Proceedings of the PSK Conference (대한약학회:학술대회논문집)

The Pharmaceutical Society of Korea (대한약학회)
권호 표지

Biodistribition of [$^{125}I$]-labeled biotinylated dendrimer derivatives for antibody pretargeting

  • Kim, Hyung-Sik (College of Pharmacy, Pusan National University) ;
  • Han, Eui-Sik (NIT) ;
  • Wong, Karen J. (Nuclear Medicine Department, Warren G. Magnuson Clinical Center, National Institutes of Health, Bethesda, M) ;
  • Paik, Chang H. (National Institutes of Health, Bethesda, MD)
  • Published : 2003.10.01
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Abstract

It is desirable to improve the tumor targeting and blood clearance pharmacokinetics of radiolabeled monoclonal antibodies. To achieve this goal, several avidin-biotin (Bt) binding systems have been developed to decouple large molecular weight antibodies from small radiolabels, thereby achieving high tumor-to-background radioactivity ratios. We inserted a readily catabolizable linker, triglycine (TG), between 3-［/sup125/I］iodobenzoate and dendrimer (G3). We also neutralized the positive charges of G3 by acylation with tetrafluorophenyl glycolate, thereby blocking proximal tubular reabsorption of G3 mediated by charge attraction. (omitted)

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