Abstract
The favorable nuclear properties of actinium-225 ((225)Ac) have led to proposal of this isotope for use in radioimmunotherapy. In an effort to reduce the toxicity of free (225)Ac, a series of ligands were evaluated for stability in vivo. Loss of (225)Ac from acyclic chelating agents resulted in high liver uptake and poor whole body clearance. The macrocyclic ligands c-DOTA, PEPA, and HEHA were evaluated, and (225)Ac-HEHA showed exceptional stability in vivo. (225)Ac chelated with EDTA, DTPA, DOTA, or PEPA permitted substantial accumulation of the radionuclide to the liver, while the (225)Ac-HEHA complex was essentially excreted within minutes of administration. The preparation of the ligands and radiolabeled complexes and the biodistribution results will be discussed.
Publication types
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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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Acetates / chemical synthesis*
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Acetates / chemistry
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Acetates / pharmacokinetics
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Actinium*
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Animals
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Chelating Agents / chemical synthesis*
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Chelating Agents / chemistry
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Drug Stability
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Female
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Ligands
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Mice
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Mice, Inbred BALB C
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Organometallic Compounds / chemical synthesis*
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Organometallic Compounds / chemistry
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Organometallic Compounds / pharmacokinetics
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Radioisotopes*
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Radiopharmaceuticals / chemical synthesis*
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Radiopharmaceuticals / chemistry
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Radiopharmaceuticals / pharmacokinetics
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Tissue Distribution
Substances
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Acetates
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Chelating Agents
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Ligands
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Organometallic Compounds
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Radioisotopes
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Radiopharmaceuticals
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actinium 1,4,7,10,13,16-hexaazacyclohexadecane-N,N',N'',N''',N'''',N'''''-hexaacetic acid
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Actinium