Chelators and metal complex stability for radiopharmaceutical applications

2019 ◽  
Vol 107 (9-11) ◽  
pp. 1087-1120 ◽  
Author(s):  
Nkemakonam C. Okoye ◽  
Jakob E. Baumeister ◽  
Firouzeh Najafi Khosroshahi ◽  
Heather M. Hennkens ◽  
Silvia S. Jurisson

Abstract Diagnostic and therapeutic nuclear medicine relies heavily on radiometal nuclides. The most widely used and well-known radionuclide is technetium-99m (99mTc), which has dominated diagnostic nuclear medicine since the advent of the 99Mo/99mTc generator in the 1960s. Since that time, many more radiometals have been developed and incorporated into potential radiopharmaceuticals. One critical aspect of radiometal-containing radiopharmaceuticals is their stability under in vivo conditions. The chelator that is coordinated to the radiometal is a key factor in determining radiometal complex stability. The chelators that have shown the most promise and are under investigation in the development of diagnostic and therapeutic radiopharmaceuticals over the last 5 years are discussed in this review.

1982 ◽  
Vol 21 (03) ◽  
pp. 85-91 ◽  
Author(s):  
R. Poppitz

Um die Strahlenexposition und das Strahlenrisiko für die Bevölkerung durch die nuklearmedizinische Diagnostik in Bulgarien zu ermitteln, wurde eine Erhebung für das Jahr 1980 über die Arten und Anzahl der Applikationen von Radiopharmaka, über die verwendeten Aktivitäten und über die Geschlechts- und Altersverteilung der untersuchten Patienten durchgeführt. Die Gesamtzahl diagnostischer in vivo Applikationen betrug 116418 (davon 40,5% bei Männern und 59,5% bei Frauen), d.h. 13,1 Applikationen per 1000 Einwohner. Die applizierte Gesamtaktivität aller 44 verwendeter Radiopharmaka betrug ca. 2,1 TBq (56 Ci). Die Geschlechts- und Altersverteilung der untersuchten Patienten war ähnlich jener in anderen Ländern: nur 17,4% aller Patienten waren im reproduktionsfähigen Alter, 52,7% waren über 45 Jahre alt. Im Vergleich zu anderen entwickelten Ländern war in Bulgarien im Jahr 1980 der Anteil der 131J-Jodid-Untersuchungen verhältnismäßig hoch.


2019 ◽  
Vol 4 (2) ◽  

In nuclear medicine, radiopharmaceuticals are administered to the patient either for the production of diagnostic images or with the intention to treat using the emitted radiation from the radiopharmaceutical. The increased use of PET-imaging causes a need for new planning of radiation protection. In radionuclide therapy, the activities are higher and the radionuclides used are often different from those used in diagnostic nuclear medicine and constitute a greater radiation protection problem. In both diagnostic and therapeutic nuclear medicine, the patient becomes a source of radiation not only for him/herself but also for staff, caregivers and the general public. All categories of staff members involved in nuclear medicine must have good knowledge of radiation protection. This is vital for patient safety as well as for the staff's own security, for caregivers and the general public.


1982 ◽  
Vol 21 (03) ◽  
pp. 92-98 ◽  
Author(s):  
R. Poppitz

Es wird über die somatisch effektiven Äquivalentdosen bei den häufigst verwendeten nuklearmedizinischen diagnostischen Applikationen in Bulgarien 1980 berichtet. Unter Verwendung der ICRP Risikofaktoren für stochastische somatische Wirkungen wurde der Erwartungswert strahleninduzierter maligner Neubildungen mit tödlichem Ausgang in der Zukunft, bedingt durch diese medizinische Bestrahlungsart, berechnet. Dieser Wert (ca. 10 Neubildungen) ist verhältnismäßig klein im Vergleich zu der Gesamtzahl der offiziell registrierten Malignome in Bulgarien. Ein Vergleich der traditionell verwendeten Bevölkerungsdosen (z.B. GSD, LSD) für Bulgarien und für andere Länder wurde ebenfalls durchgeführt. Es wird empfohlen, durch eine verminderte Anwendung von 131J-Jodid in der in vivo Schilddrüsendiagnostik eine Herabsetzung der Strahlenbelastung der Patienten zu erreichen.


2002 ◽  
Vol 2 (4) ◽  
pp. 235-243 ◽  
Author(s):  
Jurij Vucina ◽  
Dragoljub Lukic

The paper deals with production and application of open radioactive sources in modern diagnostic and therapeutic nuclear medicine. In principle, besides adequate physical, chemical and biological properties a reliable route for the routine production of both radionuclide and radiopharmaceutical should be on disposal. The favorite route are radionuclidic generators as they enable simple production of shorter-lived radionuclides at relatively low costs. The main radionuclide in diagnosis is technetium-99m. Its advantages are favorable nuclear properties, availability of large activities of high quality 99mTc at reasonable prices by using (n,f)99Mo/99mTc generators and versatile chemistry. It is used in the investigation of practically all organs and tissues in the human body. Among the betaemitters the radionuclides of rhenium have been recently proposed as suitable candidates for therapeutic applications. The most important is 188Re which is obtained from 188W/188Re generator. Some of the important radiopharmaceuticals labeled with rhenium radionuclides used for certain specific indications are also shown. The activities performed in the Laboratory for Radioisotopes (Vinca Institute of Nuclear Sciences) are also enclosed.


1991 ◽  
Vol 264 (4) ◽  
pp. 213-218 ◽  
Author(s):  
K.T. Kelsey ◽  
K.J. Donohoe ◽  
A. Memisoglu ◽  
B. Baxter ◽  
M. Caggana ◽  
...  

1983 ◽  
Vol 8 (9) ◽  
pp. 434-439 ◽  
Author(s):  
WALTER A. GOETZ ◽  
WILLIAM R. HENDEE ◽  
DAVID L. GILDAY

2001 ◽  
Vol 40 (03) ◽  
pp. 59-70 ◽  
Author(s):  
W. Becker ◽  
J. Meiler

SummaryFever of unknown origin (FUO) in immunocompetent and non neutropenic patients is defined as recurrent fever of 38,3° C or greater, lasting 2-3 weeks or longer, and undiagnosed after 1 week of appropriate evaluation. The underlying diseases of FUO are numerous and infection accounts for only 20-40% of them. The majority of FUO-patients have autoimmunity and collagen vascular disease and neoplasm, which are responsible for about 50-60% of all cases. In this respect FOU in its classical definition is clearly separated from postoperative and neutropenic fever where inflammation and infection are more common. Although methods that use in-vitro or in-vivo labeled white blood cells (WBCs) have a high diagnostic accuracy in the detection and exclusion of granulocytic pathology, they are only of limited value in FUO-patients in establishing the final diagnosis due to the low prevalence of purulent processes in this collective. WBCs are more suited in evaluation of the focus in occult sepsis. Ga-67 citrate is the only commercially available gamma emitter which images acute, chronic, granulomatous and autoimmune inflammation and also various malignant diseases. Therefore Ga-67 citrate is currently considered to be the tracer of choice in the diagnostic work-up of FUO. The number of Ga-67-scans contributing to the final diagnosis was found to be higher outside Germany than it has been reported for labeled WBCs. F-l 8-2’-deoxy-2-fluoro-D-glucose (FDG) has been used extensively for tumor imaging with PET. Inflammatory processes accumulate the tracer by similar mechanisms. First results of FDG imaging demonstrated, that FDG may be superior to other nuclear medicine imaging modalities which may be explained by the preferable tracer kinetics of the small F-l 8-FDG molecule and by a better spatial resolution of coincidence imaging in comparison to a conventional gamma camera.


2008 ◽  
Vol 47 (06) ◽  
pp. 267-274 ◽  
Author(s):  
F. Boldt ◽  
C. Kobe ◽  
W. Eschner ◽  
H. Schicha ◽  
F. Sudbrock

Summary Aim: After application of radiopharmaceuticals the patient becomes a radioactive source which leads to radiation exposure in the proximity. The photon dose rates after administration of different radiopharmaceuticals used in diagnostic nuclear medicine were measured at several distances and different time intervals. These data are of importance for estimating the exposure of technologists and members of the public. Patients, method: In this study dose rates were measured for 67 patients after application of the following radiopharmaceuticals: 99mTc-HDP as well as 99mTcpertechnetate, 18F-fluorodeoxyglucose, 111In-Octreotid and Zevalin® and 123I-mIBG in addition to 123I-NaI. The dose rates were measured immediately following application at six different distances to the patient. After two hours the measurements were repeated and – whenever possible – after 24 hours and seven days. Results: Immediately following application the highest dose rates were below 1 mSv / h: with a maximum at 780 μSv/h for 18F (370 MBq), 250 μSv/h for 99mTc (700 MBq), 150 μSv/h for 111In (185 MBq) and 132 μSv/ h for 123I (370 MBq). At a distance of 0.5 m the values decrease significantly by an order of magnitude. Two hours after application the values are diminished to 1/3 (99mTc, 18F), to nearly ½ (123I) but remain in the same order of magnitude for the longer-lived 111In radiopharmaceuticals. Conclusion: For greater distances the doses remain below the limits outlined in the national legislation.


2020 ◽  
Vol 28 ◽  
Author(s):  
Justyna Hajtuch ◽  
Karolina Niska ◽  
Iwona Inkielewicz-Stepniak

Background: Cancer along with cardiovascular diseases are globally defined as leading causes of death. Importantly, some risk factors are common to these diseases. The process of angiogenesis and platelets aggregation are observed in cancer development and progression. In recent years, studies have been conducted on nanodrugs in these diseases that have provided important information on the biological and physicochemical properties of nanoparticles. Their attractive features are that they are made of biocompatible, well-characterized and easily functionalized materials. Unlike conventional drug delivery, sustained and controlled drug release can be obtained by using nanomaterials. Methods: In this article, we review the latest research to provide comprehensive information on nanoparticle-based drugs for the treatment of cancer, cardiovascular disease associated with abnormal haemostasis, and the inhibition of tumorassociated angiogenesis. Results: The results of the analysis of data based on nanoparticles with drugs confirm their improved pharmaceutical and biological properties, which gives promising antiplatelet, anticoagulant and antiangiogenic effects. Moreover, the review included in vitro, in vivo research and presented nanodrugs with chemotherapeutics approved by Food and Drug Administration. Conclusion: By the optimization of nanoparticles size and surface properties, nanotechnology are able to deliver drugs with enhanced bioavailability in treatment of cardiovascular disease, cancer and inhibition of cancer-related angiogenesis. Thus, nanotechnology can improve the therapeutic efficacy of the drug, but there is a need for a better understanding of the nanodrugs interaction in the human body, because this is a key factor in the success of potential nanotherapeutics.


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