Preclinical Evaluation of Ga-DOTA-Minigastrin for the Detection of Cholecystokinin-2/Gastrin Receptor-Positive Tumors
In comparison to somatostatin receptor scintigraphy, gastrin receptor scintigraphy using 111 In-DTPA-minigastrin (MG0) showed added value in diagnosing neuroendocrine tumors. We investigated whether the 68 Ga-labeled gastrin analogue DOTA-MG0 is suited for positron emission tomography (PET), which c...
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| Format: | Article |
| Language: | English |
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SAGE Publishing
2011-03-01
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| Series: | Molecular Imaging |
| Online Access: | https://doi.org/10.2310/7290.2010.00032 |
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| author | Maarten Brom Lieke Joosten Peter Laverman Wim J.G. Oyen Martin Béhé Martin Gotthardt Otto C. Boerman |
| author_facet | Maarten Brom Lieke Joosten Peter Laverman Wim J.G. Oyen Martin Béhé Martin Gotthardt Otto C. Boerman |
| author_sort | Maarten Brom |
| collection | DOAJ |
| description | In comparison to somatostatin receptor scintigraphy, gastrin receptor scintigraphy using 111 In-DTPA-minigastrin (MG0) showed added value in diagnosing neuroendocrine tumors. We investigated whether the 68 Ga-labeled gastrin analogue DOTA-MG0 is suited for positron emission tomography (PET), which could improve image quality. Targeting of cholecystokinin-2 (CCK 2 )/gastrin receptor-positive tumor cells with DOTA-MG0 labeled with either 111 In or 68 Ga in vitro was investigated using the AR42J rat tumor cell line. Biodistribution was examined in BALB/c nude mice with a subcutaneous AR42J tumor. In vivo PET imaging was performed using a preclinical PET-computed tomographic scanner. DOTA-MG0 showed high receptor affinity in vitro. Biodistribution studies revealed high tumor uptake of 68 Ga-DOTA-MG0: 4.4 ± 1.3 %ID/g at 1 hour postinjection. Coadministration of an excess unlabeled peptide blocked the tumor uptake (0.7 ± 0.1 %ID/g), indicating CCK 2 /gastrin receptor-mediated uptake ( p = .0005). The biodistribution of 68 Ga-DOTA-MG0 was similar to that of 111 In-DOTA-MG0. Subcutaneous and intraperitoneal tumors were clearly visualized by small-animal PET imaging with 5 MBq 68 Ga-DOTA-MG0. 111 In- and 68 Ga-labeled DOTA-MG0 specifically accumulate in CCK 2 /gastrin receptor-positive AR42J tumors with similar biodistribution apart from the kidneys. AR42J tumors were clearly visualized by microPET. Therefore, 68 Ga-DOTA-MG0 is a promising tracer for PET imaging of CCK 2 /gastrin receptor-positive tumors in humans. |
| format | Article |
| id | doaj-art-998480fc328044f9bd4d29da3fd87ffb |
| institution | Kabale University |
| issn | 1536-0121 |
| language | English |
| publishDate | 2011-03-01 |
| publisher | SAGE Publishing |
| record_format | Article |
| series | Molecular Imaging |
| spelling | doaj-art-998480fc328044f9bd4d29da3fd87ffb2025-01-03T01:24:46ZengSAGE PublishingMolecular Imaging1536-01212011-03-011010.2310/7290.2010.0003210.2310_7290.2010.00032Preclinical Evaluation of Ga-DOTA-Minigastrin for the Detection of Cholecystokinin-2/Gastrin Receptor-Positive TumorsMaarten BromLieke JoostenPeter LavermanWim J.G. OyenMartin BéhéMartin GotthardtOtto C. BoermanIn comparison to somatostatin receptor scintigraphy, gastrin receptor scintigraphy using 111 In-DTPA-minigastrin (MG0) showed added value in diagnosing neuroendocrine tumors. We investigated whether the 68 Ga-labeled gastrin analogue DOTA-MG0 is suited for positron emission tomography (PET), which could improve image quality. Targeting of cholecystokinin-2 (CCK 2 )/gastrin receptor-positive tumor cells with DOTA-MG0 labeled with either 111 In or 68 Ga in vitro was investigated using the AR42J rat tumor cell line. Biodistribution was examined in BALB/c nude mice with a subcutaneous AR42J tumor. In vivo PET imaging was performed using a preclinical PET-computed tomographic scanner. DOTA-MG0 showed high receptor affinity in vitro. Biodistribution studies revealed high tumor uptake of 68 Ga-DOTA-MG0: 4.4 ± 1.3 %ID/g at 1 hour postinjection. Coadministration of an excess unlabeled peptide blocked the tumor uptake (0.7 ± 0.1 %ID/g), indicating CCK 2 /gastrin receptor-mediated uptake ( p = .0005). The biodistribution of 68 Ga-DOTA-MG0 was similar to that of 111 In-DOTA-MG0. Subcutaneous and intraperitoneal tumors were clearly visualized by small-animal PET imaging with 5 MBq 68 Ga-DOTA-MG0. 111 In- and 68 Ga-labeled DOTA-MG0 specifically accumulate in CCK 2 /gastrin receptor-positive AR42J tumors with similar biodistribution apart from the kidneys. AR42J tumors were clearly visualized by microPET. Therefore, 68 Ga-DOTA-MG0 is a promising tracer for PET imaging of CCK 2 /gastrin receptor-positive tumors in humans.https://doi.org/10.2310/7290.2010.00032 |
| spellingShingle | Maarten Brom Lieke Joosten Peter Laverman Wim J.G. Oyen Martin Béhé Martin Gotthardt Otto C. Boerman Preclinical Evaluation of Ga-DOTA-Minigastrin for the Detection of Cholecystokinin-2/Gastrin Receptor-Positive Tumors Molecular Imaging |
| title | Preclinical Evaluation of Ga-DOTA-Minigastrin for the Detection of Cholecystokinin-2/Gastrin Receptor-Positive Tumors |
| title_full | Preclinical Evaluation of Ga-DOTA-Minigastrin for the Detection of Cholecystokinin-2/Gastrin Receptor-Positive Tumors |
| title_fullStr | Preclinical Evaluation of Ga-DOTA-Minigastrin for the Detection of Cholecystokinin-2/Gastrin Receptor-Positive Tumors |
| title_full_unstemmed | Preclinical Evaluation of Ga-DOTA-Minigastrin for the Detection of Cholecystokinin-2/Gastrin Receptor-Positive Tumors |
| title_short | Preclinical Evaluation of Ga-DOTA-Minigastrin for the Detection of Cholecystokinin-2/Gastrin Receptor-Positive Tumors |
| title_sort | preclinical evaluation of ga dota minigastrin for the detection of cholecystokinin 2 gastrin receptor positive tumors |
| url | https://doi.org/10.2310/7290.2010.00032 |
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