Effect of Chelators on the Pharmacokinetics of Tc-99m-Labeled Imaging Agents for the Prostate-Specific Membrane Antigen (PSMA)
- Authors
- Banerjee, Sangeeta Ray; Pullambhatla, Mrudula; Foss, Catherine A.; Falk, Alexander; Byun, Youngjoo; Nimmagadda, Sridhar; Mease, Ronnie C.; Pomper, Martin G.
- Issue Date
- 8-8월-2013
- Publisher
- AMER CHEMICAL SOC
- Citation
- JOURNAL OF MEDICINAL CHEMISTRY, v.56, no.15, pp.6108 - 6121
- Indexed
- SCIE
SCOPUS
- Journal Title
- JOURNAL OF MEDICINAL CHEMISTRY
- Volume
- 56
- Number
- 15
- Start Page
- 6108
- End Page
- 6121
- URI
- https://scholar.korea.ac.kr/handle/2021.sw.korea/102469
- DOI
- 10.1021/jm400823w
- ISSN
- 0022-2623
- Abstract
- Technetium-99m, the most commonly used radionuclide in nuclear medicine, can be attached to biologically important molecules through a variety of chelating agents, the choice of which depends upon the imaging application. The prostate-specific membrane antigen (PSMA) is increasingly recognized as an important target for imaging and therapy of prostate cancer (PCa). Three different Tc-99m-labeling methods were employed to investigate the effect of the chelator on the biodistribution and PCa tumor uptake profiles of 12 new urea-based PSMA-targeted radiotracers. This series includes hydrophilic ligands for radiolabeling with the [Tc-99m(CO)(3)](+) core (L8-L10), traditional NxSy-based chelating agents with varying charge and polarity for the Tc-99m-oxo core (L11-L18), and a Tc-99m-organohydrazine-labeled radioligand (L19). Tc-99m(I)-Tricarbonyl-labeled [Tc-99m]L8 produced the highest PSMA+ PC3 PIP to PSMA- PC3 flu tumor ratios and demonstrated the lowest retention in normal tissues including kidney after 2 h. These results suggest that choice of chelator is an important pharmacokinetic consideration in the development of Tc-99m-labeled radiopharmaceuticals targeting PSMA.
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Collections - College of Pharmacy > Department of Pharmaceutical Science > 1. Journal Articles
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