This is an open-label positron emission tomography/computed tomography (PET/CT) study to investigate the diagnostic performance and evaluation efficacy of 68Ga-NOTA-Aca-BBN(7-14) in glioma patients. A single dose of 111-148 Mega-Becquerel (MBq) 68Ga-NOTA-Aca-BBN(7-14) will be injected intravenously. Visual and semiquantitative method will be used to assess the PET/CT images.

Start Date01 Jan 2015

Sponsor / Collaborator

Peking Union Medical College Hospital

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100 Clinical Results associated with Gallium-68-NOTA-Aca-BBN(7-14)

100 Translational Medicine associated with Gallium-68-NOTA-Aca-BBN(7-14)

100 Patents (Medical) associated with Gallium-68-NOTA-Aca-BBN(7-14)

Literatures (Medical) associated with Gallium-68-NOTA-Aca-BBN(7-14)

03 Jan 2020·NanotechnologyQ3 · MATERIALS SCIENCE

Preliminary studies of ⁶⁸Ga-NODA-USPION-BBN as a dual-modality contrast agent for use in positron emission tomography/magnetic resonance imaging

Q3 · MATERIALS SCIENCE

Article

Author: Afsaneh Lahooti ; Sophie Laurent ; Saeed Shanehsazzadeh

The aim of this study was to propose a new dual-modality nanoprobe for positron emission tomography/magnetic resonance imaging (PET/MRI) for the early diagnosis of breast cancer. For synthesis of the nanoprobe, polyethylene glycol-coated ultra-small superparamagnetic iron-oxide nanoparticles (USPION) armed with NODA-GA chelate and grafted with bombesin (BBN) were radiolabeled with ⁶⁸Ga. After characterization, in vitro studies to evaluate the cell binding affinity of the nanoprobe were done by performing Perl's Prussian blue cell staining and MRI imaging. Finally, for in vivo studies, magnetic resonance images were taken in SCID mice bearing breast cancer tumor pre- and post-injection, and a multimodal nanoScan PET/computed tomography was used to perform preclinical imaging of the radiolabeled nanoparticles. Afterwards, a biodistribution study was done on sacrificed mice. The results showed that the highest r₁ and r₂ values were measured for USPIONs at 20 and 60 MHz, respectively. From the in vitro studies, the optical density of the cells after incubation increased with the increase of the iron concentration and the duration of incubation. However, the T₂ values decreased when the iron concentration increased. Furthermore, from in vivo studies, the T₂ and signal intensity decreased during the elapsed time post-injection in the tumor area. In this study, the in vitro studies showed that the affinity of cancer cells to nanoprobe increases meaningfully after conjugation with BBN, and also by increasing the duration of incubation and the iron concentration. Meanwhile, the in vivo results confirmed that the blood clearance of the nanoprobe happened during the first 120 min post-injection of the radiolabeled nanoprobe and also confirmed the targeting ability of that to a gastrin-releasing peptide receptor positive tumor.

21 Feb 2018·Bioconjugate ChemistryQ2 · CHEMISTRY

Positron Emission Tomography Imaging of Prostate Cancer with Ga-68-Labeled Gastrin-Releasing Peptide Receptor Agonist BBN_7–14 and Antagonist RM26

Q2 · CHEMISTRY

Article

Author: Niu, Gang ; Wang, Zhantong ; Chen, Xiaoyuan ; Jacobson, Orit ; Yung, Bryant ; Lang, Lixin ; Zhu, Xiaohua ; Gu, Dongyu ; Cheng, Siyuan ; Ma, Ying ; Zhu, Guizhi

Radiolabeled bombesin (BBN) analogs have long been used for developing gastrin-releasing peptide receptor (GRPR) targeted imaging probes, and tracers with excellent in vivo performance including high tumor uptake, high contrast, and favorable pharmacokinetics are highly desired. In this study, we compared the ⁶⁸Ga-labeled GRPR agonist (Gln-Trp-Ala-Val-Gly-His-Leu-Met-NH₂, BBN_7-14) and antagonist (d-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH₂, RM26) for the positron emission tomography (PET) imaging of prostate cancer. The in vitro stabilities, receptor binding, cell uptake, internalization, and efflux properties of the probes ⁶⁸Ga-1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA)-Aca-BBN_7-14 and ⁶⁸Ga-NOTA-poly(ethylene glycol)₃ (PEG₃)-RM26 were studied in PC-3 cells, and the in vivo GRPR targeting abilities and kinetics were investigated using PC-3 tumor xenografted mice. BBN_7-14, PEG₃-RM26, NOTA-Aca-BBN_7-14, and NOTA-PEG₃-RM26 showed similar binding affinity to GRPR. In PC-3 tumor-bearing mice, the tumor uptake of ⁶⁸Ga-NOTA-PEG₃-RM26 remained at around 3.00 percentage of injected dose per gram of tissue within 1 h after injection, in contrast with ⁶⁸Ga-NOTA-Aca-BBN_7-14, which demonstrated rapid elimination and high background signal. Additionally, the majority of the ⁶⁸Ga-NOTA-PEG₃-RM26 remained intact in mouse serum at 5 min after injection, while almost all of the ⁶⁸Ga-NOTA-Aca-BBN_7-14 was degraded under the same conditions, demonstrating more-favorable in vivo pharmacokinetic properties and metabolic stabilities of the antagonist probe relative to its agonist counterpart. Overall, the antagonistic GRPR targeted probe ⁶⁸Ga-NOTA-PEG₃-RM26 is a more-promising candidate than the agonist ⁶⁸Ga-NOTA-Aca-BBN_7-14 for the PET imaging of prostate cancer patients.

04 Apr 2016·Molecular PharmaceuticsQ2 · MEDICINE

Metabolically Stabilized ⁶⁸Ga-NOTA-Bombesin for PET Imaging of Prostate Cancer and Influence of Protease Inhibitor Phosphoramidon

Q2 · MEDICINE

Article

Author: Krieger, Stephanie ; Rogers, Buck E. ; Wuest, Melinda ; Richter, Susan ; Wuest, Frank ; Bergman, Cody N.

Peptide receptor-based targeted molecular imaging and therapy of cancer is on the current forefront of nuclear medicine preclinical research and clinical practice. The frequent overexpression of gastrin-releasing peptide (GRP) receptors in prostate cancer stimulated the development of radiolabeled bombesin derivatives as high affinity peptide ligands for selective targeting of the GRP receptor. In this study, we have evaluated a novel (68)Ga-labeled bombesin derivative for PET imaging of prostate cancer in vivo. In addition, we were interested in testing the recently proposed "serve-and-protect" strategy to improve metabolic stability of radiolabeled peptides in vivo and to enhance tumor uptake. GRP receptor targeting peptides NOTA-BBN2 and (nat)Ga-NOTA-BBN2 demonstrated a characteristic antagonistic profile and high binding affinity toward the GRP receptor in PC3 cells (IC50 4.6-8.2 nM). Radiolabeled peptide (68)Ga-NOTA-BBN2 was obtained from NOTA-BBN2 in radiochemical yields greater than 62% (decay-corrected). Total synthesis time was 35 min, including purification using solid-phase extraction. (68)Ga-NOTA-BBN2 exhibited favorable resistance against metabolic degradation by peptidases in vivo within the investigated time frame of 60 min. Interestingly, metabolic stability was not further enhanced in the presence of protease inhibitor phosphoramidon. Dynamic PET studies showed high tumor uptake in both PC3- and LNCaP-bearing BALB/c nude mice (SUV5min > 0.6; SUV60min > 0.5). Radiotracer (68)Ga-NOTA-BBN2 represents a novel radiometal-based bombesin derivative suitable for GRP receptor targeting in PC3 and LNCaP mouse xenografts. Further increase of metabolic stability in vivo and enhanced tumor uptake were not observed upon administration of protease inhibitor phosphoramidon. This led to the conclusion that the recently proposed "serve-and-protect" strategy may not be valid for peptides exhibiting favorable intrinsic metabolic stability in vivo.

100 Deals associated with Gallium-68-NOTA-Aca-BBN(7-14)

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Indication	Highest Phase	Country/Location	Organization	Date
Diagnostic agents	Phase 1	-	Beijing Xiehe Bioengineering United Company	-
Glioma	Discovery	CN	Peking Union Medical College Hospital	01 Jan 2015

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