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

Frontiers in Medicine

article

Nicolas Lepareur¹  Franck Lacœuille³  Christelle Bouvry¹  François Hindré⁴  Emmanuel Garcion⁴  Michel Chérel⁴  Nicolas Noiret⁵  Etienne Garin¹  F. F. Russ Knapp, Jr.⁹ 

[1] Comprehensive Cancer Center Eugène Marquis;Institut NUMECAN (Nutrition;Angers University Hospital;CRCINA (Centre de Recherche en Cancérologie et Immunologie Nantes—Angers)—UMR 1232;ISCR (Institut des Sciences Chimiques de Rennes)—UMR 6226;Univ Angers, PRIMEX (Plateforme de Radiobiologie et d'Imagerie EXperimentale);ICO (Institut de Cancérologie de l'Ouest), Comprehensive Cancer Center René Gauducheau;ENSCR (Ecole Nationale Supérieure de Chimie de Rennes);Medical Radioisotopes Program, ORNL (Oak Ridge National Laboratory), United States

关键词: bone pain palliation;    oncology;    peptides;    radioembolization;    radionuclide therapy;    radiopharmaceuticals;    Rhenium-188;   

DOI  :  10.3389/fmed.2019.00132

学科分类：社会科学、人文和艺术（综合）

来源: Frontiers

【 摘 要 】

Rhenium-188 ( 188 Re) 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 188 Re as an important therapeutic radioisotope for routine clinical use. Moreover, the highly reproducible on-demand availability of 188 Re from the 188 W/ 188 Re generator system is an important feature and permits installation in hospital-based or central radiopharmacies for cost-effective availability of no-carrier-added (NCA) 188 Re. Rhenium-188 and technetium-99 m exhibit similar chemical properties and represent a “theranostic pair.” Thus, preparation and targeting of 188 Re agents for therapy is similar to imaging agents prepared with 99m Tc, the most commonly used diagnostic radionuclide. Over the last three decades, radiopharmaceuticals based on 188 Re-labeled small molecules, including peptides, antibodies, Lipiodol and particulates have been reported. The successful application of these 188 Re-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 188 Re-radiopharmaceuticals which have been investigated in patients for cancer treatment, demonstrating that 188 Re represents a cost effective alternative for routine clinical use in comparison to more expensive and/or less readily available therapeutic radioisotopes.

【 授权许可】

CC BY