The Radiopharmaceutical Chemistry of the Radioisotopes of Iodine

Vaidyanathan, Ganesan; Zalutsky, Michael R.

doi:10.1007/978-3-319-98947-1_22

Cited by 9 publications

(10 citation statements)

References 89 publications

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“…In this regard, iodine radionuclides offer different isotopes to perform medium-term ( 123 I, t 1/2 = 13.3 h) or long-term imaging studies ( 125 I, t 1/2 = 60.5 d) and even radiotherapy ( 131 I, t 1/2 = 8 d, b À ) with the same molecule. 59 There is an extensive variety of useful SPECT radionuclides; not only for the radiolabelling of small molecules, peptides, proteins or antibodies, but also for the radiolabelling of nanomaterials (Table 2).…”

Section: Radionuclides For Spectmentioning

confidence: 99%

“…the nanomaterial core contains the same element as the radionuclide dopant) which allows imaging of the in vivo fate of some nanomaterials without modifications to the NP structure. For instance, diverse gold NPs have been doped with 195 Au, 198 Au or 199 Au or iron oxide NPs with 59 Fe for similar purposes. [105][106][107][108][109][110][111] For example, Zhao et al doped Au NPs with 199 Au to study the biodistribution in tumour-bearing mice model after conjugation with D-Ala1peptide T-amide (DAPTA) (Fig.…”

Section: Non-chelator Radiolabellingmentioning

confidence: 99%

“…128 In addition to proton activation radiolabelling reactions, neutron activation has been also carried out for the radiolabelling of holmiumbased garnet magnetic NPs (HoIG) via the 165 Ho(n,g) 166 Ho nuclear reaction and more recently, boron nitride nanotubes (BNNTs) with 153 Sm and 159 Gd through 152 Sm(n,g) 153 Sm and 158 Gd(n,g) 159 Gd nuclear reactions respectively. 129,130 A high control over the radiolabelling location represents the main advantage of this method, as only specific atoms can Ac, 64 Cu, 59 Fe, 68 Ga, 111 In 109-111 and 115-119 Gold NPs 195 Au, 198 Au, 199 Au 105-108 Up-converting NPs 153 Sm, 90 undergo the nuclear reaction, with a consequently high RCS. However, this method has a key drawback in the requirement of a proton/neutron beam source, which involves the use of complex instruments that are not widely available.…”

Section: Non-chelator Radiolabellingmentioning

confidence: 99%

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Radiolabelling of nanomaterials for medical imaging and therapy

2021

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Section: Radionuclides For Spectmentioning

confidence: 99%

Section: Non-chelator Radiolabellingmentioning

confidence: 99%

Section: Non-chelator Radiolabellingmentioning

confidence: 99%

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Radiolabelling of nanomaterials for medical imaging and therapy

2021

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“…52 Among the functionalized aromatic compounds, the most common strategy so far has been aryl-tin agents in which the 211 At is introduced as an astatine-carbon bond in the aryl ring through an electrophilic destannylation reaction. 51,53,54 It should be noted that the bond strength of the astatinecarbon bond has been calculated to be weaker than the corresponding iodine-carbon bond. 55 The stability of the 211 At-aryl carbon bond was recently evaluated by Teze et al and the results showed that the apparent instability can be attributed to oxidative decomposition, which in vivo particularly occurs in lysosomes after cell internalization.…”

Section: At Radiopharmaceutical Synthesismentioning

confidence: 99%

Realizing Clinical Trials with Astatine-211: The Chemistry Infrastructure

Lindegren

Albertsson

Bäck

et al. 2020

Cancer Biotherapy and Radiopharmaceuticals

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Despite the consensus around the clinical potential of the a-emitting radionuclide astatine-211 (211 At), there are only a limited number of research facilities that work with this nuclide. There are three main reasons for this: (1) Scarce availability of the nuclide. Despite a relatively large number of globally existing cyclotrons capable of producing 211 At, few cyclotron facilities produce the nuclide on a regular basis. (2) Lack of a chemical infrastructure, that is, isolation of 211 At from irradiated targets and the subsequent synthesis of an astatinated product. At present, the research groups that work with 211 At depend on custom systems for recovering 211 At from the irradiated targets. Setting up and implementing such custom units require long lead times to provide a proper working system. (3) The chemistry of 211 At. Compared with radiometals there are no well-established and generally accepted synthesis methods for forming sufficiently stable bonds between 211 At and the tumor-specific vector to allow for systemic applications. Herein we present an overview of the infrastructure of producing 211 At radiopharmaceuticals, from target to radiolabeled product including chemical strategies to overcome hurdles for advancement into clinical trials with 211 At.

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“…In the case of carbon-11, which is typically added as the electrophilic [ 11 C]methyl iodide, the precursor must be sufficiently nucleophilic [24]; whereas, in the case of [ 18 F], the precursor is usually an electrophile to allow for the addition of the nucleophilic [ 18 F]fluoride anions [25]. In the case of the other halogens, Br or I, this typically proceeds via nucleophilic aromatic substitution of tributyltin (SnBu 3 ) derivative [21,26].…”

Section: Radionuclide Choice: Chelation Vs Covalent Attachmentmentioning

confidence: 99%

Radiochemical Approaches to Imaging Bacterial Infections: Intracellular versus Extracellular Targets

Northrup

Mach

Sellmyer

2019

IJMS

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The discovery of penicillin began the age of antibiotics, which was a turning point in human healthcare. However, to this day, microbial infections are still a concern throughout the world, and the rise of multidrug-resistant organisms is an increasing challenge. To combat this threat, diagnostic imaging tools could be used to verify the causative organism and curb inappropriate use of antimicrobial drugs. Nuclear imaging offers the sensitivity needed to detect small numbers of bacteria in situ. Among nuclear imaging tools, radiolabeled antibiotics traditionally have lacked the sensitivity or specificity necessary to diagnose bacterial infections accurately. One reason for the lack of success is that the antibiotics were often chelated to a radiometal. This was done without addressing the ramifications of how the radiolabeling would impact probe entry to the bacterial cell, or the mechanism of binding to an intracellular target. In this review, we approach bacterial infection imaging through the lens of bacterial specific molecular targets, their intracellular or extracellular location, and discuss radiochemistry strategies to guide future probe development.

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The Radiopharmaceutical Chemistry of the Radioisotopes of Iodine

Cited by 9 publications

References 89 publications

Radiolabelling of nanomaterials for medical imaging and therapy

Radiolabelling of nanomaterials for medical imaging and therapy

Realizing Clinical Trials with Astatine-211: The Chemistry Infrastructure

Radiochemical Approaches to Imaging Bacterial Infections: Intracellular versus Extracellular Targets

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