Rhenium-188 Labeled Radiopharmaceuticals: Current Clinical Applications in Oncology and Promising Perspectives

Lepareur, Nicolas; Lacœuille, Franck; Bouvry, Christelle; Hindré, François; Garcion, Emmanuel; Chérel, Michel; Noiret, Nicolas; Garin, Etienne; Knapp, F. F.  Russ

doi:10.3389/fmed.2019.00132

Title: Rhenium-188 Labeled Radiopharmaceuticals: Current Clinical Applications in Oncology and Promising Perspectives

Journal Article · Fri Jun 14 00:00:00 EDT 2019 · Frontiers in Medicine

DOI:https://doi.org/10.3389/fmed.2019.00132· OSTI ID:1628049

Lepareur, Nicolas ^[1]; Lacœuille, Franck ^[2]; Bouvry, Christelle ^[3]; Hindré, François ^[4]; Garcion, Emmanuel ^[4]; Chérel, Michel ^[5]; Noiret, Nicolas ^[6]; Garin, Etienne ^[1]; Knapp, F. F. Russ ^[7]

Comprehensive Cancer Center Eugène Marquis, Rennes (France); Univ. Rennes (France). Inst. NUMECAN (Nutrition, Métabolismes et Cancer)
Angers Univ. Hospital, Angers (France); Angers Univ. (France). Univ. Nantes. CRCINA (Centre de Recherche en Cancérologie et Immunologie Nantes—Angers)
Comprehensive Cancer Center Eugène Marquis, Rennes (France); Univ Rennes, Rennes (France). CNRS, ISCR (Institut des Sciences Chimiques de Rennes)
Univ. Angers (France). Univ. Nantes. CRCINA (Centre de Recherche en Cancérologie et Immunologie Nantes—Angers); Univ.Angers (France). PRIMEX (Plateforme de Radiobiologie et d’Imagerie EXperimentale)
Univ. Angers (France). Univ. Nantes. CRCINA (Centre de Recherche en Cancérologie et Immunologie Nantes—Angers); ICO (Institut de Cancérologie de l’Ouest), Comprehensive Cancer Center René Gauducheau, Saint-Herblain (France)
Univ Rennes, Rennes (France). CNRS, ISCR (Institut des Sciences Chimiques de Rennes); ENSCR (Ecole Nationale Supérieure de Chimie de Rennes), Rennes (France)
Oak Ridge National Lab. (ORNL), Oak Ridge, TN (United States). Medical Radioisotopes Program

Rhenium-188 (¹⁸⁸Re) is a high energy beta-emitting radioisotope with a short 16.9 h physical half-life, which has been shown to be a very attractive candidate for use in therapeutic nuclear medicine. The high beta emission has an average energy of 784 keV and a maximum energy of 2.12 MeV, sufficient to penetrate and destroy targeted abnormal tissues. In addition, the low-abundant gamma emission of 155 keV (15%) is efficient for imaging and for dosimetric calculations. These key characteristics identify ¹⁸⁸Re as an important therapeutic radioisotope for routine clinical use. Moreover, the highly reproducible on-demand availability of ¹⁸⁸Re from the ¹⁸⁸W/¹⁸⁸Re generator system is an important feature and permits installation in hospital-based or central radiopharmacies for cost-effective availability of no-carrier-added (NCA) ¹⁸⁸Re. Rhenium-188 and technetium-99 m exhibit similar chemical properties and represent a “theranostic pair.” Thus, preparation and targeting of ¹⁸⁸Re agents for therapy is similar to imaging agents prepared with ^99mTc, the most commonly used diagnostic radionuclide. Over the last three decades, radiopharmaceuticals based on ¹⁸⁸Re-labeled small molecules, including peptides, antibodies, Lipiodol and particulates have been reported. The successful application of these ¹⁸⁸Re-labeled therapeutic radiopharmaceuticals has been reported in multiple early phase clinical trials for the management of various primary tumors, bone metastasis, rheumatoid arthritis, and endocoronary interventions. This article reviews the use of ¹⁸⁸Re-radiopharmaceuticals which have been investigated in patients for cancer treatment, demonstrating that 188Re represents a cost effective alternative for routine clinical use in comparison to more expensive and/or less readily available therapeutic radioisotopes.

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Research Organization:: Oak Ridge National Laboratory (ORNL), Oak Ridge, TN (United States)

Sponsoring Organization:: USDOE Office of Science (SC)

Grant/Contract Number:: AC05-00OR22725

OSTI ID:: 1628049

Journal Information:: Frontiers in Medicine, Vol. 6; ISSN 2296-858X

Publisher:: Frontiers Media S.A.Copyright Statement

Country of Publication:: United States

Language:: English

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Radionuclide therapy Chatal, Jean-Francois; Hoefnagel, Cornelis A. The Lancet, Vol. 354, Issue 9182 https://doi.org/10.1016/s0140-6736(99)06002-x	journal	September 1999
Uptake of the 188Re(V)-DMSA complex by cervical carcinoma cells in nude mice: pharmacokinetics and dosimetry Garcı́a-Salinas, Laura; Ferro-Flores, Guillermina; Arteaga-Murphy, Consuelo Applied Radiation and Isotopes, Vol. 54, Issue 3 https://doi.org/10.1016/s0969-8043(00)00278-5	journal	March 2001
Preparation of 188Re-labeled paper for treating skin cancer Jeong, Jae Min; Lee, Yong Jin; Kim, Eun-Hee Applied Radiation and Isotopes, Vol. 58, Issue 5 https://doi.org/10.1016/s0969-8043(03)00063-0	journal	May 2003
Preparation of 188Re-RC-160 somatostatin analog: a peptide for local/regional radiotherapy Zamora, P. O.; Marek, M. J.; (Russ) Knapp, F. F. Applied Radiation and Isotopes, Vol. 48, Issue 3 https://doi.org/10.1016/s0969-8043(96)00226-6	journal	March 1997
An alternative approach to the preparation of 188Re radiopharmaceuticals from generator-produced [188ReO4]−: efficient synthesis of 188Re(V)-meso-2,3-dimercaptosuccinic acid Bolzati, Cristina; Boschi, Alessandra; Uccelli, Licia Nuclear Medicine and Biology, Vol. 27, Issue 3 https://doi.org/10.1016/s0969-8051(00)00079-2	journal	April 2000
Effect of reaction conditions on preparations of rhenium-188 hydroxyethylidene diphosphonate complexes Lin, Wan-Yu; Hsieh, Jih-Fang; Lin, Chih-Phoon Nuclear Medicine and Biology, Vol. 26, Issue 4 https://doi.org/10.1016/s0969-8051(99)00007-4	journal	May 1999
Comparison of various rhenium-188-labeled diphosphonates for the treatment of bone metastases Hsieh, Bor-Tsung; Hsieh, Jih-Fang; Tsai, Shih-Chuan Nuclear Medicine and Biology, Vol. 26, Issue 8 https://doi.org/10.1016/s0969-8051(99)00075-x	journal	November 1999
Management of Postsurgical Recurrence of Hepatocellular Carcinoma with Rhenium 188–HDD Labeled Iodized Oil Kumar, Ajay; Srivastava, Deep N.; Bal, Chandrasekhar Journal of Vascular and Interventional Radiology, Vol. 17, Issue 1 https://doi.org/10.1097/01.rvi.0000195321.20579.f2	journal	January 2006
A comparative study of 188Re-HEDP, 186Re-HEDP, 153Sm-EDTMP and 89Sr in the treatment of painful skeletal metastases Liepe, Knut; Kotzerke, Joerg Nuclear Medicine Communications, Vol. 28, Issue 8 https://doi.org/10.1097/mnm.0b013e32825a6adc	journal	January 2007
Biodistribution and internal dosimetry of the 188Re-labelled humanized monoclonal antibody anti-epidemal growth factor receptor, nimotuzumab, in the locoregional treatment of malignant gliomas Torres, Leonel A.; Coca, Marco A.; Batista, Juan F. Nuclear Medicine Communications, Vol. 29, Issue 1 https://doi.org/10.1097/mnm.0b013e3282f1bbce	journal	January 2008
Radiolabeled Antibodies to Bacillus anthracis Toxins Are Bactericidal and Partially Therapeutic in Experimental Murine Anthrax Rivera, Johanna; Nakouzi, Antonio S.; Morgenstern, Alfred Antimicrobial Agents and Chemotherapy, Vol. 53, Issue 11 https://doi.org/10.1128/aac.01269-08	journal	August 2009
Studies on Neoplasms with the aid of Radioactive Phosphorus. i. the Total Phosphorus Metabolism of Normal and Leukemic mice 1 Lawrence, J. H.; Tuttle, L. W.; Scott, K. G. Journal of Clinical Investigation, Vol. 19, Issue 2 https://doi.org/10.1172/jci101129	journal	March 1940
Unrelated marrow transplantation for adult patients with poor-risk acute lymphoblastic leukemia: strong graft-versus-leukemia effect and risk factors determining outcome Cornelissen, Jan J.; Carston, Michael; Kollman, Craig Blood, Vol. 97, Issue 6 https://doi.org/10.1182/blood.v97.6.1572	journal	March 2001
Repeated Bone-Targeted Therapy for Hormone-Refractory Prostate Carcinoma: Randomized Phase II Trial With the New, High-Energy Radiopharmaceutical Rhenium-188 Hydroxyethylidenediphosphonate Palmedo, Holger; Manka-Waluch, Agnieska; Albers, Peter Journal of Clinical Oncology, Vol. 21, Issue 15 https://doi.org/10.1200/jco.2003.12.060	journal	August 2003
Initial Study of Radiological and Clinical Efficacy Radioembolization Using 188Re-Human Serum Albumin (HSA) Microspheres in Patients with Progressive, Unresectable Primary or Secondary Liver Cancers Pawlak, Dariusz Medical Science Monitor, Vol. 20 https://doi.org/10.12659/msm.890480	journal	January 2014
Treatment of painful bone metastases in prostate and breast cancer patients with the therapeutic radiopharmaceutical rhenium-188-HEDP: Clinical benefit in a real-world study Lange, Rogier; Overbeek, Floor; de Klerk, John Nuklearmedizin, Vol. 55, Issue 05 https://doi.org/10.3413/nukmed-0828-16-05	journal	January 2016

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Selective and efficient removal of perrhenate by an imidazolium based hexapodal receptor in water medium Ghosh, Rajib; Ghosh, Tamal Kanti; Ghosh, Pradyut Dalton Transactions, Vol. 49, Issue 10 https://doi.org/10.1039/d0dt00365d	journal	January 2020
Towards 99mTc- and Re-Based Multifunctional Silica Platforms for Theranostic Applications Wuillemin, Michel A.; Reber, Michael J.; Fox, Thomas MDPI Publishing https://doi.org/10.5167/uzh-180161	text	January 2019
Towards 99mTc- and Re-Based Multifunctional Silica Platforms for Theranostic Applications Wuillemin, Michel A.; Reber, Michael J.; Fox, Thomas Inorganics, Vol. 7, Issue 11 https://doi.org/10.3390/inorganics7110134	journal	November 2019
Towards 99mTc- and Re-based multifunctional silica platforms for theranostic applications Wuillemin, Michel A.; Reber, Michael; Fox, Thomas MDPI https://doi.org/10.21256/zhaw-18730	text	January 2019

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