The discovery and development of new Tc-based radiopharmaceuticals or labeled drugs in general is based on innovative, pure chemistry and subsequent, application-targeted research. This was the case for all currently clinically applied imaging agents. Most of them were market-introduced some 20 years ago, and the few more recent ones are based on even older chemistry, albeit technetium chemistry has made substantial progress over the last 20 years. This progress though is not mirrored by new molecular imaging agents and is even accompanied by a steady decrease in the number of groups active in pure and applied technetium chemistry, a contrast to the trends in most other fields in which d-elements play a central role. The decrease in research with technetium has been partly counterbalanced by a strong increase of research activities with homologous, cold rhenium compounds for therapy, disclosing in the future eventually a quite unique opportunity for theranostics. This Viewpoint analyzes the pathways that led to radiopharmaceuticals in the past and their underlying fundamental contributions. It attempts to tackle the question of why new chemistry still does not lead to new imaging agents, i.e., the question of whether pure technetium chemistry is still needed at all.
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http://dx.doi.org/10.1021/acs.inorgchem.3c01620 | DOI Listing |
Pharmaceutics
January 2025
Laboratory of Nuclear Medicine (LIM-43), Hospital das Clinicas HCFMUSP, Faculdade de Medicina, Universidade de Sao Paulo, Sao Paulo 05403-911, SP, Brazil.
Background/objectives: Dithiocarbazates (DTCs) and their metal complexes have been studied regarding their property as anticancer activities. In this work, using S-benzyl-5-hydroxy-3-methyl-5-phenyl-4,5-dihydro-1H-pirazol-1-carbodithionate (Hbdtc), we prepared [ReO(bdtc)(Hbdtc)] and [[Tc]TcO(bdtc)(Hbdtc)] complexes for tumor uptake and animal biodistribution studies.
Methods: Re complex was prepared by a reaction of H2bdtc and (NBu)[ReOCl], the final product was characterized by IR, H NMR, CHN, and MS-ESI.
Eur J Med Chem
January 2025
Key Laboratory of Radiopharmaceuticals of Ministry of Education, NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals (National Medical Products Administration), College of Chemistry, Beijing Normal University, Beijing, 100875, China. Electronic address:
Cyclin-dependent kinase 4/6 (CDK4/6) plays a crucial role in cell cycle regulation, is overexpressed in various cancers and is an important target in the development of radiotracers for tumour imaging. Despite the increasing recognition of CDK4/6 inhibitors in cancer therapy, their application is limited by the lack of suitable biomarkers. Herein, we developed a series of technetium-99m-labelled CDK4/6 radiotracers and utilized a linker optimization strategy to reduce their abdominal uptake and enhance their imaging properties.
View Article and Find Full Text PDFAppl Radiat Isot
March 2025
Radiopharmacy Unit, Department of Pharmacy, Groupement Hospitalier Sud - Hospices Civils de Lyon, 165 chemin du Grand Revoyet, 69495, Pierre-Bénite, France; Department of Pharmacy - Groupement Hospitalier Sud - Hospices Civils de Lyon, 165 chemin du Grand Revoyet, 69495, Pierre-Bénite, France.
For hepatobiliary scintigraphy, the radiopharmaceutical drug, ETIFENIN (TECHIDA®), labelled with technetium-99m, is used as a substitute for MEBROFENIN (CHOLEDIAM®). It is generally accepted that radiopharmaceuticals should be checked prior to injection, in particular by determining radiochemical purity, to ensure high-quality images. Radiochromatographic techniques or methods described in the Summary of Product Characteristics (SmPC) and the European Pharmacopeia (Ph.
View Article and Find Full Text PDFJ Environ Manage
February 2025
Savannah River Ecology Laboratory, University of Georgia, Aiken, SC 29802, USA. Electronic address:
The primary approach to assessing monitored natural attenuation (MNA) is currently based on a conceptual model utilizing the total contaminant concentrations, assuming a single aqueous species. However, many contaminants, such as metals and radionuclide - including iodine, can exist in multiple species that behave chemically differently in the environment and can exist simultaneously. For example, radioiodine often occurs concurrently as three major aqueous species: iodide (I), iodate (IO), and organo-I, which undergo distinct attenuation pathways and exhibit markedly different mobility and geochemical behavior.
View Article and Find Full Text PDFMolecules
December 2024
M. V. Lomonosov Institute of Fine Chemical Technology, MIREA-Russian Technological University, 86 Vernadsky Av., 119571 Moscow, Russia.
The use of radiopharmaceuticals for diagnostics in oncology allows for the detection of the disease at an early stage. Among diagnostic radionuclides, Tc is a promising isotope that has been used to create several drugs for clinical use. One of the most effective Tc chelators is 6-hydrazinylnicotinic acid (HYNIC), which, when combined with various vector molecules, can be used for targeted delivery of radionuclides to tumor tissues.
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