68Ga-NOTA-BBN-RGD(68Ga-NOTA-BBN-RGD) - 药物靶点：GRPR x αvβ3_专利_临床

概要

基本信息

药物类型

多肽偶联核素、诊断用放射药物

别名-

靶点

GRPR x αvβ3

作用机制

GRPR调节剂(胃泌素释放肽前体受体调节剂)、αvβ3调节剂(整合素α-V/β-3复合体调节剂)、PET imaging(正电子发射断层成像术增强剂)

治疗领域

肿瘤皮肤和肌肉骨骼疾病泌尿生殖系统疾病

在研适应症-

非在研适应症

乳腺癌前列腺癌

原研机构

National Institute For Biomedical Imaging And Bioengineering (Nibib)

在研机构-

非在研机构

National Institute For Biomedical Imaging And Bioengineering (Nibib)

最高研发阶段无进展临床1期

首次获批日期-

最高研发阶段(中国)无进展

特殊审评-

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结构

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关联

2

项与 68Ga-NOTA-BBN-RGD 相关的临床试验

NCT02749019 / Unknown status临床1期IIT

68Ga-NOTA-BBN-RGD PET/CT in Breast Cancer Patients

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

开始日期2015-07-01

申办/合作机构

北京协和医院

[+1]

NCT02747290 / Unknown status早期临床1期IIT

Safety and Diagnostic Performance of 68Gallium-labeled NOTA-BBN-RGD PET/CT in Prostate Cancer Patients

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

开始日期2014-07-01

申办/合作机构

北京协和医院

[+1]

100 项与 68Ga-NOTA-BBN-RGD 相关的临床结果

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100 项与 68Ga-NOTA-BBN-RGD 相关的转化医学

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100 项与 68Ga-NOTA-BBN-RGD 相关的专利（医药）

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5

项与 68Ga-NOTA-BBN-RGD 相关的文献（医药）

2022-07-01·Journal of Medical Physics

Human Dose Assessment of 68Ga-NODAGA-RGD-BBN Heterodimer Peptide based on Animal Data

Article

作者: Alirezapour, Behrouz ; Amraee, Naeimeh ; Hosntalab, Mohammad ; Yousefnia, Hassan

Aims:Calculation of the absorbed dose in human organs is one of the first steps for developing new radiopharmaceuticals. The aim of this study is to estimate the human absorbed dose of a newly developed 68Ga-NODAGA-RGD-BBN radiolabeled compound.Materials and Methods:68Ga-NODAGA-RGD-BBN was prepared by varying different parameters at optimized conditions. The stability of the radiolabeled peptide in phosphate-buffered saline (PBS) and in human serum was evaluated for 120 min. Afterward, the biodistribution of the complex was assessed in normal and tumor-bearing mice, at least for 120 min postinjection. Finally, the human absorbed dose of 68Ga-NODAGA-RGD-BBN was estimated based on mice data using Radiation Dose Assessment Resource and Spark method.Results:68Ga-NODAGA-RGD-BBN was produced with radiochemical purity of more than 98% (high-performance liquid chromatography/ radio thin layer chromatography (RTLC)) with high stability in PBS buffer and in human serum at least for 2 h. The complex demonstrated high uptake in gastrin-releasing peptide receptor-expressing tumors compared to other nontarget organs. Furthermore, the dose assessment for the complex showed that the kidneys receive the highest absorbed dose in comparison with other organs.Conclusion:The result of this study showed that 68Ga-NODAGA-RGD-BBN is an effective and radiolabeled ligand for tumor detection, however more studies are still needed.

2018-06-01·Journal of Nuclear Medicine1区 · 医学

PET Using a GRPR Antagonist ⁶⁸Ga-RM26 in Healthy Volunteers and Prostate Cancer Patients

1区 · 医学

Article

作者: Zhang, Jingjing ; Hou, Guozhu ; Niu, Gang ; Wu, Huanwen ; Chen, Libo ; Zhu, Zhaohui ; Fan, Xinrong ; Chen, Xiaoyuan ; Lang, Lixin ; Li, Fang

This study was designed to analyze the safety, biodistribution, and radiation dosimetry of a gastrin-releasing peptide receptor (GRPR) antagonist PET tracer, ⁶⁸Ga-RM26; to assess its clinical diagnostic value in prostate cancer patients; and to perform a direct comparison between GRPR antagonist ⁶⁸Ga-RM26 and agonist ⁶⁸Ga-BBN. Methods: Five healthy volunteers were enrolled to validate the safety of ⁶⁸Ga-RM26 and calculate dosimetry. A total of 28 patients with prostate cancer (17 newly diagnosed and 11 posttherapy) were recruited and provided written informed consent. All the cancer patients underwent PET/CT at 15-30 min after intravenous injection of 1.85 MBq (0.05 mCi) per kilogram of body weight of ⁶⁸Ga-RM26. Among them, 22 patients (11 newly diagnosed and 11 posttherapy) underwent ⁶⁸Ga-BBN PET/CT for comparison within 1 wk. ^99mTc-MDP (methylene diphosphonate) bone scans were obtained within 2 wk for comparison. GRPR immunohistochemical staining of tumor samples was performed. Results: The administration of ⁶⁸Ga-M26 was well tolerated by all subjects, with no adverse symptoms being noticed or reported during the procedure and at 2-wk follow-up. The total effective dose equivalent and effective dose were 0.0912 ± 0.0140 and 0.0657 ± 0.0124 mSv/MBq, respectively. In the 17 patients with newly diagnosed prostate cancer, ⁶⁸Ga-RM26 PET/CT showed positive prostate-confined findings in 15 tumors with an SUV_max of 6.49 ± 2.37. In the 11 patients who underwent prostatectomy or brachytherapy with or without androgen deprivation therapy, ⁶⁸Ga-RM26 PET/CT detected 8 metastatic lymph nodes in 3 patients with an SUV_max of 4.28 ± 1.25 and 21 bone lesions in 8 patients with an SUV_max of 3.90 ± 3.07. Compared with ⁶⁸Ga-RM26 PET/CT, GRPR agonist ⁶⁸Ga-BBN PET/CT detected fewer primary lesions and lymph node metastases as well as demonstrated lower tracer accumulation. There was a significant positive correlation between SUV derived from ⁶⁸Ga-RM26 PET and the expression level of GRPR (P < 0.001). Conclusion: This study indicates the safety and significant efficiency of GRPR antagonist ⁶⁸Ga-RM26. ⁶⁸Ga-RM26 PET/CT would have remarkable value in detecting both primary prostate cancer and metastasis. ⁶⁸Ga-RM26 is also expected to be better than GRPR agonist as an imaging marker to evaluate GRPR expression in prostate cancer.

2017-02-01·Journal of Nuclear Medicine1区 · 医学

Clinical Translation of a Dual Integrin α_vβ₃– and Gastrin-Releasing Peptide Receptor–Targeting PET Radiotracer, ⁶⁸Ga-BBN-RGD

1区 · 医学

Article

作者: Chen, Xiaoyuan ; Huo, Li ; Li, Zhiyuan ; Yao, Shaobo ; Zhu, Zhaohui ; Chen, Libo ; Zhang, Jingjing ; Lang, Lixin ; Yan, Weigang ; Niu, Gang ; Li, Fang ; Fan, Xinrong ; Yan, Xuefeng

This study aimed to document the first-in-human application of a ⁶⁸Ga-labeled heterodimeric peptide BBN-RGD (bombesin-RGD) that targets both integrin α_vβ₃ and gastrin-releasing peptide receptor (GRPR). We evaluated the safety and assessed the clinical diagnostic value of ⁶⁸Ga-BBN-RGD PET/CT in prostate cancer patients in comparison with ⁶⁸Ga-BBN.METHODSFive healthy volunteers (4 men and 1 woman; age range, 28-53 y) were enrolled to validate the safety of ⁶⁸Ga-BBN-RGD. Dosimetry was calculated using the OLINDA/EXM software. Thirteen patients with prostate cancer (4 newly diagnosed and 9 posttherapy) were enrolled. All the patients underwent PET/CT scans 15-30 min after intravenous injection of 1.85 MBq (0.05 mCi) per kilogram of body weight of ⁶⁸Ga-BBN-RGD and also accepted ⁶⁸Ga-BBN PET/CT within 2 wk for comparison.RESULTSWith a mean injected dose of 107.3 ± 14.8 MBq per patient, no side effect was found during the whole procedure and 2 wk follow-up, demonstrating the safety of ⁶⁸Ga-BBN-RGD. A patient would be exposed to a radiation dose of 2.90 mSv with an injected dose of 129.5 MBq (3.5 mCi), which is much lower than the dose limit set by the Food and Drug Administration. In 13 patients with prostate cancer diagnosed by biopsy, ⁶⁸Ga-BBN-RGD PET/CT detected 3 of 4 primary tumors, 14 metastatic lymph nodes, and 20 bone lesions with an SUV_max of 4.46 ± 0.50, 6.26 ± 2.95, and 4.84 ± 1.57, respectively. Only 2 of 4 primary tumors, 5 lymph nodes, and 12 bone lesions were positive on ⁶⁸Ga-BBN PET/CT, with the SUV_max of 2.98 ± 1.24, 4.17 ± 1.89, and 3.61 ± 1.85, respectively.CONCLUSIONThis study indicates the safety and efficiency of a new type of dual integrin α_vβ₃- and GRPR-targeting PET radiotracer in prostate cancer diagnosis and staging.

100 项与 68Ga-NOTA-BBN-RGD 相关的药物交易

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研发状态

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适应症	最高研发状态	国家/地区	公司	日期
乳腺癌	临床1期	中国	National Institute For Biomedical Imaging And Bioengineering (Nibib)	2015-07-01
前列腺癌	临床1期	中国	National Institute For Biomedical Imaging And Bioengineering (Nibib)	2014-07-01