Technetium-99m galactosyl-neoglycoalbumin: Preparation and preclinical studies

D. R. Vera, R. C. Stadalnik, K. A. Krohn

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Abstract

Technetium-99m galactosyl-neoglycoalbumin ([Tc]NGA), a labeled analog ligand to the hepatocyte-specific receptor, hepatic binding protein (HBP), was prepared and tested for labeling yield, stability, biodistribution, toxicity, and dosimetry. The ligand was synthesized by the covalent coupling of a carbohydrate bifunctional reagent, 2-imino-2-ethyloxymethyl-1-thiogalactose, to human serum albumin. Testing in mice and rabbits revealed the product to be nontoxic and apyrogenic. Technetium labeling yields in excess of 95%, by the electrolytic method, did not alter the molecular weight profile of the neoglycoalbumin. The NGA-bound activity remained stable for at least 4 hr. Biodistribution studies in rabbits demonstrated the liver as the single focus of tracer uptake. Dosimetry was based on kinetic studies in 3 baboons. Absorbed doses to liver, small intestine, urinary bladder wall, and uterus were 0.089, 0.28, 0.56, and 0.88 rad/mCi, respectively. Total body, lens of the eye, red marrow, ovaries, and testes were less than 0.06 rad/mCi. High liver specificity imparted by receptor binding combined with high-labeling yield, stability, acceptable dosimetry, and safety provide [Tc]NGA with the attributes required for routine clinical assessment of hepatocyte function.

Original languageEnglish (US)
Pages (from-to)1157-1167
Number of pages11
JournalJournal of Nuclear Medicine
Volume26
Issue number10
StatePublished - Jan 1 1986

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ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging

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