Evidence map›Paper›PMID 25687450›Full record

ArticleNuclear medicine and biology2015

Stability and in vivo behavior of Rh[16aneS4-diol]211 at complex: a potential precursor for astatine radiopharmaceuticals.

Marek Pruszyński, Monika Łyczko, Aleksander Bilewicz, Michael R Zalutsky

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Nuclear medicine and biology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

7 citing papers in PubMed.

  1. Review
  2. Review
  3. Review
  4. Review
  5. HarnessingJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2022
    Review
  6. Design and Evaluation ofMaterials (Basel, Switzerland) · 2020
    Article
  7. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

4 authors.

Marek PruszyńskiCentre of Radiochemistry and Nuclear Chemistry, Institute of Nuclear Chemistry and Technology, Dorodna 16, 03-195 Warsaw, Poland. Electronic address: m.pruszynski@ichtj.waw.pl.
Monika ŁyczkoCentre of Radiochemistry and Nuclear Chemistry, Institute of Nuclear Chemistry and Technology, Dorodna 16, 03-195 Warsaw, Poland.
Aleksander BilewiczCentre of Radiochemistry and Nuclear Chemistry, Institute of Nuclear Chemistry and Technology, Dorodna 16, 03-195 Warsaw, Poland.
Michael R ZalutskyDepartments of Radiology and Radiation Oncology, Duke University Medical Center, Durham, NC, USA.

Funding

Vaccine Immunotoxin and Radioimmunotherapy of Primary and Metastatic CNS TumorsP01CA154291 · NCI · DUKE UNIVERSITY · PI BIGNER, DARELL D · 2012 to 2016
$14.5M
RADIOTHERAPY USING MONOCLONAL ANTIBODIES AND ASTATINER01CA042324 · NCI · DUKE UNIVERSITY · PI ZALUTSKY, MICHAEL ROD · 1985 to 2020
$4.6M
ASTATINE AND IODINE RADIOLABELED MONOCLONAL ANTIBODIESR37CA042324 · NCI · DUKE UNIVERSITY · PI ZALUTSKY, MICHAEL ROD · 1999 to 2008
$3.8M
NCI NIH HHS CA154291NCI NIH HHS CA42324NCI NIH HHS P01 CA154291NCI NIH HHS R01 CA042324NCI NIH HHS R37 CA042324
6 · The paper itself

Abstract

introductionThe heavy halogen (211)At is of great interest for targeted radiotherapy because it decays by the emission of short-range, high-energy α-particles. However, many astatine compounds that have been synthesized are unstable in vivo, providing motivation for seeking other (211)At labeling strategies. One relatively unexplored approach is to utilize prosthetic groups based on astatinated rhodium (III) complex stabilized with a tetrathioether macrocyclic ligand - Rh[16aneS(4)-diol](211)At. The purpose of the current study was to evaluate the in vitro and in vivo stability of this complex in comparison to its iodine analog - Rh[16aneS(4)-diol](131)I.

methodsRh[16aneS(4)-diol](211)At and Rh[16aneS(4)-diol](131)I complexes were synthesized and purified by HPLC. The stability of both complexes was evaluated in vitro by incubation in phosphate-buffered saline (PBS) and human serum at different temperatures. The in vivo behavior of the two radiohalogenated complexes was assessed by a paired-label biodistribution study in normal Balb/c mice.

resultsBoth complexes were synthesized in high yield and purity. Almost no degradation was observed for Rh[16aneS(4)-diol](131)I in PBS over a 72 h incubation. The astatinated analog exhibited good stability in PBS over 14 h. A slow decline in the percentage of intact complex was observed for both tracers in human serum. In the biodistribution study, retention of (211)At in most tissues was higher than that of (131)I at all time points, especially in spleen and lungs. Renal clearance of Rh[16aneS(4)-diol](211)At and Rh[16aneS(4)-diol](131)I predominated, with 84.1 ± 2.3% and 94.6 ± 0.9% of injected dose excreted via the urine at 4 h.

conclusionsThe Rh[16aneS(4)-diol](211)At complex might be useful for constructing prosthetic groups for the astatination of biomolecules and further studies are planned to evaluate this possibility.

Indexed as

AnimalsAstatineDrug StabilityEthers, CyclicHumansMaleMiceMice, Inbred BALB COrganometallic CompoundsRadiochemistryRadiopharmaceuticalsTissue DistributionAstatineEthers, CyclicOrganometallic CompoundsRadiopharmaceuticalsrhodium tetrathiacyclohexadecanediol dichlorideAstatine-211Macrocyclic thioetherProsthetic groupsRadioiodinationRhodium complexes

Identifiers

PMID25687450
PMCPMC4387111

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.