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European Journal of Nuclear Medicine... Jul 2022Radiopharmaceuticals are essential components of nuclear medicine and serve as one of the cornerstones of molecular imaging and precision medicine. They provide new... (Review)
Review
Radiopharmaceuticals are essential components of nuclear medicine and serve as one of the cornerstones of molecular imaging and precision medicine. They provide new means and approaches for early diagnosis and treatment of diseases. After decades of development and hard efforts, a relatively matured radiopharmaceutical production and management system has been established in China with high-quality facilities. This review provides an overview of the current status of radiopharmaceuticals on production and distribution, clinical application, and regulatory supervision and also describes some important advances in research and development and clinical translation of radiopharmaceuticals in the past 10 years. Moreover, some prospects of research and development of radiopharmaceuticals in the near future are discussed.
Topics: China; Humans; Nuclear Medicine; Precision Medicine; Radiopharmaceuticals
PubMed: 34767047
DOI: 10.1007/s00259-021-05615-6 -
International Journal of Molecular... Apr 2023In medical imaging, techniques such as magnetic resonance imaging, contrast-enhanced computerized tomography, positron emission tomography (PET), and single-photon... (Review)
Review
In medical imaging, techniques such as magnetic resonance imaging, contrast-enhanced computerized tomography, positron emission tomography (PET), and single-photon emission computed tomography (SPECT) are extensively available and routinely used for disease diagnosis. PET probes with peptide-based targeting are typically composed of small peptides especially developed to have high affinity and specificity for a range of cellular and tissue targets. These probes' key benefits include being less expensive than traditional antibody-based PET tracers and having an effective chemical modification process that allows them to be radiolabeled with almost any radionuclide, making them highly appealing for clinical usage. Currently, as with every pharmaceutical design, the use of in silico strategies is steadily growing in this field, even though it is not part of the standard toolkit used during radiopharmaceutical design. This review describes the recent applications of computational design approaches in the design of novel peptide-based radiopharmaceuticals.
Topics: Positron-Emission Tomography; Peptides; Tomography, Emission-Computed, Single-Photon; Radioisotopes; Radiopharmaceuticals; Computer-Aided Design
PubMed: 37047831
DOI: 10.3390/ijms24076856 -
Molecules (Basel, Switzerland) Apr 2023Quantitative nuclear imaging techniques are in high demand for various disease diagnostics and cancer theranostics. The non-invasive imaging modality requires... (Review)
Review
Quantitative nuclear imaging techniques are in high demand for various disease diagnostics and cancer theranostics. The non-invasive imaging modality requires radiotracing through the radioactive decay emission of the radionuclide. Current preclinical and clinical radiotracers, so-called nuclear imaging probes, are radioisotope-labeled small molecules. Liposomal radiotracers have been rapidly developing as novel nuclear imaging probes. The physicochemical properties and structural characteristics of liposomes have been elucidated to address their long circulation and stability as radiopharmaceuticals. Various radiolabeling methods for synthesizing radionuclides onto liposomes and synthesis strategies have been summarized to render them biocompatible and enable specific targeting. Through a variety of radionuclide labeling methods, radiolabeled liposomes for use as nuclear imaging probes can be obtained for in vivo biodistribution and specific targeting studies. The advantages of radiolabeled liposomes including their use as potential clinical nuclear imaging probes have been highlighted. This review is a comprehensive overview of all recently published liposomal SPECT and PET imaging probes.
Topics: Liposomes; Tissue Distribution; Radioisotopes; Tomography, Emission-Computed, Single-Photon; Positron-Emission Tomography; Radiopharmaceuticals
PubMed: 37175207
DOI: 10.3390/molecules28093798 -
Molecules (Basel, Switzerland) Aug 2022Advances in the field of molecular biology have had an impact on biomedical applications, which provide greater hope for both imaging and therapeutics. Work has been... (Review)
Review
Advances in the field of molecular biology have had an impact on biomedical applications, which provide greater hope for both imaging and therapeutics. Work has been intensified on the development of radionuclides and their application in radiopharmaceuticals (RP) which will certainly influence and expand therapeutic approaches in the future treatment of patients. Alpha or beta particles and Auger electrons are used for therapy purposes, and each has advantages and disadvantages. The radionuclides labeled drug delivery system will deliver the particles to the specific targeting cell. Different radioligands can be chosen to uniquely target molecular receptors or intracellular components, making them suitable for personal patient-tailored therapy in modern cancer therapy management. Advances in nanotechnology have enabled nanoparticle drug delivery systems that can allow for specific multivalent attachment of targeted molecules of antibodies, peptides, or ligands to the surface of nanoparticles for therapy and imaging purposes. This review presents fundamental radionuclide properties with particular reference to tumor biology and receptor characteristic of radiopharmaceutical targeted therapy development.
Topics: Beta Particles; Diagnostic Imaging; Humans; Neoplasms; Radioisotopes; Radiopharmaceuticals
PubMed: 36014472
DOI: 10.3390/molecules27165231 -
PET Clinics Oct 2021Novel diagnostic and therapeutic radiopharmaceuticals are increasingly becoming a central part of personalized medicine. Continued innovation in the development of new... (Review)
Review
Novel diagnostic and therapeutic radiopharmaceuticals are increasingly becoming a central part of personalized medicine. Continued innovation in the development of new radiopharmaceuticals is key to sustained growth and advancement of precision medicine. Artificial intelligence has been used in multiple fields of medicine to develop and validate better tools for patient diagnosis and therapy, including in radiopharmaceutical design. In this review, we first discuss common in silico approaches and focus on their usefulness and challenges in radiopharmaceutical development. Next, we discuss the practical applications of in silico modeling in design of radiopharmaceuticals in various diseases.
Topics: Artificial Intelligence; Computer Simulation; Forecasting; Humans; Precision Medicine; Radiopharmaceuticals
PubMed: 34364818
DOI: 10.1016/j.cpet.2021.06.008 -
American Society of Clinical Oncology... May 2018Radiopharmaceutical therapies have provided an attractive therapeutic approach since the introduction of I to treat thyroid cancer. New insights in cancer biology and... (Review)
Review
Radiopharmaceutical therapies have provided an attractive therapeutic approach since the introduction of I to treat thyroid cancer. New insights in cancer biology and radiochemistry have brought radiopharmaceuticals to the leading edge of oncology clinical research. National Cancer Institute (NCI) programs watch for new radiopharmaceutical breakthroughs that should be used to treat patients with unmet therapeutic needs. Such efforts occur through leveraged partnerships between NCI's Cancer Therapy Evaluation Program and its Radiation Research Program. If groundbreaking discoveries are made, NCI pulls together clinician scientists to design novel radiopharmaceutical phase I and II monotherapy or combination trials. The specific infrastructure needs, such as radiopharmaceutical dosimetry and treatment planning, demand new programmatic workflow and regulatory oversight. This article discusses a modern approach to the development of radiopharmaceutical therapies in the era of personalized medicine.
Topics: Clinical Trials as Topic; DNA Damage; Drugs, Investigational; Humans; Intersectoral Collaboration; National Cancer Institute (U.S.); Neoplasms; Radiometry; Radiopharmaceuticals; Treatment Outcome; United States
PubMed: 30231365
DOI: 10.1200/EDBK_200199 -
Theranostics Dec 2013Positron Emission Tomography (PET) experienced accelerated development and has become an established method for medical research and clinical routine diagnostics on... (Review)
Review
Positron Emission Tomography (PET) experienced accelerated development and has become an established method for medical research and clinical routine diagnostics on patient individualized basis. Development and availability of new radiopharmaceuticals specific for particular diseases is one of the driving forces of the expansion of clinical PET. The future development of the ⁶⁸Ga-radiopharmaceuticals must be put in the context of several aspects such as role of PET in nuclear medicine, unmet medical needs, identification of new biomarkers, targets and corresponding ligands, production and availability of ⁶⁸Ga, automation of the radiopharmaceutical production, progress of positron emission tomography technologies and image analysis methodologies for improved quantitation accuracy, PET radiopharmaceutical regulations as well as advances in radiopharmaceutical chemistry. The review presents the prospects of the ⁶⁸Ga-based radiopharmaceutical development on the basis of the current status of these aspects as well as wide range and variety of imaging agents.
Topics: Animals; Drug Discovery; Gallium Radioisotopes; Humans; Positron-Emission Tomography; Radiopharmaceuticals
PubMed: 24396515
DOI: 10.7150/thno.7447 -
Journal of Nuclear Medicine Technology Jun 2020To celebrate the 50th anniversary of the founding of the SNMMI Technologist Section in 1970, the Radiopharmaceutical Sciences Council board of directors is pleased to... (Review)
Review
To celebrate the 50th anniversary of the founding of the SNMMI Technologist Section in 1970, the Radiopharmaceutical Sciences Council board of directors is pleased to contribute to this celebratory supplement of the with a perspective highlighting major developments in the radiopharmaceutical sciences that have occurred in the last 50 years.
Topics: Anniversaries and Special Events; Humans; Nuclear Medicine; Periodicals as Topic; Radiopharmaceuticals; Societies, Medical
PubMed: 32605944
DOI: No ID Found -
Journal of Nanobiotechnology Jul 2021Cerenkov luminescence imaging (CLI) is a novel optical imaging technique that has been applied in clinic using various radionuclides and radiopharmaceuticals. However,...
Cerenkov luminescence imaging (CLI) is a novel optical imaging technique that has been applied in clinic using various radionuclides and radiopharmaceuticals. However, clinical application of CLI has been limited by weak optical signal and restricted tissue penetration depth. Various fluorescent probes have been combined with radiopharmaceuticals for improved imaging performances. However, as most of these probes only interact with Cerenkov luminescence (CL), the low photon fluence of CL greatly restricted it's interaction with fluorescent probes for in vivo imaging. Therefore, it is important to develop probes that can effectively convert energy beyond CL such as β and γ to the low energy optical signals. In this study, a Eu doped gadolinium oxide (GdO:Eu) was synthesized and combined with radiopharmaceuticals to achieve a red-shifted optical spectrum with less tissue scattering and enhanced optical signal intensity in this study. The interaction between GdO:Eu and radiopharmaceutical were investigated using F-fluorodeoxyglucose (F-FDG). The ex vivo optical signal intensity of the mixture of GdO:Eu and F-FDG reached 369 times as high as that of CLI using F-FDG alone. To achieve improved biocompatibility, the GdO:Eu nanoparticles were then modified with polyvinyl alcohol (PVA), and the resulted nanoprobe PVA modified GdO:Eu (GdO:Eu@PVA) was applied in intraoperative tumor imaging. Compared with F-FDG alone, intraoperative administration of GdO:Eu@PVA and F-FDG combination achieved a much higher tumor-to-normal tissue ratio (TNR, 10.24 ± 2.24 vs. 1.87 ± 0.73, P = 0.0030). The use of GdO:Eu@PVA and F-FDG also assisted intraoperative detection of tumors that were omitted by preoperative positron emission tomography (PET) imaging. Further experiment of image-guided surgery demonstrated feasibility of image-guided tumor resection using GdO:Eu@PVA and F-FDG. In summary, GdO:Eu can achieve significantly optimized imaging property when combined with F-FDG in intraoperative tumor imaging and image-guided tumor resection surgery. It is expected that the development of the GdO:Eu nanoparticle will promote investigation and application of novel nanoparticles that can interact with radiopharmaceuticals for improved imaging properties. This work highlighted the impact of the nanoprobe that can be excited by radiopharmaceuticals emitting CL, β, and γ radiation for precisely imaging of tumor and intraoperatively guide tumor resection.
Topics: Animals; Female; Fluorodeoxyglucose F18; Gadolinium; Luminescence; Mice; Mice, Inbred BALB C; Mice, Nude; Molecular Imaging; Nanoparticles; Neoplasms; Optical Imaging; Positron-Emission Tomography; Radiopharmaceuticals; Surgery, Computer-Assisted
PubMed: 34271928
DOI: 10.1186/s12951-021-00920-6 -
Molecules (Basel, Switzerland) Feb 2023The β emitter, rhenium-188 (Re), has long been recognized as an attractive candidate for targeted cancer radionuclide therapy (TRNT). This transition metal shares... (Review)
Review
The β emitter, rhenium-188 (Re), has long been recognized as an attractive candidate for targeted cancer radionuclide therapy (TRNT). This transition metal shares chemical similarities with its congener element technetium, whose nuclear isomer technetium-99m (Tc) is the current workhorse of diagnostic nuclear medicine. The differences between these two elements have a significant impact on the radiolabelling methods and should always receive critical attention. This review aims to highlight what needs to be considered to design a successful radiopharmaceutical incorporating Re. Some of the most effective strategies for preparing therapeutic radiopharmaceuticals with Re are illustrated and rationalized using the concept of the inorganic functional group (core) and a simple ligand field theoretical model combined with a qualitative definition of frontiers orbitals. Of special interest are the Re(V) oxo and Re(V) nitrido functional groups. Suitable ligands for binding to these cores are discussed, successful clinical applications are summarized, and a prediction of viable future applications is presented. Rhenium-188 decays through the emission of a high energy beta particle (2.12 MeV max energy) and a half-life of 16.9 h. An ideal biological target would therefore be a high-capacity target site (transporters, potential gradients, tumour microenvironment) with less emphasis on saturable targets such as overexpressed receptors on smaller metastases.
Topics: Radiopharmaceuticals; Technetium; Radioisotopes; Rhenium
PubMed: 36771153
DOI: 10.3390/molecules28031487