Abstract
A robust formulation was developed for [(177)Lu]Lu-AMBA ((177)Lu-DO3A-CH(2)CO-G-[4-aminobenzoyl]-QWAVGHLM-NH(2)), a Bombesin-like agonist with high affinity for Gastrin Releasing Peptide (GRP) receptors. During optimization of labeling, the effect of several radiostabilizers was evaluated; a combination of selenomethionine and ascorbic acid showed superiority over other tested radiostabilizers. The resulting two-vial formulation maintains a radiochemical purity (RCP) of >90% for at least 2 days at room temperature. The method of stabilization should be useful for other methionine-containing peptide radiopharmaceuticals in diagnostic and therapeutic applications.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Drug Stability
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Freezing
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Humans
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Hydrogen-Ion Concentration
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Ligands
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Lutetium / chemistry*
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Lutetium / therapeutic use
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Oligopeptides / chemical synthesis*
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Oligopeptides / therapeutic use
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Radiation-Protective Agents / chemistry
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Radioisotopes / chemistry*
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Radioisotopes / therapeutic use
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Radiopharmaceuticals / chemical synthesis*
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Radiopharmaceuticals / therapeutic use
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Receptors, Bombesin
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Reducing Agents / chemistry
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Selenomethionine / chemistry
Substances
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DO3A-CH2CO-G-4-aminobenzoyl-Q-W-A-V-G-H-L-M-NH2
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Ligands
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Oligopeptides
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Radiation-Protective Agents
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Radioisotopes
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Radiopharmaceuticals
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Receptors, Bombesin
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Reducing Agents
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Lutetium
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Selenomethionine