Preclinical Evaluation of 68 Ga-DOTA-Minigastrin for the Detection of Cholecystokinin-2/Gastrin Receptor-Positive Tumors | Zendy

Maarten Brom | Zendy; Lieke Joosten | Zendy; Peter Laverman | Zendy; Wim J.G. Oyen | Zendy; Martin Béhé | Zendy; Martin Gotthardt | Zendy; Otto C. Boerman | Zendy

Open Access

Preclinical Evaluation of ⁶⁸ Ga-DOTA-Minigastrin for the Detection of Cholecystokinin-2/Gastrin Receptor-Positive Tumors

Author(s) -

Maarten Brom,

Lieke Joosten,

Peter Laverman,

Wim J.G. Oyen,

Martin Béhé,

Martin Gotthardt,

Otto C. Boerman

Publication year - 2011

Publication title -

molecular imaging

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.815

H-Index - 60

eISSN - 1536-0121

pISSN - 1535-3508

DOI - 10.2310/7290.2010.00032

Subject(s) - biodistribution , dota , gastrin , chemistry , nuclear medicine , cholecystokinin , cholecystokinin b receptor , in vivo , cholecystokinin receptor , receptor , cancer research , medicine , in vitro , chelation , biology , biochemistry , microbiology and biotechnology , organic chemistry , secretion

In comparison to somatostatin receptor scintigraphy, gastrin receptor scintigraphy using 111In-DTPA-minigastrin (MG0) showed added value in diagnosing neuroendocrine tumors. We investigated whether the 68Ga-labeled gastrin analogue DOTA-MG0 is suited for positron emission tomography (PET), which could improve image quality. Targeting of cholecystokinin-2 (CCK2)/gastrin receptor-positive tumor cells with DOTA-MG0 labeled with either 111In or 68Ga 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 68Ga-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 CCK2/gastrin receptor-mediated uptake (p = .0005). The biodistribution of 68Ga-DOTA-MG0 was similar to that of 111In-DOTA-MG0. Subcutaneous and intraperitoneal tumors were clearly visualized by small-animal PET imaging with 5 MBq 68Ga-DOTA-MG0. 111In- and 68Ga-labeled DOTA-MG0 specifically accumulate in CCK2/gastrin receptor-positive AR42J tumors with similar biodistribution apart from the kidneys. AR42J tumors were clearly visualized by microPET. Therefore, 68Ga-DOTA-MG0 is a promising tracer for PET imaging of CCK2/gastrin receptor-positive tumors in humans

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