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Technetium-99m Labeling of Antineoplaston A10 and Its Bioevaluation as a Potential Tumor Imaging Agent


Antineoplastons (ANPs) are compounds that have antitumor activities. ANPA10 was labeled with technetium-99m using stannous chloride as a reducing agent with the labeling yield of approximately 98% at pH 6. The conditions required to optimize the labeling yield were studied in details. The tumor binding specificity of the [99mTc]Tc-ANPA10 radiotracer was evaluated. The uptake of [99mTc]Tc-ANPA10 in ascitic fluid uptake was 10, 16, and 12.8% ID/g at 30, 60, and 120 min post injection. The preclinical biological evaluation of [99mTc]Tc-ANPA10 complex in solid tumor bearing mice showed a high tumor uptake at 1 h post injection (11.2 ± 0.30 % ID/g). The selective uptake of [99mTc]Tc-ANPA10 in solid tumors and rapid clearance from nontarget organs make it promising for solid tumor imaging, but further clinical trials are required.

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Correspondence to I. T. Ibrahim.

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Dawood, M., Alani, B.G., Salim, K.S. et al. Technetium-99m Labeling of Antineoplaston A10 and Its Bioevaluation as a Potential Tumor Imaging Agent. Radiochemistry 64, 219–227 (2022).

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  • antineoplaston
  • technetium-99m
  • selective uptake
  • tumor imaging