Radiometal-Labeled Agents (Non-Technetium) for Diagnostic Imaging

Anderson, Carolyn J.; Welch, Michael J.

doi:10.1021/cr980451q

Cited by 441 publications

(353 citation statements)

References 105 publications

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“…This chelating agent allows the complexation of radiometal and͞or lanthanide agents such as 111 In, which is one of the most common radionuclides used in biodistribution studies of therapeutic molecules (31). The dianhydride form of DTPA readily reacts with CNT 1 (Scheme 1), and the derived DTPA-CNT can be subsequently chelated with 111 In.…”

Section: Resultsmentioning

confidence: 99%

Tissue biodistribution and blood clearance rates of intravenously administered carbon nanotube radiotracers

Singh

Pantarotto

Lacerda

et al. 2006

Proc. Natl. Acad. Sci. U.S.A.

977

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Carbon nanotubes (CNT) are intensively being developed for biomedical applications including drug and gene delivery. Although all possible clinical applications will require compatibility of CNT with the biological milieu, their in vivo capabilities and limitations have not yet been explored. In this work, water-soluble, singlewalled CNT (SWNT) have been functionalized with the chelating molecule diethylentriaminepentaacetic (DTPA) and labeled with indium ( 111 In) for imaging purposes. Intravenous (i.v.) administration of these functionalized SWNT (f-SWNT) followed by radioactivity tracing using gamma scintigraphy indicated that f-SWNT are not retained in any of the reticuloendothelial system organs (liver or spleen) and are rapidly cleared from systemic blood circulation through the renal excretion route. The observed rapid blood clearance and half-life (3 h) of f-SWNT has major implications for all potential clinical uses of CNT. Moreover, urine excretion studies using both f-SWNT and functionalized multiwalled CNT followed by electron microscopy analysis of urine samples revealed that both types of nanotubes were excreted as intact nanotubes. This work describes the pharmacokinetic parameters of i.v. administered functionalized CNT relevant for various therapeutic and diagnostic applications.nanomedicine ͉ blood circulation half-life ͉ drug delivery ͉ pharmacokinetics ͉ nanotoxicology

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Section: Resultsmentioning

confidence: 99%

Tissue biodistribution and blood clearance rates of intravenously administered carbon nanotube radiotracers

Singh

Pantarotto

Lacerda

et al. 2006

Proc. Natl. Acad. Sci. U.S.A.

977

728

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“…Numerous chelators have been reported for complexing copper [5][6][7][8][9][10][11][12][13][14][15][16] and several of these have been functionalized to allow attachment to antibodies [17][18][19][20][21][22][23][24][25][26][27][28][29][30][31][32][33][34] and are now commercially available. The choice of antibody/BFC combination will affect efficacy as an imaging or therapy agent.…”

Section: Introductionmentioning

confidence: 99%

Comparison of ⁶⁴Cu-Complexing Bifunctional Chelators for Radioimmunoconjugation: Labeling Efficiency, Specific Activity, and in Vitro/in Vivo Stability

et al. 2012

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High radiolabeling efficiency, preferably to high specific activity, and good stability of the radioimmunoconjugate are essential features for a successful immunoconjugate for imaging or therapy. In this study, the radiolabeling efficiency, in vitro stability and biodistribution of immunoconjugates with eight different bifunctional chelators labeled with 64 Cu were compared. The anti-CD20 antibody, rituximab, was conjugated to four macrocyclic bifunctional chelators (p-SCN-Bn-DOTA, p- , three DTPA derivatives (p-SCN-Bn-DTPA, p-SCN-CHX-A"-DTPA and ITC-2B3M-DTPA) and a macrobicyclic hexamine ("sarcophagine") chelator (sar-CO 2 H) = (1-NH 2 -8-NHCO(CH 2 ) 3 CO 2 H)sar where sar = sarcophagine = 3, 6,10,13,16,19-hexaazabicyclo[6.6.6]icosane). Radiolabeling efficiency under various conditions, in vitro stability in serum at 37°C and in vivo biodistribution and imaging in normal mice over 48 h were studied. All chelators except sar-CO 2 H were conjugated to rituximab by thiourea bond formation with an average of 4.9 +/− 0.9 chelators per antibody molecule. Sar-CO 2 H was conjugated to rituximab by amide bond formation with 0.5 chelators per antibody molecule. Efficiencies of 64 Cu radiolabeling were dependent on the concentration of immunoconjugate. Notably, the 64 Cu-NOTA-rituximab conjugate demonstrated highest radiochemical yield (95%) under very dilute conditions (31 nM NOTA-rituximab conjugate). Similarly, sar-CO-rituximab, containing 1/10 th the number of chelators per antibody compared to other conjugates retained high labeling efficiency (98 %) at an antibody concentration of 250 nM. In contrast to the radioimmunoconjugates containing DTPA derivatives, which demonstrated poor serum stability, all macrocyclic radioimmunoconjugates were very stable in serum with <6 % dissociation of 64 Cu over 48 h. In vivo biodistribution profiles in normal female Balb/C mice were similar for all the macrocyclic radioimmunoconjugates with most of the activity remaining in the blood pool up to 48 h. Whilst all the macrocyclic bifunctional chelators are suitable for molecular imaging using 64 Cu-labeled antibody conjugates, NOTA and sar-CO 2 H show significant advantages over the others in that they can be radiolabeled rapidly at room temperature, under dilute conditions resulting in high specific activity. Europe PMC Funders Group

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“…Na Tabela III estão resumidas as características físi-cas de radionuclídeos usados em diagnóstico (Saha, 1998;Anderson et al, 1999). Tc.…”

Section: Radiofármacos Para Diagnósticounclassified

“…São vários os fatores que influenciam na interação dos radiofármacos com os receptores (Vallabhajosula, 2001) A Tabela IV apresenta radiofármacos de perfusão usados em diagnóstico e as suas aplicações (Jurisson et al, 1993;Rakias et al, 1996;Dilworth et al, 1998;Saha, 1998;Anderson et al, 1999).…”

Section: Tabela II -Geradores Utilizados Em Medicina Nuclearunclassified

Preparações radiofarmacêuticas e suas aplicações

Oliveira¹,

Santos²,

Ferreira³

et al. 2006

Rev. Bras. Cienc. Farm.

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Radiometal-Labeled Agents (Non-Technetium) for Diagnostic Imaging

Abstract: His current research interests are in the medical application of radionuclides, the development of accelerator targetry, and the development of new radiolabeling techniques.

Cited by 441 publications

References 105 publications

Tissue biodistribution and blood clearance rates of intravenously administered carbon nanotube radiotracers

Tissue biodistribution and blood clearance rates of intravenously administered carbon nanotube radiotracers

Comparison of ⁶⁴Cu-Complexing Bifunctional Chelators for Radioimmunoconjugation: Labeling Efficiency, Specific Activity, and in Vitro/in Vivo Stability

Preparações radiofarmacêuticas e suas aplicações

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Radiometal-Labeled Agents (Non-Technetium) for Diagnostic Imaging

Abstract: His current research interests are in the medical application of radionuclides, the development of accelerator targetry, and the development of new radiolabeling techniques.

Cited by 441 publications

References 105 publications

Tissue biodistribution and blood clearance rates of intravenously administered carbon nanotube radiotracers

Tissue biodistribution and blood clearance rates of intravenously administered carbon nanotube radiotracers

Comparison of 64Cu-Complexing Bifunctional Chelators for Radioimmunoconjugation: Labeling Efficiency, Specific Activity, and in Vitro/in Vivo Stability

Preparações radiofarmacêuticas e suas aplicações

Contact Info

Product

Resources

About

Comparison of ⁶⁴Cu-Complexing Bifunctional Chelators for Radioimmunoconjugation: Labeling Efficiency, Specific Activity, and in Vitro/in Vivo Stability