Products Cited in Publications Worldwide Differences in the Renal Accumulation of Radiogallium-Labeled (Glu) 14 Peptides Containing Different Optical Isomers of Glutamic Acid

Differences in the Renal Accumulation of Radiogallium-Labeled (Glu) 14 Peptides Containing Different Optical Isomers of Glutamic Acid

Ogawa, Kazuma; Nishizawa, Kota; Mishiro, Kenji; Munekane, Masayuki; Fuchigami, Takeshi; Echigo, Hiroaki; Wakabayashi, Hiroshi; Kinuya, Seigo

DOI:

Abstract

Acidic amino acid peptides have a high affinity for bone. Previously, we demonstrated that radiogallium complex-conjugated oligo-acidic amino acids possess promising properties as bone-seeking radiopharmaceuticals. Here, to elucidate the effect of stereoisomers of Glu in Glu-containing peptides [(Glu)14] on their accumulation in the kidney, the biodistributions of [67Ga]Ga-N,N′ -bis-[2-hydroxy- 5-(carboxyethyl)benzyl]ethylenediamine-N,N′ -diacetic acid-conjugated (L-Glu)14 ([67Ga]Ga-HBED-CC- (L-Glu)14), [67Ga]Ga-HBED-CC-(D-Glu)14, [67Ga]Ga-HBED-CC-(DL-Glu)14, and [67Ga]Ga-HBED-CC- (D-Glu-L-Glu)7 were compared. Although the accumulation of these compounds in the bone was comparable, their kidney accumulation and retention were strikingly different, with [67Ga]Ga-HBED-CC- (D-Glu-L-Glu)7 exhibiting the lowest level of kidney accumulation among these compounds. Repeated D- and L-peptides may be a useful method for reducing renal accumulation in some cases.

Keywords

kidney accumulation ; bone imaging ; ; bone metastases ; gallium

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Fmoc-Glu(OtBu)-OH

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