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4. PSMA PET/CT: joint EANM procedure guideline/SNMMI procedure standard for prostate cancer imaging 2.0.

Author

Fendler, Wolfgang P, Eiber, Matthias, Beheshti, Mohsen, Bomanji, Jamshed, Calais, Jeremie, Ceci, Francesco, Cho, Steve Y, Fanti, Stefano, Giesel, Frederik L, Goffin, Karolien, Haberkorn, Uwe, Jacene, Heather, Koo, Phillip J, Kopka, Klaus, Krause, Bernd J, Lindenberg, Liza, Marcus, Charles, Mottaghy, Felix M, Oprea-Lager, Daniela E, Osborne, Joseph R, Piert, Morand, Rowe, Steven P, Schöder, Heiko, Wan, Simon, Wester, Hans-Jürgen, Hope, Thomas A, and Herrmann, Ken

Subjects
Humans, Prostatic Neoplasms, Gallium Radioisotopes, Edetic Acid, Oligopeptides, Male, Positron Emission Tomography Computed Tomography, Guideline, PET, PSMA, Prostate cancer, Restaging, Staging, Biomedical Imaging, Urologic Diseases, Aging, Prostate Cancer, Cancer, Other Physical Sciences, Clinical Sciences, Nuclear Medicine & Medical Imaging
Abstract

Here we aim to provide updated guidance and standards for the indication, acquisition, and interpretation of PSMA PET/CT for prostate cancer imaging. Procedures and characteristics are reported for a variety of available PSMA small radioligands. Different scenarios for the clinical use of PSMA-ligand PET/CT are discussed. This document provides clinicians and technicians with the best available evidence, to support the implementation of PSMA PET/CT imaging in research and routine practice.

Published
2023

18. Biodistribution and Radiation Dosimetry for a Probe Targeting Prostate-Specific Membrane Antigen for Imaging and Therapy

Author

Herrmann, Ken, Bluemel, Christina, Weineisen, Martina, Schottelius, Margret, Wester, Hans-Jürgen, Czernin, Johannes, Eberlein, Uta, Beykan, Seval, Lapa, Constantin, Riedmiller, Hubertus, Krebs, Markus, Kropf, Saskia, Schirbel, Andreas, Buck, Andreas K, and Lassmann, Michael

Subjects
Biomedical and Clinical Sciences, Clinical Sciences, Oncology and Carcinogenesis, Bioengineering, Biomedical Imaging, Aging, Cancer, Urologic Diseases, Radiation Oncology, Prostate Cancer, Aged, Antigens, Surface, Bone Marrow, Edetic Acid, Gallium Isotopes, Gallium Radioisotopes, Glutamate Carboxypeptidase II, Humans, Kidney, Male, Middle Aged, Oligopeptides, Positron-Emission Tomography, Prostatic Neoplasms, Radiometry, Radiopharmaceuticals, Salivary Glands, Spleen, Tissue Distribution, Whole Body Imaging, PET, PSMA, Ga-68, dosimetry, prostate cancer, 68Ga, Nuclear Medicine & Medical Imaging, Clinical sciences
Abstract

UnlabelledProstate-specific membrane antigen (PSMA) is a promising target for diagnosis and treatment of prostate cancer. EuK-Subkff-(68)Ga-DOTAGA ((68)Ga-PSMA Imaging & Therapy [PSMA I&T]) is a recently introduced PET tracer for imaging PSMA expression in vivo. Whole-body distribution and radiation dosimetry of this new probe were evaluated.MethodsFive patients with a history of prostate cancer were injected intravenously with 91-148 MBq of (68)Ga-PSMA I&T (mean ± SD, 128 ± 23 MBq). After an initial series of rapid whole-body scans, 3 static whole-body scans were acquired at 1, 2, and 4 h after tracer injection. Time-dependent changes of the injected activity per organ were determined. Mean organ-absorbed doses and effective doses were calculated using OLINDA/EXM.ResultsInjection of 150 MBq of (68)Ga-PSMA I&T resulted in an effective dose of 3.0 mSv. The kidneys were the critical organ (33 mGy), followed by the urinary bladder wall and spleen (10 mGy each), salivary glands (9 mGy each), and liver (7 mGy).Conclusion(68)Ga-PSMA I&T exhibits a favorable dosimetry, delivering organ doses that are comparable to (kidneys) or lower than those delivered by (18)F-FDG.

Published
2015

22. Single Lesion on Prostate-specific Membrane Antigen-ligand Positron Emission Tomography and Low Prostate-specific Antigen Are Prognostic Factors for a Favorable Biochemical Response to Prostate-specific Membrane Antigen-targeted Radioguided Surgery in Recurrent Prostate Cancer

Author

Horn, Thomas, Krönke, Markus, Rauscher, Isabel, Haller, Bernhard, Robu, Stephanie, Wester, Hans-Jürgen, Schottelius, Margret, van Leeuwen, Fijs W.B., van der Poel, Henk G., Heck, Matthias, Gschwend, Jürgen E., Weber, Wolfgang, Eiber, Matthias, and Maurer, Tobias

Published
2019
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27. Consensus on molecular imaging and theranostics in prostate cancer

Author

Fanti, Stefano, Minozzi, Silvia, Antoch, Gerald, Banks, Ian, Briganti, Alberto, Carrio, Ignasi, Chiti, Arturo, Clarke, Noel, Eiber, Matthias, De Bono, Johann, Fizazi, Karim, Gillessen, Silke, Gledhill, Sam, Haberkorn, Uwe, Herrmann, Ken, Hicks, Rodney J, Lecouvet, Frederic, Montironi, Rodolfo, Ost, Piet, O'Sullivan, Joe M, Padhani, Anwar R, Schalken, Jack A, Scher, Howard I, Tombal, Bertrand, van Moorselaar, R Jeroen A, Van Poppel, Heindrik, Vargas, Hebert Alberto, Walz, Jochen, Weber, Wolfgang A, Wester, Hans-Jürgen, and Oyen, Wim J G

Published
2018
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28. 68Ga-PSMA I&T PET/CT for primary staging of prostate cancer

Author

Cytawa, Wojciech, Seitz, Anna Katharina, Kircher, Stefan, Fukushima, Kazuhito, Tran-Gia, Johannes, Schirbel, Andreas, Bandurski, Tomasz, Lass, Piotr, Krebs, Markus, Połom, Wojciech, Matuszewski, Marcin, Wester, Hans-Jürgen, Buck, Andreas K., Kübler, Hubert, and Lapa, Constantin

Published
2020
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29. EANM procedure guidelines for radionuclide therapy with 177Lu-labelled PSMA-ligands (177Lu-PSMA-RLT)

Author

Kratochwil, Clemens, Fendler, Wolfgang Peter, Eiber, Matthias, Baum, Richard, Bozkurt, Murat Fani, Czernin, Johannes, Delgado Bolton, Roberto C., Ezziddin, Samer, Forrer, Flavio, Hicks, Rodney J., Hope, Thomas A., Kabasakal, Levant, Konijnenberg, Mark, Kopka, Klaus, Lassmann, Michael, Mottaghy, Felix M., Oyen, Wim, Rahbar, Kambiz, Schöder, Heiko, Virgolini, Irene, Wester, Hans-Jürgen, Bodei, Lisa, Fanti, Stefano, Haberkorn, Uwe, and Herrmann, Ken

Published
2019
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30. Comparison of 68 Ga-PSMA ligand PET/CT versus conventional cross-sectional imaging for target volume delineation for metastasis-directed radiotherapy for metachronous lymph node metastases from prostate cancer

Author

Walacides, Daniel, Meier, Astrid, Knöchelmann, Anne Caroline, Meinecke, Daniele, Derlin, Thorsten, Bengel, Frank M., Ross, Tobias L., Wester, Hans-Jürgen, Derlin, Katja, Kuczyk, Markus A., von Klot, Christoph A. J., Christiansen, Hans, and Henkenberens, Christoph

Published
2019
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31. Preclinical Evaluation of Minigastrin Analogs and Proof-of-Concept [68Ga]Ga-DOTA-CCK-66 PET/CT in 2 Patients with Medullary Thyroid Cancer

Author

Günther, Thomas, primary, Holzleitner, Nadine, additional, Viering, Oliver, additional, Beck, Roswitha, additional, Wienand, Georgine, additional, Dierks, Alexander, additional, Pfob, Christian H., additional, Bundschuh, Ralph A., additional, Kircher, Malte, additional, Lapa, Constantin, additional, and Wester, Hans-Jürgen, additional

Published
2023
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35. Imaging of chemokine receptor CXCR4 expression in culprit and nonculprit coronary atherosclerotic plaque using motion-corrected [68Ga]pentixafor PET/CT

Author

Derlin, Thorsten, Sedding, Daniel G., Dutzmann, Jochen, Haghikia, Arash, König, Tobias, Napp, L. Christian, Schütze, Christian, Owsianski-Hille, Nicole, Wester, Hans-Jürgen, Kropf, Saskia, Thackeray, James T., Bankstahl, Jens P., Geworski, Lilli, Ross, Tobias L., Bauersachs, Johann, and Bengel, Frank M.

Published
2018
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38. Heterogeneity of prostate-specific membrane antigen (PSMA) and PSMA-ligand uptake detection combining autoradiography, histopathology and immunohistochemistry in primary prostate cancer

Author

Wang, Hui, primary, Remke, Marianne, additional, Horn, Thomas, additional, Schwamborn, Kristina, additional, Chen, Yiyao, additional, Steiger, Katja, additional, Weichert, Wilko, additional, Wester, Hans-Jürgen, additional, Schottelius, Margret, additional, Weber, Wolfgang, additional, and Eiber, Matthias, additional

Published
2023
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39. Preclinical Comparison of the64Cu- and68Ga-Labeled GRPR-Targeted Compounds RM2 and AMTG, as Well as First-in-Humans [68Ga]Ga-AMTG PET/CT

Author

Koller, Lena, primary, Joksch, Markus, additional, Schwarzenböck, Sarah, additional, Kurth, Jens, additional, Heuschkel, Martin, additional, Holzleitner, Nadine, additional, Beck, Roswitha, additional, von Amsberg, Gunhild, additional, Wester, Hans-Jürgen, additional, Krause, Bernd Joachim, additional, and Günther, Thomas, additional

Published
2023
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42. Systemic Radioligand Therapy with 177Lu Labeled Prostate Specific Membrane Antigen Ligand for Imaging and Therapy in Patients with Metastatic Castration Resistant Prostate Cancer

Author

Heck, Matthias M., Retz, Margitta, D'Alessandria, Calogero, Rauscher, Isabel, Scheidhauer, Klemens, Maurer, Tobias, Storz, Enno, Janssen, Friederike, Schottelius, Margret, Wester, Hans-Jürgen, Gschwend, Jürgen E., Schwaiger, Markus, Tauber, Robert, and Eiber, Matthias

Published
2016
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44. Development and Preclinical Evaluation of Radiolabeled GLP-1 Receptor Ligands and PSMA Inhibitors

Author

Wester, Hans-Jürgen (Prof. Dr.), Wester, Hans-Jürgen (Prof. Dr.);Elber, Matthias (Prof. Dr.), Felber, Veronika Barbara, Wester, Hans-Jürgen (Prof. Dr.), Wester, Hans-Jürgen (Prof. Dr.);Elber, Matthias (Prof. Dr.), and Felber, Veronika Barbara

Abstract

To investigate whether the kidney uptake of radiolabeled GLP-1 receptor ligands can be reduced, short-chained GLP-1R ligands were developed and evaluated in vitro. Furthermore, it was investigated whether the increased uptake of radiolabeled inhibitors of the prostate-specific membrane antigen (PSMA) in salivary glands can be reduced. Therefore, ligands with modifications at the urea-based inhibitor unit were synthesized and evaluated in vitro and in vivo., Um zu untersuchen, ob die Nierenaufnahme von radiomarkierten GLP-1 Rezeptorliganden verringert werden kann, wurden kurzkettige GLP-1R Liganden entwickelt und in vitro evaluiert. Des Weiteren wurde untersucht, ob die erhöhte Aufnahme von radiomarkierten Inhibitoren des prostataspezifischen Membranantigens (PSMA) in Speicheldrüsen reduziert werden kann. Dazu wurden Liganden mit Modifikationen an der ureabasierten Inhibitoreinheit synthetisiert und in vitro und in vivo evaluiert.

Published
2022

45. Novel Structural Concepts for the Development of complex-based Radiopharmaceuticals and Ligand Systems

Author

Wester, Hans-Jürgen (Prof. Dr.), Wester, Hans-Jürgen (Prof. Dr.);Eiber, Matthias (Prof. Dr.), Wurzer, Alexander Josef, Wester, Hans-Jürgen (Prof. Dr.), Wester, Hans-Jürgen (Prof. Dr.);Eiber, Matthias (Prof. Dr.), and Wurzer, Alexander Josef

Abstract

In this work, different radiohybrid ligands targeting the prostate-specific membrane antigen (PSMA) were developed. These ligands can be used for diagnosis and endoradiotherapy of prostate cancer. The developed concept allows to label the PSMA-addressing agents with either a suitable radio metal or [18F]fluorine. The optimizations led to 18F-rhPSMA-7.3, which is currently further evaluated in clinical trials for PET-imaging of prostate cancer., In dieser Arbeit wurden verschiedene radiohybride Liganden entwickelt, die das Prostataspezifische Membranantigen (PSMA) adressieren und für die Diagnose sowie die Endoradiotherapie des Prostatakarzinoms eingesetzt werden können. Das entwickelte Konzept ermöglicht dabei die PSMA-adressierenden Verbindungen entweder mit einem geeigneten Radio-Metall oder mit [18F]Fluor radioaktiv zu markieren. Die Optimierungen führten dabei zu 18F-rhPSMA-7.3, das derzeit in klinischen Studien für die PET-Bildgebung von Prostatakrebs untersucht wird.

Published
2022

47. Novel 18F-labeled Radiopharmaceuticals comprising Silicon-based Fluoride Acceptors

Author

Wester, Hans-Jürgen (Prof. Dr.), D'Alessandria, Calogero (Priv.-Doz. Dr.);Kühn, Fritz E. (Prof. Dr.), Di Carlo, Daniel, Wester, Hans-Jürgen (Prof. Dr.), D'Alessandria, Calogero (Priv.-Doz. Dr.);Kühn, Fritz E. (Prof. Dr.), and Di Carlo, Daniel

Abstract

In this dissertation, a series of 18F-labeled prostate-specific membrane antigen- (PSMA-) and folate receptor- (FR-)targeting ligands exploiting the Silicon-based Fluoride Acceptor technology were developed. As a key component, a pharmacokinetic modifier was introduced into the radiotracers to counterbalance and fine-tune the elevated lipophilicity induced by the labeling moiety. The optimization work, which also included a novel [18F]fluoride preparation technique for improved radiofluorination, led to the promising ligands [18F]siPSMA-14 and [18F]natLu-rhFolate-03., In dieser Dissertation wurden eine Serie von 18F-markierten Prostataspezifischen Membranantigen- (PSMA-) und Folatrezeptor- (FR-)gerichteten Liganden unter Verwendung Silicium-basierter Fluoridakzeptoren entwickelt. Als Schlüsselkomponente kam in den Radiotracern ein pharmakokinetischer Modifier zum Einsatz, um die durch die Markierungseinheit hervorgerufene erhöhte Lipophilie zu kompensieren und präzise einzustellen. Die Optimierungsarbeiten, welche auch ein neuartiges Verfahren zur Präparation von [18F]Fluorid für eine verbesserte Radiofluorierung umfassten, führten zu den vielversprechenden Liganden [18F]siPSMA-14 und [18F]natLu-rhFolate-03.

Published
2023

48. The Concise Guide to PHARMACOLOGY 2023/24:G protein-coupled receptors

Author

Alexander, Stephen P H, Christopoulos, Arthur, Davenport, Anthony P, Kelly, Eamonn, Mathie, Alistair A, Peters, John A, Veale, Emma L, Armstrong, Jane F, Faccenda, Elena, Harding, Simon D, Davies, Jamie A, Abbracchio, Maria Pia, Abraham, George, Agoulnik, Alexander, Alexander, Wayne, Al-Hosaini, Khaled, Bäck, Magnus, Baker, Jillian G, Barnes, Nicholas M, Bathgate, Ross, Beaulieu, Jean-Martin, Beck-Sickinger, Annette G, Behrens, Maik, Bernstein, Kenneth E, Bettler, Bernhard, Birdsall, Nigel J M, Blaho, Victoria, Boulay, Francois, Bousquet, Corinne, Bräuner-Osborne, Hans, Burnstock, Geoffrey, Caló, Girolamo, Castaño, Justo P, Catt, Kevin J, Ceruti, Stefania, Chazot, Paul, Chiang, Nan, Chini, Bice, Chun, Jerold, Cianciulli, Antonia, Civelli, Olivier, Clapp, Lucie H, Couture, Réjean, Cox, Helen M, Csaba, Zsolt, Dahlgren, Claes, Dent, Gordon, Douglas, Steven D, Dournaud, Pascal, Eguchi, Satoru, Escher, Emanuel, Filardo, Edward J, Fong, Tung, Fumagalli, Marta, Gainetdinov, Raul R, Garelja, Michael L, de Gasparo, Marc, Gerard, Craig, Gershengorn, Marvin, Gobeil, Fernand, Goodfriend, Theodore L, Goudet, Cyril, Grätz, Lukas, Gregory, Karen J, Gundlach, Andrew L, Hamann, Jörg, Hanson, Julien, Hauger, Richard L, Hay, Debbie L, Heinemann, Akos, Herr, Deron, Hollenberg, Morley D, Holliday, Nicholas D, Horiuchi, Mastgugu, Hoyer, Daniel, Hunyady, László, Husain, Ahsan, IJzerman, Adriaan P, Inagami, Tadashi, Jacobson, Kenneth A, Jensen, Robert T, Jockers, Ralf, Jonnalagadda, Deepa, Karnik, Sadashiva, Kaupmann, Klemens, Kemp, Jacqueline, Kennedy, Charles, Kihara, Yasuyuki, Kitazawa, Takio, Kozielewicz, Pawel, Kreienkamp, Hans-Jürgen, Kukkonen, Jyrki P, Langenhan, Tobias, Larhammar, Dan, Leach, Katie, Lecca, Davide, Lee, John D, Leeman, Susan E, Leprince, Jérôme, Li, Xaria X, Lolait, Stephen J, Lupp, Amelie, Macrae, Robyn, Maguire, Janet, Malfacini, Davide, Mazella, Jean, McArdle, Craig A, Melmed, Shlomo, Michel, Martin C, Miller, Laurence J, Mitolo, Vincenzo, Mouillac, Bernard, Müller, Christa E, Murphy, Philip M, Nahon, Jean-Louis, Ngo, Tony, Norel, Xavier, Nyimanu, Duuamene, O'Carroll, Anne-Marie, Offermanns, Stefan, Panaro, Maria Antonietta, Parmentier, Marc, Pertwee, Roger G, Pin, Jean-Philippe, Prossnitz, Eric R, Quinn, Mark, Ramachandran, Rithwik, Ray, Manisha, Reinscheid, Rainer K, Rondard, Philippe, Rovati, G Enrico, Ruzza, Chiara, Sanger, Gareth J, Schöneberg, Torsten, Schulte, Gunnar, Schulz, Stefan, Segaloff, Deborah L, Serhan, Charles N, Singh, Khuraijam Dhanachandra, Smith, Craig M, Stoddart, Leigh A, Sugimoto, Yukihiko, Summers, Roger, Tan, Valerie P, Thal, David, Thomas, Walter Wally, Timmermans, Pieter B M W M, Tirupula, Kalyan, Toll, Lawrence, Tulipano, Giovanni, Unal, Hamiyet, Unger, Thomas, Valant, Celine, Vanderheyden, Patrick, Vaudry, David, Vaudry, Hubert, Vilardaga, Jean-Pierre, Walker, Christopher S, Wang, Ji Ming, Ward, Donald T, Wester, Hans-Jürgen, Willars, Gary B, Williams, Tom Lloyd, Woodruff, Trent M, Yao, Chengcan, Ye, Richard D, Alexander, Stephen P H, Christopoulos, Arthur, Davenport, Anthony P, Kelly, Eamonn, Mathie, Alistair A, Peters, John A, Veale, Emma L, Armstrong, Jane F, Faccenda, Elena, Harding, Simon D, Davies, Jamie A, Abbracchio, Maria Pia, Abraham, George, Agoulnik, Alexander, Alexander, Wayne, Al-Hosaini, Khaled, Bäck, Magnus, Baker, Jillian G, Barnes, Nicholas M, Bathgate, Ross, Beaulieu, Jean-Martin, Beck-Sickinger, Annette G, Behrens, Maik, Bernstein, Kenneth E, Bettler, Bernhard, Birdsall, Nigel J M, Blaho, Victoria, Boulay, Francois, Bousquet, Corinne, Bräuner-Osborne, Hans, Burnstock, Geoffrey, Caló, Girolamo, Castaño, Justo P, Catt, Kevin J, Ceruti, Stefania, Chazot, Paul, Chiang, Nan, Chini, Bice, Chun, Jerold, Cianciulli, Antonia, Civelli, Olivier, Clapp, Lucie H, Couture, Réjean, Cox, Helen M, Csaba, Zsolt, Dahlgren, Claes, Dent, Gordon, Douglas, Steven D, Dournaud, Pascal, Eguchi, Satoru, Escher, Emanuel, Filardo, Edward J, Fong, Tung, Fumagalli, Marta, Gainetdinov, Raul R, Garelja, Michael L, de Gasparo, Marc, Gerard, Craig, Gershengorn, Marvin, Gobeil, Fernand, Goodfriend, Theodore L, Goudet, Cyril, Grätz, Lukas, Gregory, Karen J, Gundlach, Andrew L, Hamann, Jörg, Hanson, Julien, Hauger, Richard L, Hay, Debbie L, Heinemann, Akos, Herr, Deron, Hollenberg, Morley D, Holliday, Nicholas D, Horiuchi, Mastgugu, Hoyer, Daniel, Hunyady, László, Husain, Ahsan, IJzerman, Adriaan P, Inagami, Tadashi, Jacobson, Kenneth A, Jensen, Robert T, Jockers, Ralf, Jonnalagadda, Deepa, Karnik, Sadashiva, Kaupmann, Klemens, Kemp, Jacqueline, Kennedy, Charles, Kihara, Yasuyuki, Kitazawa, Takio, Kozielewicz, Pawel, Kreienkamp, Hans-Jürgen, Kukkonen, Jyrki P, Langenhan, Tobias, Larhammar, Dan, Leach, Katie, Lecca, Davide, Lee, John D, Leeman, Susan E, Leprince, Jérôme, Li, Xaria X, Lolait, Stephen J, Lupp, Amelie, Macrae, Robyn, Maguire, Janet, Malfacini, Davide, Mazella, Jean, McArdle, Craig A, Melmed, Shlomo, Michel, Martin C, Miller, Laurence J, Mitolo, Vincenzo, Mouillac, Bernard, Müller, Christa E, Murphy, Philip M, Nahon, Jean-Louis, Ngo, Tony, Norel, Xavier, Nyimanu, Duuamene, O'Carroll, Anne-Marie, Offermanns, Stefan, Panaro, Maria Antonietta, Parmentier, Marc, Pertwee, Roger G, Pin, Jean-Philippe, Prossnitz, Eric R, Quinn, Mark, Ramachandran, Rithwik, Ray, Manisha, Reinscheid, Rainer K, Rondard, Philippe, Rovati, G Enrico, Ruzza, Chiara, Sanger, Gareth J, Schöneberg, Torsten, Schulte, Gunnar, Schulz, Stefan, Segaloff, Deborah L, Serhan, Charles N, Singh, Khuraijam Dhanachandra, Smith, Craig M, Stoddart, Leigh A, Sugimoto, Yukihiko, Summers, Roger, Tan, Valerie P, Thal, David, Thomas, Walter Wally, Timmermans, Pieter B M W M, Tirupula, Kalyan, Toll, Lawrence, Tulipano, Giovanni, Unal, Hamiyet, Unger, Thomas, Valant, Celine, Vanderheyden, Patrick, Vaudry, David, Vaudry, Hubert, Vilardaga, Jean-Pierre, Walker, Christopher S, Wang, Ji Ming, Ward, Donald T, Wester, Hans-Jürgen, Willars, Gary B, Williams, Tom Lloyd, Woodruff, Trent M, Yao, Chengcan, and Ye, Richard D

Abstract

The Concise Guide to PHARMACOLOGY 2023/24 is the sixth in this series of biennial publications. The Concise Guide provides concise overviews, mostly in tabular format, of the key properties of approximately 1800 drug targets, and about 6000 interactions with about 3900 ligands. There is an emphasis on selective pharmacology (where available), plus links to the open access knowledgebase source of drug targets and their ligands (https://www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. Although the Concise Guide constitutes almost 500 pages, the material presented is substantially reduced compared to information and links presented on the website. It provides a permanent, citable, point-in-time record that will survive database updates. The full contents of this section can be found at http://onlinelibrary.wiley.com/doi/bph.16177. G protein-coupled receptors are one of the six major pharmacological targets into which the Guide is divided, with the others being: ion channels, nuclear hormone receptors, catalytic receptors, enzymes and transporters. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. The landscape format of the Concise Guide is designed to facilitate comparison of related targets from material contemporary to mid-2023, and supersedes data presented in the 2021/22, 2019/20, 2017/18, 2015/16 and 2013/14 Concise Guides and previous Guides to Receptors and Channels. It is produced in close conjunction with the Nomenclature and Standards Committee of the International Union of Basic and Clinical Pharmacology (NC-IUPHAR), therefore, providing official IUPHAR classification and nomenclature for human drug targets, where appropriate.

Published
2023

49. Preclinical comparison of [177Lu]Lu-rhPSMA-10.1 and [177Lu]Lu-rhPSMA-10.2 for endoradiotherapy of prostate cancer: biodistribution and dosimetry studies.

Author

Wurzer, Alexander, De Rose, Francesco, Fischer, Sebastian, Schwaiger, Markus, Weber, Wolfgang, Nekolla, Stephan, Wester, Hans-Jürgen, Eiber, Matthias, and D'Alessandria, Calogero

Subjects
MEDICAL dosimetry, PROSTATE cancer, SERUM albumin, EXTERNAL beam radiotherapy, STEREOISOMERS, ISOMERS
Abstract

Background: Radiohybrid PSMA-targeted ligands (rhPSMA) have been introduced as a novel platform for theranostic applications. Among a variety of rhPSMA-ligands developed for radioligand therapy, two stereoisomers [177Lu]Lu-rhPSMA-10.1 and -10.2 have been synthesized and initially characterized in preclinical experiments with the aim to provide an optimized binding profile to human serum albumin, a reduction of charge, and thus accelerated kidney excretion, and unaffected or even improved tumor uptake. As both isomers showed similar in vitro characteristics and tumor uptake at 24 h post injection in tumor bearing mice and in order to identify the isomer with the most favorable pharmacokinetics for radioligand therapy, we carried out in-depth biodistribution and dosimetry studies in tumor-bearing and healthy mice. Results: rhPSMA-10.1 and -10.2 were radiolabeled with lutetium-177 according to the established procedures of other DOTA-based PSMA ligands and displayed a high and comparable stability in all buffers and human serum (> 97%, 24 h). Biodistribution studies revealed fast clearance from the blood pool (0.3–0.6%ID/g at 1 h) and other background tissues within 48 h. Distinctive differences were found in the kidneys, where [177Lu]Lu-rhPSMA-10.1 displayed lower initial uptake and faster excretion kinetics compared to [177Lu]Lu-rhPSMA-10.2 expressed by a 1.5-fold and ninefold lower uptake value at 1 h and 24 h in healthy animals, respectively. Tumor uptake was comparable and in the range of 8.6–11.6%ID/g for both isomers over 24 h and was maintained up to 168 h at a level of 2.2 ± 0.8 and 4.1 ± 1.4%ID/g for [177Lu]Lu-rhPSMA-10.1 and [177Lu]Lu-rhPSMA-10.2, respectively. Conclusion: Our preclinical data on biodistribution and dosimetry indicate a more favorable profile of [177Lu]Lu-rhPSMA-10.1 compared to [177Lu]Lu-rhPSMA-10.2 for PSMA-targeted radioligand therapy. [177Lu]Lu-rhPSMA-10.1 shows fast kidney clearance kinetics resulting in excellent tumor-to-organ ratios over a therapy relevant time course. Meanwhile, [177Lu]Lu-rhPSMA-10.1 is currently being investigated in clinical phase I/II studies in patients with mCRPC (NCT05413850), in patients with high-risk localized PC (NCT06066437, Nautilus Trial) and after external beam radiotherapy (NCT06105918). [ABSTRACT FROM AUTHOR]

Published
2024
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