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Review
. 2010 Dec;44(4):233-40.
doi: 10.1007/s13139-010-0056-6. Epub 2010 Oct 12.

(68)Ga-labeled radiopharmaceuticals for positron emission tomography

Dinesh Shetty  1 , Yun-Sang Lee  1 , Jae Min Jeong  1
Affiliations
Review

(68)Ga-labeled radiopharmaceuticals for positron emission tomography

Dinesh Shetty et al. Nucl Med Mol Imaging. 2010 Dec.

Abstract

(68)Ga is a promising emerging radionuclide for positron emission tomography (PET). It is produced using a (68)Ge/(68)Ga-generator, and thus, would enable the cyclotron-independent distribution of PET. However, new (68)Ga-labeled radiopharmaceuticals that can replace (18)F-labeled agents like [(18)F]fluorodeoxyglucose (FDG) are needed. Most of the (68)Ga-labeled derivatives currently used are peptide agents, but the developments of other agents, such as amino acid derivatives, nitroimidazole derivatives, and glycosylated human serum albumin, are being actively pursued in many laboratories. Thus, appearance of new (68)Ga-labeled radiopharmaceuticals with high impact are expected in the near future. Here, we present an overview of (68)Ga-labeled agents in terms of their clinical significances and relevances to the management of certain tumors, and pertinent pre-clinical developments.

Keywords: BAPEN; DOTA; Ga-68; Gallium-68; MSA; NOTA; PET; Peptide.

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Figures

Fig. 1
Fig. 1
Chemical structures of 68Ga-labeled radiopharmaceuticals
Fig. 2
Fig. 2
Some open chain and macrocyclic BCAs used for 68Ga-radiopharmaceutical synthesis
Fig. 3
Fig. 3
Small-animal PET of 68Ga-NOTA-RGD in mice bearing SNU-C4 xenografts at 1 and 2 h after injection without or with cold c(RGDyK) (a and b, respectively). Arrows indicate tumor positions. Reprinted by permission of the Society of Nuclear Medicine from: Jeong JM, et al. (2008) Preparation of a promising angiogenesis PET imaging agent: 68Ga-labeled c(RGDyK)-isothiocyanatobenzyl-1,4,7-triazacyclononane-1,4,7-triacetic acid and feasibility studies in mice. J Nucl Med 49:830–836
Fig. 4
Fig. 4
Micro-PET image of 68Ga-NOTA-aminoalanine in mouse colon cancer (CT-26) showing clear uptake by the cancer lesion located at the right shoulder
Fig. 5
Fig. 5
A micro-PET-CT image of 68Ga-MSA after injection into a mouse footpad. Radioactivity was present at the inguinal lymph node
See this image and copyright information in PMC

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