Abstract
The radiolanthanides (149)Pm, (166)Ho, and (177)Lu possess a range of half-lives and alpha(-) beta(-) energies for targeted radiotherapy of cancer. (149)Pm-, (166)Ho-, and (177)Lu-DOTA-biotin were pretargeted to LS174T colorectal tumors in nude mice with CC49 scFvSA antibody-streptavidin fusion protein. Tumor uptakes of (149)Pm (22.9% ID/g), (166)Ho (30.2% ID/g), and (177)Lu (35.4% ID/g) peaked at 1-4 h. Rapid blood disappearance was accompanied by urinary excretion of 59-66% ID within 1 h. Biodistributions of these agents show promise for pretargeted radioimmunotherapy of cancer.
Publication types
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Comparative Study
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Evaluation Study
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Animals
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Antibodies, Neoplasm / administration & dosage
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Antibodies, Neoplasm / metabolism*
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Biotin / administration & dosage
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Biotin / analogs & derivatives*
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Biotin / pharmacokinetics*
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Cell Line, Tumor
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Colonic Neoplasms / metabolism*
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Colonic Neoplasms / radiotherapy
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Drug Delivery Systems / methods*
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Holmium / administration & dosage
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Holmium / pharmacokinetics
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Humans
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Immunoglobulin Fragments / administration & dosage
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Immunoglobulin Fragments / metabolism
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Injections, Intravenous
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Lutetium / administration & dosage
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Lutetium / pharmacokinetics
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Metabolic Clearance Rate
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Mice
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Mice, Nude
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Organ Specificity
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Organometallic Compounds / administration & dosage
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Organometallic Compounds / pharmacokinetics*
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Promethium / administration & dosage
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Promethium / pharmacokinetics
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Radioimmunotherapy / methods*
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Radioisotopes / administration & dosage
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Radioisotopes / pharmacokinetics*
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Radiopharmaceuticals / administration & dosage
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Radiopharmaceuticals / pharmacokinetics
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Recombinant Fusion Proteins / administration & dosage
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Recombinant Fusion Proteins / pharmacokinetics
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Streptavidin / administration & dosage
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Streptavidin / pharmacokinetics*
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Tissue Distribution
Substances
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Antibodies, Neoplasm
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B72.3 antibody
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DOTA-biotin
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Immunoglobulin Fragments
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Organometallic Compounds
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Radioisotopes
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Radiopharmaceuticals
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Recombinant Fusion Proteins
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Lutetium
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Biotin
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Streptavidin
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Holmium
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Promethium