immunoPET imaging and radioimmunotherapy for lymphoma in preclinical models.
Article
Medicine, Research & Experimental
Nutthanit Thumrongsiri, Paweena Dana, Rand Bawab, Prattana Tanyapanyachon, Chaichana Treetidnipa, Nattika Saengkrit, Sith Sathornsumetee
Summary: The study demonstrated that liposomes conjugated with RTX and modified with tween-80 can effectively penetrate the blood-brain barrier, targeting lymphoma cells in the CNS. The Lip/RTX showed comparable antitumor activity to free RTX and inhibited tumor aggressiveness. Systemic administration of Lip/RTX significantly prolonged the survival of mice with intracranial lymphoma xenografts.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Article
Oncology
Tabassom Mohajershojai, Douglas Spangler, Saloni Chopra, Fredrik Y. Frejd, Paul J. Yazaki, Marika Nestor
Summary: Combination therapy with onalespib and Lu-177-DOTA-M5A has demonstrated promising therapeutic effects for colorectal cancer treatment. The combination treatment showed enhanced tumor growth suppression and increased apoptosis, achieving comparable or superior effects with a lower dose of Lu-177-DOTA-M5A. This approach has the potential to expand the patient population that can benefit from targeted treatment.
Article
Multidisciplinary Sciences
Mario Bunse, Janina Pfeilschifter, Julia Bluhm, Maria Zschummel, Jara J. Joedicke, Anthea Wirges, Helen Stark, Vivien Kretschmer, Markus Chmielewski, Wolfgang Uckert, Hinrich Abken, Joerg Westermann, Armin Rehm, Uta E. Hoepken
Summary: The study demonstrates that CAR-T cells targeting CXCR5 effectively inhibit tumor growth by depleting both B cells and follicular T helper cells in lymphoma models, suggesting a promising treatment strategy for nodal B-NHLs.
NATURE COMMUNICATIONS
(2021)
Article
Oncology
Takaaki Fujimura, Yoriko Yamashita-Kashima, Natsumi Kawasaki, Shigeki Yoshiura, Naoki Harada, Yasushi Yoshimura
Summary: Retreatment with obinutuzumab in combination with chemotherapeutic agents is effective in CD20-positive obinutuzumab-induced direct-cell-death-resistant cells, showing significant antitumor effects in mouse xenograft models.
MOLECULAR CANCER THERAPEUTICS
(2021)
Article
Oncology
Rouslan Kotchetkov, Ian R. Drennan, David Susman, Erica DiMaria, Lauren Gerard, Derek Nay, Anca Prica
Summary: This study compared the safety and efficacy of BR therapy in elderly and younger patients. The results showed that elderly patients were more likely to experience treatment delays and dose reductions, but the disease control outcome was similar between the two groups.
INTERNATIONAL JOURNAL OF CANCER
(2023)
Article
Radiology, Nuclear Medicine & Medical Imaging
Chul-Hee Lee, Ilhan Lim, Sang-Keun Woo, Wook Kim, Kwang Il Kim, Kyo Chul Lee, Kanghyon Song, Sang Moo Lim
Summary: The study evaluated the radiation dosimetry of alpha-emitter Ac-225-DOTA-rituximab using Monte Carlo simulation of Cu-64-DOTA-rituximab. Results showed specific binding of tumors with Cu-64-DOTA-rituximab and significantly higher tumor uptake of Ac-225-DOTA-rituximab compared to Cu-64-DOTA-rituximab, indicating potential for targeted alpha therapy in lymphoma.
ANNALS OF NUCLEAR MEDICINE
(2021)
Article
Hematology
Natsumi Kawasaki, Yukari Nishito, Yasushi Yoshimura, Shigeki Yoshiura
Summary: This study investigated the molecular basis of the combination therapy of Polatuzumab vedotin (Pola) with Rituximab (Rit) for the treatment of diffuse large B-cell lymphoma (DLBCL). The results showed that Pola treatment increased CD20 expression and sensitivity to Rit-induced cytotoxicity in Pola-refractory cells, and this combination efficacy depended on the phosphorylation of AKT and ERK. Furthermore, Pola treatment increased CD20 expression and demonstrated enhanced antitumor activity in Pola-refractory xenografted tumors when combined with Rit.
BRITISH JOURNAL OF HAEMATOLOGY
(2022)
Article
Radiology, Nuclear Medicine & Medical Imaging
Ayca Londalen, Johan Blakkisrud, Mona-Elisabeth Revheim, Ulf Erik Madsbu, Jostein Dahle, Arne Kolstad, Caroline Stokke
Summary: This study aimed to investigate the therapeutic effect of Lu-177-lilotomab satetraxetan in patients with non-Hodgkin lymphoma, and found no correlation between tumor-absorbed doses and changes in FDG PET or ceCT parameters in treatment-induced changes after diagnosis.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
(2021)
Article
Radiology, Nuclear Medicine & Medical Imaging
Lorain Geenen, Julie Nonnekens, Mark Konijnenberg, Sarah Baatout, Marion De Jong, An Aerts
Summary: Peptide receptor radionuclide therapy (PRRT) is used for treating GEP-NETs but may cause nephrotoxic effects. Lowering the absorbed dose to the kidneys can help to increase the therapeutic window.
NUCLEAR MEDICINE AND BIOLOGY
(2021)
Review
Oncology
Emanuel Christ, Kwadwo Antwi, Melpomeni Fani, Damian Wild
ENDOCRINE-RELATED CANCER
(2020)
Article
Endocrinology & Metabolism
Julie Refardt, Johannes Hofland, Antwi Kwadwo, Guillaume P. Nicolas, Christof Rottendurger, Melpomeni Fani, Damian Wild, Emanuel Christ
Summary: Neuroendocrine neoplasms (NENs) are a heterogeneous group of tumors with diverse potential therapeutic targets, such as SST2 and GLP-1R, as well as newly identified targets. By targeting these receptors, diagnostic and therapeutic interventions can be carried out, with further research needed to explore additional potential treatments.
REVIEWS IN ENDOCRINE & METABOLIC DISORDERS
(2021)
Article
Radiology, Nuclear Medicine & Medical Imaging
Rosalba Mansi, Karim Abid, Guillaume P. Nicolas, Luigi Del Pozzo, Eric Grouzmann, Melpomeni Fani
Article
Oncology
Mairene Coto-Llerena, Caner Ercan, Venkatesh Kancherla, Stephanie Taha-Mehlitz, Serenella Eppenberger-Castori, Savas D. Soysal, Charlotte K. Y. Ng, Martin Bolli, Markus von Flue, Guillaume P. Nicolas, Luigi M. Terracciano, Melpomeni Fani, Salvatore Piscuoglio
FRONTIERS IN ONCOLOGY
(2020)
Article
Chemistry, Medicinal
Melpomeni Fani, Viktoria Weingaertner, Petra Kolenc Peitl, Rosalba Mansi, Raghuvir H. Gaonkar, Piotr Garnuszek, Renata Mikolajczak, Doroteja Novak, Urban Simoncic, Alicja Hubalewska-Dydejczyk, Christine Rangger, Piriya Kaeopookum, Clemens Decristoforo
Summary: Recently, radiolabelled antagonists targeting somatostatin receptors subtype 2 (SST2) in neuroendocrine neoplasms demonstrated certain superior properties over agonists. Within the ERA-PerMED project TECANT two Tc-99m-Tetramine (N4)-derivatized SST2 antagonists (TECANT-1 and TECANT-2) were studied for the selection of the best candidate for clinical translation. The preclinical study provided the basis of selection of [Tc-99m]Tc-TECANT-1 for clinical translation of the first Tc-99m-based SST2 antagonist.
Review
Oncology
Valentina Ambrosini, Jolanta Kunikowska, Eric Baudin, Lisa Bodei, Catherine Bouvier, Jaume Capdevila, Marta Cremonesi, Wouter W. de Herder, Clarisse Dromain, Massimo Falconi, Melpomeni Fani, Stefano Fanti, Rodney J. Hicks, Levent Kabasakal, Gregory Kaltsas, Val Lewington, Silvia Minozzi, Michela Cinquini, Kjell Oberg, Wim J. G. Oyen, Dermot O'Toole, Marianne Pavel, Philippe Ruszniewski, Aldo Scarpa, Jonathan Strosberg, Anders Sundin, David Taieb, Irene Virgolini, Damian Wild, Ken Herrmann, James Yao
Summary: Nuclear medicine plays a crucial role in managing neuroendocrine neoplasms, using techniques such as peptide receptor radionuclide therapy and positron emission tomography. Recommendations from the European Association of Nuclear Medicine provide valuable guidance for the diagnosis and treatment of NETs.
EUROPEAN JOURNAL OF CANCER
(2021)
Article
Chemistry, Medicinal
Raghuvir Haridas Gaonkar, Fabius Wiesmann, Luigi Del Pozzo, Lisa McDougall, Sandra Zanger, Renata Mikolajczak, Rosalba Mansi, Melpomeni Fani
Summary: [Tc-99m]Tc-HYNIC-TOC is a commonly used radiotracer for SST-expressing tumors, but recent studies have shown that Tc-99m-labeled SST antagonists may have better diagnostic efficacy. Different spacers were investigated to improve the affinity of HYNIC conjugates with SST2 antagonists. The use of Ahx as a spacer significantly improved the cellular uptake of the conjugates, demonstrating its potential for imaging agents.
Article
Chemistry, Multidisciplinary
Rosalba Mansi, Melpomeni Fani
Summary: The Division of Radiopharmaceutical Chemistry at the University Hospital Basel has made significant progress in developing peptide-based radiopharmaceuticals, covering the entire spectrum of development process from bench-to-bedside. Their research plays an important role in targeting and treating tumors effectively.
Article
Radiology, Nuclear Medicine & Medical Imaging
Damian Wild, Kwadwo Antwi, Melpomeni Fani, Emanuel R. Christ
Summary: GLP-1R PET/CT imaging is more sensitive in detecting benign insulinomas and nesidioblastosis compared to other imaging modalities, leading to recommendations in clinical guidelines. Prospective studies have shown the clinical relevance and potential for GLP-1R imaging to replace invasive localization methods for insulinomas.
JOURNAL OF NUCLEAR MEDICINE
(2021)
Article
Chemistry, Medicinal
Rosalba Mansi, Pascale Plas, Georges Vauquelin, Melpomeni Fani
Summary: Comparing the binding kinetics and cellular mechanisms of [Lu-177]Lu-OPS201 and [Lu-177]Lu-DOTA-TATE, the study found that [Lu-177]Lu-OPS201 recognized more receptor binding sites, with faster association and slower dissociation, explaining the improved therapeutic efficacy of [Lu-177]Lu-OPS201 compared to [Lu-177]Lu-DOTA-TATE.
Article
Oncology
Melpomeni Fani, Rosalba Mansi, Guillaume P. Nicolas, Damian Wild
Summary: Somatostatin receptors (SSTs) are highly expressed in neuroendocrine tumors and neuroendocrine neoplasms, making them favorable molecular targets. Radiolabeled SST agonists, such as Ga-68-DOTA-TOC and Ga-68-DOTA-TATE, are used for PET/CT imaging and play an important role in staging and restaging these tumors. New developments, including the use of SST2 antagonists and more cytotoxic radioisotopes, show promise in enhancing diagnostic accuracy and therapeutic efficacy for SST-expressing tumors. However, further research is needed to determine if these new developments can surpass the established radiolabeled SST analogs and beta(-)-emitter PRRT.
Article
Radiology, Nuclear Medicine & Medical Imaging
Jacopo Millul, Lennart Koepke, Gaonkar Raghuvir Haridas, Konstantin M. J. Sparrer, Rosalba Mansi, Melpomeni Fani
Summary: This study compared different strategies for targeting fibroblast activation protein-alpha (FAP) using radioligands. It was found that dimerization and cyclic peptide structures could prolong tumor residence time, while the outcome of the albumin binding strategy depended on the albumin binding moiety. These findings suggest that FAP-targeting radioligands have therapeutic potential, but the choice of strategy should depend on specific conditions.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
(2023)
Article
Chemistry, Medicinal
Raghuvir Haridas Gaonkar, Yannik Tim Schmidt, Rosalba Mansi, Yasser Almeida-Hernanadez, Elsa Sanchez-Garcia, Mirja Harms, Jan Muench, Melpomeni Fani
Summary: The peptide fragment of human serum albumin, EPI-X4, was investigated as a scaffold for CXCR4-targeted radiotheragnostics. Ligand-7 (JM#21 derivative) showed the best CXCR4-tumor targeting and low uptake in non-targeted organs. These findings support the feasibility of using EPI-X4-based radioligands for CXCR4 targeting with ligand-7 as a lead candidate for further optimization.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Pharmacology & Pharmacy
Doroteja Novak, Barbara Janota, Anton Amadeus Hoermann, Agnieszka Sawicka, Marko Kroselj, Alicja Hubalewska-Dydejczyk, Melpomeni Fani, Renata Mikolajczak, Petra Kolenc, Clemens Decristoforo, Piotr Garnuszek
Summary: The broad availability and cost-effectiveness of Mo-99/Tc-99m generators worldwide have supported the use and development of novel Tc-99m-labelled radiopharmaceuticals. This study aimed to provide a reliable method for the facile preparation of a Tc-99m-labelled SST2 antagonist, [Tc-99m]Tc-TECANT-1, in a hospital radiopharmacy setting for a multi-centre clinical trial. A freeze-dried three-vial kit was successfully developed to ensure successful and reproducible on-site preparation of the radiopharmaceutical for human use shortly before administration.
Article
Medicine, Research & Experimental
Joana Grand-Guillaume, Rosalba Mansi, Raghuvir H. Gaonkar, Sandra Zanger, Melpomeni Fani, Philippe J. Eugster, Maja Beck Popovic, Eric Grouzmann, Karim Abid
Summary: Pharmacological induction of transporters can enhance the uptake of mIBG, improving imaging and therapy of NB and PHEO cells both in vitro and in vivo.
JOURNAL OF TRANSLATIONAL MEDICINE
(2023)