ProCA1.GRPR: A New Imaging Agent in Cancer Detection

Pu, Fan; Xue, Shenghui; Yang, Jenny J.

doi:10.2217/bmm-2016-0040

Cited by 4 publications

(2 citation statements)

References 18 publications

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“…The overexpression of GRPR in several cancers makes it an attractive candidate for imaging and targeted therapy [ 4 ]. GRPR remains expressed at high level in lymph-nodes or distant metastases allowing the follow-up of the spread of the disease [ 20 , 30 , 31 ]. Most of GRPR-targeting radioligands developed for the diagnosis and therapy of GRPR-expressing tumors are analogues of amphibian bombesin [ 21 , 23 , 24 ].…”

Section: Discussionmentioning

confidence: 99%

In Vivo Biodistribution and Efficacy Evaluation of NeoB, a Radiotracer Targeted to GRPR, in Mice Bearing Gastrointestinal Stromal Tumor

Montemagno

Raes

Ahmadi

et al. 2021

Cancers

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NeoB is a radiotracer targeting the gastrin-releasing peptide receptor (GRPR), a G-protein–coupled receptor expressed in various cancers. The aim of the present study was to evaluate the biodistribution and efficacy of this new therapeutic agent in Gastrointestinal Stromal Tumors (GIST). Eighty-two SCID mice bearing GIST-882 tumors were employed. [177Lu]Lu-NeoB biodistribution was evaluated up to seven days by organ sampling (200 pmol/0.8 MBq, i.v.). For efficacy evaluation, mice received either saline, 400 pmol or 800 pmol of [177Lu]Lu-NeoB (37MBq, 1/w, 3 w, i.v.). SPECT/CT imaging was performed at 24 h, and tumor volume was determined up to 100 days. Elevated and specific [177Lu]Lu-NeoB uptake was found in the GIST tumor, as demonstrated by in vivo competition (19.1 ± 3.9 %ID/g vs. 0.3 ± 0.1 %ID/g at 4h). [177Lu]Lu-NeoB tumor retention (half-life of 40.2 h) resulted in elevated tumor-to-background ratios. Tumor volumes were significantly reduced in both treated groups (p < 0.01), even leading to complete tumor regression at the 400 pmol dose. [177Lu]Lu-NeoB exhibited excellent pharmacokinetics with elevated and prolonged tumor uptake and low uptake in non-target organs such as pancreas. The potential of this new theragnostic agent in different indications, including GIST, is under evaluation in the FIH [177Lu]Lu-NeoB clinical trial.

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Section: Discussionmentioning

confidence: 99%

In Vivo Biodistribution and Efficacy Evaluation of NeoB, a Radiotracer Targeted to GRPR, in Mice Bearing Gastrointestinal Stromal Tumor

Montemagno

Raes

Ahmadi

et al. 2021

Cancers

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“…[11] The modified native protein approach led not only to stable Gd(III) ion capture with exceptionally high relaxivity in MRI applications, but also to successful preclinical demonstrations of applications. [9,12-15]…”

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confidence: 99%

Insulin Hexamer‐Caged Gadolinium Ion as MRI Contrast‐o‐phore

Taylor

Tran

Liu

et al. 2018

Chemistry A European J

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High-relaxivity protein-complexes of Gd are being pursued as MRI contrast agents in hope that they can be used at much lower doses that would minimize toxic-side effects of Gd release from traditional contrast agents. We construct here a new type of protein-based MRI contrast agent, a proteinaceous cage based on a stable insulin hexamer in which Gd is captured inside a water filled cavity. The macromolecular structure and the large number of "free" Gd coordination sites available for water binding lead to exceptionally high relaxivities per one Gd ion. The Gd slowly diffuses out of this cage, but this diffusion can be prevented by addition of ligands that bind to the hexamer. The ligands that trigger structural changes in the hexamer, SCN , Cl and phenols, modulate relaxivities through an outside-in signaling that is allosterically transduced through the protein cage. Contrast-o-phores based on protein-caged metal ions have potential to become clinical contrast agents with environmentally-sensitive properties.

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Synthesis, preclinical, and initial clinical evaluation of integrin αVβ3 and gastrin-releasing peptide receptor (GRPR) dual-targeting radiotracer [68Ga]Ga-RGD-RM26-03

Wen,

Wang,

et al. 2024

Eur J Nucl Med Mol Imaging

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ProCA1.GRPR: A New Imaging Agent in Cancer Detection

Cited by 4 publications

References 18 publications

In Vivo Biodistribution and Efficacy Evaluation of NeoB, a Radiotracer Targeted to GRPR, in Mice Bearing Gastrointestinal Stromal Tumor

In Vivo Biodistribution and Efficacy Evaluation of NeoB, a Radiotracer Targeted to GRPR, in Mice Bearing Gastrointestinal Stromal Tumor

Insulin Hexamer‐Caged Gadolinium Ion as MRI Contrast‐o‐phore

Synthesis, preclinical, and initial clinical evaluation of integrin αVβ3 and gastrin-releasing peptide receptor (GRPR) dual-targeting radiotracer [68Ga]Ga-RGD-RM26-03

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