Specific Radiopharmaceuticals Research Articles

The clinical value of quantitative cardiovascular molecular imaging: a step towards precision medicine.

Cardiovascular diseases (CVD) are the leading cause of death worldwide and have an increasing impact on society. Precision medicine, in which optimal care is identified for an individual or a group of individuals rather than for the average population, might provide significant health benefits for this patient group and decrease CVD morbidity and mortality. Molecular imaging provides the opportunity to assess biological processes in individuals in addition to anatomical context provided by other imaging modalities and could prove to be essential in the implementation of precision medicine in CVD. New developments in single-photon emission computed tomography (SPECT) and positron emission tomography (PET) systems, combined with rapid innovations in promising and specific radiopharmaceuticals, provide an impressive improvement of diagnostic accuracy and therapy evaluation. This may result in improved health outcomes in CVD patients, thereby reducing societal impact. Furthermore, recent technical advances have led to new possibilities for accurate image quantification, dynamic imaging, and quantification of radiotracer kinetics. This potentially allows for better evaluation of disease activity over time and treatment response monitoring. However, the clinical implementation of these new methods has been slow. This review describes the recent advances in molecular imaging and the clinical value of quantitative PET and SPECT in various fields in cardiovascular molecular imaging, such as atherosclerosis, myocardial perfusion and ischemia, infiltrative cardiomyopathies, systemic vascular diseases, and infectious cardiovascular diseases. Moreover, the challenges that need to be overcome to achieve clinical translation are addressed, and future directions are provided.

Alpha-induced production and robust radiochemical separation of 43Sc as an emerging radiometal for formulation of PET radiopharmaceuticals

Scandium-43 is an emerging PET radiometal that was produced by α-particle bombardment on natural CaCO3 target via natCa (α,p) 43Sc and natCa (α,n) 43Ti→43Sc reactions using K-130 cyclotron at VECC. A robust radiochemical procedure based on selective precipitation of 43Sc as Sc(OH)3 was developed for separation of the radioisotope from the irradiated target. The overall yield of the separation process was >85% and it was obtained in a form suitable for preparation of target specific radiopharmaceuticals for PET imaging of cancer.

Theranostics of Primary Prostate Cancer: Beyond PSMA and GRP-R.

First, we prospectively performed neurotensin receptor-1 (NTS1) IHC in a series of patients receiving both [68Ga]Ga-PSMA-617 and [68Ga]Ga-RM2 before prostatectomy. In this series, PSMA and GRP-R IHC were also available (n = 16). Next, we aimed at confirming the PSMA/GRP-R/NTS1 expression profile by retrospective autoradiography (n = 46) using a specific radiopharmaceuticals study and also aimed to decipher the expression of less-investigated targets such as NTS2, SST2 and CXCR4. In the IHC study, all samples with negative PSMA staining (two patients with ISUP 2 and one with ISUP 3) were strongly positive for NTS1 staining. No samples were negative for all three stains-for PSMA, GRP-R or NTS1. In the autoradiography study, binding of [111In]In-PSMA-617 was high in all ISUP groups. However, some samples did not bind or bound weakly to [111In]In-PSMA-617 (9%). In these cases, binding of [111n]In-JMV 6659 and [111In]In-JMV 7488 towards NTS1 and NTS2 was high. Targeting PSMA and NTS1/NTS2 could allow for the detection of all intraprostatic lesions.

Clinical Testing of a New Radiopharmaceutical [<sup>99m</sup>Тс]-Al<sub>2</sub>O<sub>3</sub> for the Diagnosis of Sentinel Lymph Nodes

Introduction. In modern oncology, the identification of sentinel lymph nodes (SLN), the first nodes that stand on the way of malignant tumor metastasis, is of increasing interest. Detection of SLN followed by morphological examination allows personalizing the surgical intervention for early breast cancer, melanoma, head and neck tumors, neoplasms of the cervix and endometrium. Currently, there is an active development of specific radiopharmaceuticals for SLN imaging. Within the framework of the grant from the Federal Target Program "Pharma-2020", an original radiopharmaceutical using gamma aluminum oxide – [99mТс]-Al2O3 was developed. Preclinical studies have been demonstrated its effectiveness and safety. Pharmacokinetic studies of [99mTc]-Al2O3 showed that 24 hours after its subcutaneous administration, about 12 % of the administered dose is accumulated in the SLN, which gives possibility for its detection.Aim. To study the possibility of clinical [99mTc]-Al2O3 using for visualization of SLN in breast, larynx and laryngopharyngeal cancer.Materials and methods. The definition of SLN was carried out in 55 patients with breast cancer and 30 patients with malignant tumors of the larynx and laryngopharynx. The study included peritumoral radiopharmaceutical injection, single-photon emission computed tomography with qualitative and quantitative analysis of the images and radioguided surgery detection of lymph nodes with their subsequent morphological examination.Results and discussion. Clinical studies have shown that radionuclide imaging of SLN using [99mTc]-Al2O3 is characterized by high sensitivity in breast cancer, larynx and laryngopharyngeal cancer patients (94.5 and 90 %, respectively), due to the high-intensity accumulation of this radiopharmaceutical in the lymph nodes. The optimal time point for SPECT and radioguided examination is an interval of 18–20 hours after injection of [99mTc]-Al2O3, which allows visualizing the maximum possible number of lymph nodes with the most optimal level of radioactivity for their detection.Conclusion. Application of radionuclide imaging of SLN with the use of [99mTc]-Al2O3 as a radiopharmaceutical is useful in planning surgical treatment of patients with tumors of the breast, larynx and laryngopharynx to determine the extent of surgery.

<sup>18</sup>F-FDG PET/CT in the Diagnosis of Cervical Cancer

Positron emission tomography coupled with computed tomography (PET/CT) has proven to be highly informative in the diagnosis of various malignant tumours. PET/CT examination takes into account biological and morphological data, which allow accurate tumour localisation and full staging of the disease, respectively. Cervical cancer (CC) is one of the most common, high-mortality cancers in women. The effectiveness of CC treatment depends on early diagnosis, which is connected to the assessment of local tumour spread and metastatic lymph node involvement and to the detection of disease recurrence. The aim of the study was to analyse the possibility of using PET/CT with 18 F-FDG for the diagnosis of CC and the evaluation of treatment effectiveness. Additionally, the study aimed to analyse the potential of using other radiopharmaceuticals as biomarkers for the assessment of tumour response. Cervical malignancies are characterised by high glycolytic activity, which explains the superiority of 18 F-FDG PET/CT over other traditional imaging methods in comprehensive diagnosis of patients with CC and, especially, in detecting nodal involvement and distant metastases. Also, 18 F-FDG PET/CT plays an important part in the assessment of treatment effectiveness in CC patients. Further development of 18 F-FDG PET/CT potential in the visualisation of malignant cervical lesions is associated with investigating the possibilities of using other specific radiopharmaceuticals to obtain information about the biological processes that support tumour cell growth: metabolism, proliferative activity, and oxygenation.

Emerging Nuclear Medicine Imaging of Atherosclerotic Plaque Formation.

Atherosclerosis is a chronic widespread cardiovascular disease and a major predisposing factor for cardiovascular events, among which there are myocardial infarction and ischemic stroke. Atherosclerotic plaque formation is a process that involves different mechanisms, of which inflammation is the most common. Plenty of radiopharmaceuticals were developed to elucidate the process of plaque formation at different stages, some of which were highly specific for atherosclerotic plaque. This review summarizes the current nuclear medicine imaging landscape of preclinical and small-scale clinical studies of these specific RPs, which are not as widespread as labeled FDG, sodium fluoride, and choline. These include oxidation-specific epitope imaging, macrophage, and other cell receptors visualization, neoangiogenesis, and macrophage death imaging. It is shown that specific radiopharmaceuticals have strength in pathophysiologically sound imaging of the atherosclerotic plaques at different stages, but this also may induce problems with the signal registration for low-volume plaques in the vascular wall.

The Possibilities of Nuclear Medicine Methods in Inflammation Diagnosis

Modern nuclear medicine is a rapidly developing field that includes various non-invasive molecular imaging techniques with the ability to examine the whole body.Inflammation is a frequent complication in surgical and traumatological practices, which is a complex, local and general pathological process that occurs in the body in response to injury. Having arisen under the influence of a damaging factor, inflammation is characterized by the development of a dynamic complex of changes. However, the search for inflammation foci of inflammation by traditional diagnostic methods in some cases is difficult even with a detailed clinical picture. In this case, nuclear medicine, which is able to visualize pathological processes, including those with a pathological increase in metabolism, may be the best option for finding the affected area.A wide variety of radiopharmaceutical drugs makes it possible to determine the localization of the inflammatory focus in a short time and with high accuracy and makes nuclear imaging methods a priority for the early diagnosis of pathophysiological reactions.This paper presents a review of domestic and foreign literature on the use of specific and nonspecific radiopharmaceuticals in the diagnosis of inflammation. Own cases is also presented.

Modern methods for radionuclide diagnosis of tumors and non-tumor pathologies of the brain

The review analyzes the global experience in the application of nuclear medicine techniques for diagnosis of tumors and non-tumor pathologies of the brain. The main groups of radiopharmaceuticals currently used for imaging of malignant brain tumors and diagnosis of cognitive impairments and neurotransmitter system disturbances by means of single-photon emission computed tomography and positron emission tomography are described.Modern approaches to the application of methods for radionuclide diagnosis in neuro-oncology and neurology are compared, and the main trends in production of new, more specific radiopharmaceuticals for visualizing brain tumors of various degrees of malignancy and diagnosing non-tumor pathologies of the brain are described. The review discusses the advantages and disadvantages of currently used techniques and radiopharmaceuticals for imaging of central nervous system disorders, depending on the clinical situation and specific diagnostic tasks.In addition, the review presents consolidated recommendations of the leading scientific schools in neuro-oncology on the use of nuclear medicine techniques in patients with brain tumors at the stages of treatment and follow-up. The presented article examines the experience of domestic scientific schools in the development of radiopharmaceuticals for neuro-oncology. The features of the development and use of new radiopharmaceuticals in patients with brain tumors and neurodegenerative diseases are highlighted. The review is based on the analysis of literature included in the Scopus, Web of Science, MedLine, The Cochrane Library, EMBASE, Global Health, and RSCI databases.

Oxygen sensing ability of positronium atom for tumor hypoxia imaging

Positronium (Ps), a hydrogen-like atom consisting of a positron and an electron, is efficiently formed in the human body during positron emission tomography (PET) examination, and its decay rate into gamma-ray photons is significantly influenced by the chemical environment, especially the dissolved oxygen concentration (pO2) due to the unpaired electrons. However, the functionality of PET has been underestimated by neglecting the specific information provided by Ps. By comparing the decay rates in O2-, N2-, and air-saturated waters, here we show that Ps probes the absolute value of pO2 with a good linearity and a resolution better than 10 mmHg. This is a sufficient sensitivity for discriminating a hypoxic region in a tumor at approximately 6 mmHg from healthy tissues at approximately 40 mmHg. This method depends only on the fundamental properties of Ps and is independent of specific radiopharmaceuticals. The applications of Ps spin states and reactions will greatly enhance PET functionalities in the next decade.

Positron-emission tomography-guided radiation therapy: Ongoing projects and future hopes

Radiation therapy has undergone significant advances these last decades, particularly thanks to technical improvements, computer science and a better ability to define the target volumes via morphological and functional imaging breakthroughs. Imaging contributes to all three stages of patient care in radiation oncology: before, during and after treatment. Before the treatment, the choice of optimal imaging type and, if necessary, the adequate functional tracer will allow a better definition of the volume target. During radiation therapy, image-guidance aims at locating the tumour target and tailoring the volume target to anatomical and tumoral variations. Imaging systems are now integrated with conventional accelerators, and newer accelerators have techniques allowing tumour tracking during the irradiation. More recently, MRI-guided systems have been developed, and are already active in a few French centres. Finally, after radiotherapy, imaging plays a major role in most patients’ monitoring, and must take into account post-radiation tissue modification specificities. In this review, we will focus on the ongoing projects of nuclear imaging in oncology, and how they can help the radiation oncologist to better treat patients. To this end, a literature review including the terms “Radiotherapy”, “Radiation Oncology” and “PET-CT” was performed in August 2019 on Medline and ClinicalTrials.gov. We chose to review successively these novelties organ-by-organ, focusing on the most promising advances. As a conclusion, the help of modern functional imaging thanks to a better definition and new specific radiopharmaceuticals tracers could allow even more precise treatments and enhanced surveillance. Finally, it could provide determinant information to artificial intelligence algorithms in “-omics” models.

Typical and atypical PET/CT findings in non-cancerous conditions.

Nuclear Medicine multimodality imaging, such as positron emission tomography/computed tomography PET/CT, refers to metabolic tissue characteristics integrated with anatomical details. Fluorine-18-fluorodeoxyglucose (18F-FDG) is the most diffuse radiopharmaceutical and its application is spreading beyond the area of oncology. The causes of high 18F-FDG uptake that were once considered false positives have been identified and the new knowledge about them led to non-cancerous pathologies that can be studied by 18F-FDG PET/CT. This technique, due to the inflammatory cells high avidity of 18F-FDG, can be useful in studying a variety of inflammatory and infectious systemic conditions. Studies performed in patients with fever of unknown origin (FUO) indicate that 18F-FDG PET/CT offer a great advantage of detecting malignancy, inflammation and infection at the same time both in adults and children. Furthermore, the 18F-FDG PET/CT has proved useful in the study of specific organs such as the heart and brain that represent separate topics also for the development of new specific radiopharmaceuticals. In all the non-oncologic conditions 18F-FDG PET/CT imaging may offer an "all-in-one" procedure, thanks also to its panoramic whole-body acquisition, as an alternative to other diagnostic procedures, reducing the number of unnecessary investigations. The 18F-FDG PET/CT finding of the simultaneous presence of radiopharmaceutical uptake for multiple disease interconnect to different medical disciplines. It is important to describe unexpected occasional typical or atypical PET/CT findings to the growth of scientific and medical community; it can be the starting point to the enlargement of PET/CT indications for a better and wider comprehension of the human system. To recognize unexpected occasional findings is very important a well knowledge of many aspects: physiological biodistribution, diagnostic imaging instrumentations and techniques, pathological aspects of the different neoplastic diseases, patient story, such as previous therapy, and its comorbidity. An unexpected occasional finding can lead to suggest further tests or investigations in order to have a wider comprehension of patients' clinical situation and they are easily explainable when we have a physician's approach towards patient.

Radiopharmaceuticals for Breast Cancer and Neuroendocrine Tumors: Two Examples of How Tissue Characterization May Influence the Choice of Therapy.

Molecular medicine has gained clinical relevance for the detection and staging of oncological diseases, to guide therapy decision making and for therapy follow-up due to the availability of new highly sensitive hybrid imaging camera systems and the development of new tailored radiopharmaceuticals that target specific molecules. The knowledge of the expression of different receptors on the primary tumor and on metastases is important for both therapeutic and prognostic purposes and several approaches are available aiming to achieve personalized medicine in different oncological diseases. In this review, we describe the use of specific radiopharmaceuticals to image and predict therapy response in breast cancer and neuroendocrine tumors since they represent a paradigmatic example of the importance of tumoral characterization of hormonal receptors in order to plan a tailored treatment. The most attractive radiopharmaceuticals for breast cancer are 16α-[18F]-fluoro-17β-estradiol for PET assessment of the estrogen expression, radiolabeled monoclonal antibody trastuzumab to image the human epidermal growth factor receptor 2, but also the imaging of androgen receptors with [18F]-fluorodihydrotestosterone.

Huntington's Disease: A Review of the Known PET Imaging Biomarkers and Targeting Radiotracers.

Huntington’s disease (HD) is a fatal neurodegenerative disease caused by a CAG expansion mutation in the huntingtin gene. As a result, intranuclear inclusions of mutant huntingtin protein are formed, which damage striatal medium spiny neurons (MSNs). A review of Positron Emission Tomography (PET) studies relating to HD was performed, including clinical and preclinical data. PET is a powerful tool for visualisation of the HD pathology by non-invasive imaging of specific radiopharmaceuticals, which provide a detailed molecular snapshot of complex mechanistic pathways within the brain. Nowadays, radiochemists are equipped with an impressive arsenal of radioligands to accurately recognise particular receptors of interest. These include key biomarkers of HD: adenosine, cannabinoid, dopaminergic and glutamateric receptors, microglial activation, phosphodiesterase 10 A and synaptic vesicle proteins. This review aims to provide a radiochemical picture of the recent developments in the field of HD PET, with significant attention devoted to radiosynthetic routes towards the tracers relevant to this disease.

Estado actual y perspectivas de la imagen molecular PET en México.

Positron-emission tomography (PET) is a medical diagnostic technique by means of which functional images are obtained by recording the spatio-temporal biodistribution of specific radiopharmaceuticals targeted at specific molecular objectives, which provides biochemical information at the molecular level. Early in the first decade of this 21st century, the Faculty of Medicine of the National Autonomous University of Mexico acquired the technology to implement this diagnostic technique in Mexico, thus becoming a pioneer in PET applications in the country and in Latin America. Almost two decades after its implementation in Mexico, PET has become an essential tool in medical clinics. This article describes the background, current state and perspectives of PET molecular imaging in Mexico, and the impact it has had on the management of patients with oncological, neurological and heart diseases.

11C]PIB PET imaging can detect white and grey matter demyelination in a non-human primate model of progressive multiple sclerosis

BackgroundMultiple sclerosis (MS) is a demyelinating and inflammatory disease of the central nervous system. Its diagnosis is clinical, often confirmed by magnetic resonance imaging. This image modality, however, is not ideal for discrimination of demyelination in grey and white matter regions from inflammatory lesions. Positron Emission Tomography (PET), using specific radiopharmaceuticals, can be a tool to differentiate between these processes. The radiopharmaceutical [11C]PIB is widely used for detection of β-amyloid plaques, but has also been suggested for the analysis of myelin content due to its consistent uptake in white matter. The aim of this study was to evaluate [11C]PIB PET imaging as a tool for detecting demyelinated regions in white and grey matter of non-human primate model of progressive MS. MethodsExperimental autoimmune encephalomyelitis (EAE) was induced in marmosets by injection of recombinant human myelin oligodendrocyte glycoprotein (rhMOG) emulsified in either Incomplete Freund's Adjuvant (IFA) or Complete Freund's Adjuvant (CFA). [11C]PIB PET images were acquired prior to immunization (baseline) and after symptoms were present (end of experiment). Brain tissue was isolated for histochemical analysis. ResultsAll rhMOG/IFA-treated and rhMOG/CFA-treated animals showed clinical signs of EAE. The rhMOG/CFA group presented a significant [11C]PIB uptake reduction only in the left motor cortex (9%, P = 0.011). For the rhMOG/IFA group, significant decrease in [11C]PIB uptake was observed in the whole brain (15%, P = 0.015), in the right hemisphere of body of corpus callosum (34%, P = 0.02), splenium of corpus callosum (38%, P = 0.004), hippocampus (19%, P = 0.036), optic tract (13%, P = 0.025), thalamus (14%, P = 0.041), Globus pallidus (23%, P = 0.017), head of caudate nucleus (25%, P = 0.045), tail of caudate nucleus (29%, P = 0.003), putamen (28%, P = 0.047) and left hemisphere of body of corpus callosum (14%, P = 0.037) and head of caudate nucleus (23%, P = 0.023). [11C]PIB uptake significantly correlated with luxol fast blue histology (myelin marker), both in the rhMOG/IFA (r2= 0.32, P < 0.0001) and the rhMOG/CFA group (r2= 0.46, P < 0.0001). Conclusion[11C]PIB PET imaging is an efficient tool for detecting demyelination in grey and white matter, in a non-human primate model of progressive MS.

Recent developments of prostate-specific membrane antigen (PSMA)-specific radiopharmaceuticals for precise imaging and therapy of prostate cancer: an overview

Despite significant research activities and subsequent progress made in the fight against cancer over the last few decades, prostate cancer remains a major health-related problem and there is no effective option available for the treatment of advanced metastatic prostate cancer as yet. There is a high clinical demand for the development of new and efficacious tumor-targeting agents together with more efficient treatment methods that could improve the prostate patient outcome. Prostate-specific membrane antigen (PSMA) is highly expressed in all types of prostate carcinomas, making PSMA a potential molecular target for detecting localized and metastatic prostate cancer. The development of PSMA-targeting agents, radiolabeled with diagnostic and/or therapeutic radionuclides, holds great clinical potential for a new era of personalized management of metastatic prostate cancer. In the past few years, several PSMA-specific tumor-targeting agents, derived from the “glutamate–urea–lysine” pharmacophore (essential for PSMA receptor recognition), conjugated to different biologically relevant linker groups and radiometal chelating agents or prosthetic groups, have been prepared and evaluated preclinically and/or clinically. Some of these PSMA ligands have gone through a long journey all the way from basic research to human studies, which is a clear example of bench to bed clinical translation. The aim of this review is to provide an overview of some of the recent advances in radiolabeled PSMA-targeting agents, mainly in diagnostic nuclear imaging.

Immuno-Imaging to Predict Treatment Response in Infection, Inflammation and Oncology.

Background: Molecular nuclear medicine plays a pivotal role for diagnosis in a preclinical phase, in genetically susceptible patients, for radio-guided surgery, for disease relapse evaluation, and for therapy decision-making and follow-up. This is possible thanks to the development of new radiopharmaceuticals to target specific biomarkers of infection, inflammation and tumour immunology. Methods: In this review, we describe the use of specific radiopharmaceuticals for infectious and inflammatory diseases with the aim of fast and accurate diagnosis and treatment follow-up. Furthermore, we focus on specific oncological indications with an emphasis on tumour immunology and visualizing the tumour environment. Results: Molecular nuclear medicine imaging techniques get a foothold in the diagnosis of a variety of infectious and inflammatory diseases, such as bacterial and fungal infections, rheumatoid arthritis, and large vessel vasculitis, but also for treatment response in cancer immunotherapy. Conclusion: Several specific radiopharmaceuticals can be used to improve diagnosis and staging, but also for therapy decision-making and follow-up in infectious, inflammatory and oncological diseases where immune cells are involved. The identification of these cell subpopulations by nuclear medicine techniques would provide personalized medicine for these patients, avoiding side effects and improving therapeutic approaches.

Facile radiochemical separation of clinical-grade 90Y from 90Sr by selective precipitation for targeted radionuclide therapy

IntroductionThe widespread clinical utilization of 90Y for preparation of target specific radiopharmaceuticals demands development of a facile, efficient and cost-effective method for radiochemical separation of 90Y from 90Sr via90Sr/90Y generator. In this article, we describe an efficient and facile method for radiochemical separation of 90Y from 90Sr for preparation of radiopharmaceuticals by exploiting the large difference in the solubility product constants (Ksp) of Y(OH)3 and Sr(OH)2. MethodsA two-step radiochemical separation procedure based on selective precipitation of 90Y under alkaline conditions from 90Sr/90Y equilibrium mixture was developed. The 90Y(OH)3 colloid formed at pH ~ 10 was selectively trapped in 0.22 μm sterile filter and was subsequently retrieved by dissolution in HCl solution. Detailed quality control analyses of obtained 90Y were carried out and its utility towards preparation of different radiopharmaceuticals was assessed. ResultsUsing the same feed solution of 90Sr (3.7 GBq), consistent and repeated separation of 90Y could be achieved in different batches with >85% yield and >99.999% radionuclidic purity. Yttrium-90 obtained from this process was found suitable for preparation of therapeutically relevant doses of three different radiopharmaceutical formulations, namely, 90Y-DOTA-TATE, 90Y-PSMA-617 and 90Y-CHX-A″-DTPA-Cetuximab with >95% radiochemical purity. ConclusionsThe promising results obtained in this study would facilitate implementation of the developed technique for obtaining 90Y in adequate quantity and of required purity from a centralized radiopharmacy setup.

Birnessite: A New‐Generation and Cost Effective Ion Exchange Material for Separation of Clinical‐Grade 90Y from 90Sr/90Y Mixture

AbstractThe widespread clinical utilization of 90Y for preparation of target specific radiopharmaceuticals stipulates design of superior advanced materials for facile and cost effective separation of 90Y. We demonstrate for the first time potential of birnessite type phylomanganates for radiochemical separation of clinical grade 90Y from 90Sr/90Y mixture. Sodium birnessite was synthesized by controlled oxidation of MnCl2.4H2O in presence of excess of NaOH and characterized thoroughly for structure, microstructure and purity. Ion exchange experiments in the presence of 90Sr/90Y equilibrium mixture confirmed the exceptionally high selectivity of synthetic sodium birnessite for exchanging Sr2+ ions and the conditions have been optimized to achieve radiochemically pure 90Y (&gt; 80% separation yield) meeting all the pharmaceutical requirements for its clinical use. Radionuclidic purity of 90Y could be achieved to &lt; 1 × 10−4 % of 90Sr which is well below the limit set internationally (2 × 10−3 %). The separated 90Y has been used to prepare 90Y radiolabeled 1,4,7,10‐tetraazacyclododecane‐1,4,7,10‐tetraacetic acid coupled dimeric cyclic RGD peptide derivative [DOTA−E[c(RGDfK)]2] and the biological efficacy of the radiotracer was established in C57/BL6 mice bearing melanoma tumors. The results indicated highly target specific radiotherapy suggesting the potential of sodium birnessite for cost effective radiochemical separation of 90Y.

RADIOPHARMACEUTICALS BASED ON THE GLUCOSE DERIVATIVES FOR TUMOR DIAGNOSIS

The purpose of the study was to review available literature on the efficacy of radiopharmaceuticals based on glucose derivatives labeled with radioactive isotopes for detection of various cancers. Material and methods. A systematic literature review was performed using the Scopus, Web of Science, MedLine, Cochrane Library, EMBASE, and Global Health databases from 2000 to 2016. Out of 900 papers in the field of nuclear medicine, 58 were included into the review. Results. 18F-fluoro-2-deoxy-D-glucose (18F-FDG) has been approved to be a powerful imaging tool for the detection of various cancers as well as for the assessment of tumor extent and therapy response. There is a continuous search for new more specific and effective radiopharmaceuticals for visualization of tumor tissue. Many studies are devoted to the development of radiopharmaceuticals based on technetium-99m labeled glucose derivatives for tumor visualization. Russian researches have made a significant progress in the development of imaging agents for single-photon emission computed tomography. Conclusion. Despite the widespread use of positron emission tomography technologies, which have proved to be effective, the specialists still have a great interest in radiopharmaceuticals based on technetium-99m. The literature review suggests that the emergence of a diagnostic radiopharmaceutical based on technetium-99m labeled glucose derivative will help to improve the availability of nuclear medicine methods and their effectiveness.