The aim is to examine the expression of αvβ3 integrin using a novel selective radiotracer in patients with chronich ischemic heart disease and investigate if it is a suitable tool for predicting myocardial recovery and thus prognosis after intervention.

Start Date01 Jan 2024

Sponsor / Collaborator

Rigshospitalet

NCT03655977

/ Unknown statusNot ApplicableIIT

Radiation Therapy Planning by Multi-parametric PET/MRI Imaging in Patients With Cervical Cancer

The main goal of this project is to evaluate the potential and feasibility of hybrid PET/MRI functional imaging to non-invasively measure tumor characteristics for radiation therapy planning (RT) for cervical cancer. It will be assessed how the complementary information of tumor characteristics can contributed to better understanding of tumor delineation. Another endpoint of this study is to evaluate a new PET-tracer (68Ga-NODAGA- E[c(RGDyK)]2) enabling imaging of tumor-angiogenesis.

Start Date01 Sep 2018

Sponsor / Collaborator

Rigshospitalet

NCT03445884

/ CompletedPhase 2IIT

68Ga-NODAGA-E[c(RGDγK)]2: a Novel Positron Emission Tomography (PET) Tracer for in Vivo Molecular Imaging of Myocardial Angiogenesis Following Myocardial Infarction

The aim is to examine the expression of αvβ3 integrin using a novel selective radiotracer in patients with myocardial infarction and investigate if it is a suitable tool for predicting myocardial recovery and thus prognosis.

Start Date20 Feb 2018

Sponsor / Collaborator

Rigshospitalet

100 Clinical Results associated with 68Ga-NODAGA-E[c(RGDyK)]2

100 Translational Medicine associated with 68Ga-NODAGA-E[c(RGDyK)]2

100 Patents (Medical) associated with 68Ga-NODAGA-E[c(RGDyK)]2

Literatures (Medical) associated with 68Ga-NODAGA-E[c(RGDyK)]2

15 Feb 2019·Zhongguo xiu fu chong jian wai ke za zhi = Zhongguo xiufu chongjian waike zazhi = Chinese journal of reparative and reconstructive surgery

[Theranostics of osteosarcoma and lung metastasis with new integrin α _vβ ₃ receptor targeted radiotracers].

Article

Author: Zhang, Lulu ; Wang, Liming ; Shao, Guoqiang ; Yao, Qingqiang ; Zhang, Pengjun ; Bu, Ting ; Sui, Jisheng

ObjectiveTo investigate the value of integrin α _vβ ₃ targeted microPET/CT imaging with ⁶⁸Ga-NODAGA-RGD ₂ as radiotracer for the detection of osteosarcoma and theranostics of osteosarcoma lung metastasis.MethodsThe ⁶⁸Ga-NODAGA-RGD ₂ and ¹⁷⁷Lu-NODAGA-RGD ₂ were prepared via one-step method and their stability and integrin α _vβ ₃ binding specificity were investigated in vitro. Forty-one nude mice were injected with human MG63 osteosarcoma to established the animal model bearing subcutaneous osteosarcoma ( n=21), osteosarcoma in tibia ( n=5), and osteosarcoma pulmonary metastatic ( n=15). The microPET-CT imaging was carried out in 3 animal models at 1 hour after tail vein injection of ⁶⁸Ga-NODAGA-RGD ₂. Biodistribution study of ⁶⁸Ga-NODAGA-RGD ₂ was performed in animal model bearing subcutaneous osteosarcoma at 10, 60, and 120 minutes. The animal model bearing pulmonary metastatic osteosarcoma was injected with ¹⁷⁷Lu-NODAGA-RGD ₂ at 7 weeks after model establishment to observe the therapeutic effect of pulmonary metastatic osteosarcoma. Histological and immunohistochemistry examinations were also done to confirm the establishment of animal model and integrin β ₃ expression in animal models bearing subcutaneous osteosarcoma and bearing pulmonary metastatic osteosarcoma.Results⁶⁸Ga-NODAGA-RGD ₂ and ¹⁷⁷Lu-NODAGA-RGD ₂ had good stability in vitro with the 50% inhibitory concentration value of (5.0±1.1) and (6.5±0.8) nmol/L, respectively. The radiochemical purity of ⁶⁸Ga-NODAGA-RGD ₂ at 1, 4, and 8 hours was 98.5%±0.3%, 98.3%±0.5%, and 97.9%±0.4%; while the radiochemical purity of ¹⁷⁷Lu-NODAGA-RGD ₂ at 1, 7, and 14 days was 99.3%±0.7%, 98.7%±1.2%, and 96.0%±2.8%. ⁶⁸Ga-NODAGA-RGD ₂ microPET-CT showed that the accumulation of ⁶⁸Ga-NODAGA-RGD ₂ in animal models bearing subcutaneous osteosarcoma and osteosarcoma in tibia and in lung metastasis as small as 1-2 mm in diameter of animal model bearing pulmonary metastatic osteosarcoma. Biodistribution study of ⁶⁸Ga-NODAGA-RGD ₂ in animal model bearing subcutaneous osteosarcoma revealed rapid clearance from blood with tumor peak uptake of (3.85±0.84) %ID/g at 120 minutes. The distribution of ¹⁷⁷Lu-NODAGA-RGD ₂ in lung metastasis was similar with ⁶⁸Ga-NODAGA-RGD ₂. The number and size of osteosarcoma metastasis decreased at 2 weeks after ¹⁷⁷Lu-NODAGA-RGD ₂ administration and integrin targeting specificity was confirmed by pathology examination.Conclusion⁶⁸Ga-NODAGA-RGD ₂ was potential for positive imaging and early detection of osteosarcoma and metastasis. Targeted radiotherapy with ¹⁷⁷Lu-NODAGA-RGD ₂ was one potential alternative for osteosarcoma lung metastasis.

01 Mar 2014·Nuclear Medicine and BiologyQ4 · MEDICINE

Comparison of two new angiogenesis PET tracers 68Ga-NODAGA-E[c(RGDyK)]2 and 64Cu-NODAGA-E[c(RGDyK)]2; in vivo imaging studies in human xenograft tumors

Q4 · MEDICINE

Article

Author: Myschetzky, Rebecca ; Brandt-Larsen, Malene ; Oxboel, Jytte ; Schjoeth-Eskesen, Christina ; El-Ali, Henrik H ; Kjaer, Andreas ; Madsen, Jacob

INTRODUCTIONThe aim of this study was to synthesize and perform a side-by-side comparison of two new tumor-angiogenesis PET tracers (68)Ga-NODAGA-E[c(RGDyK)](2) and (64)Cu-NODAGA-E[c(RGDyK)](2) in vivo using human xenograft tumors in mice. Human radiation burden was estimated to evaluate potential for future use as clinical PET tracers for imaging of neo-angiogenesis.METHODSA (68)Ge/(68)Ga generator was used for the synthesis of (68)Ga-NODAGA-E[c(RGDyK)](2). (68)Ga and (64)Cu labeled NODAGA-E[c(RGDyK)](2) tracers were administrated in nude mice bearing either human glioblastoma (U87MG) or human neuroendocrine (H727) xenograft tumors. PET/CT scans at 3 time points were used for calculating the tracer uptake in tumors (%ID/g), integrin αVβ3 target specificity was shown by blocking with cold NODAGA-E[c(RGDyK)](2), and biodistribution in normal organs were also examined. From biodistribution data in mice human radiation-absorbed doses were estimated using OLINDA/EXM software.RESULTS(68)Ga-NODAGA-E[c(RGDyK)](2) was synthesized with a radiochemical purity of 89%-99% and a specific activity (SA) of 16-153 MBq/nmol. (64)Cu-NODAGA-E[c(RGDyK)](2) had a purity of 92%-99% and an SA of 64-78 MBq/nmol. Both tracers showed similar uptake in xenograft tumors 1h after injection (U87MG: 2.23 vs. 2.31%ID/g; H727: 1.53 vs. 1.48%ID/g). Both RGD dimers showed similar tracer uptake in non-tumoral tissues and a human radiation burden of less than 10 mSv with an administered dose of 200 MBq was estimated.CONCLUSION(68)Ga-NODAGA-E[c(RGDyK)](2) and (64)Cu-NODAGA-E[c(RGDyK)](2) can be easily synthesized and are both promising candidates for PET imaging of integrin αVβ3 positive tumor cells. (68)Ga-NODAGA-E[c(RGDyK)](2) showed slightly more stable tumor retention. With the advantage of in-house commercially (68)Ge/(68)Ga generators, (68)Ga-NODAGA-E[c(RGDyK)](2) may be the best choice for future clinical PET imaging in humans.

DiagnosticsQ4 · MEDICINE

Angiogenesis PET Tracer Uptake (68Ga-NODAGA-E[(cRGDyK)]2) in Induced Myocardial Infarction in Minipigs

Q4 · MEDICINE

ArticleOA

Author: Emil Christensen, Thomas ; Kjær, Andreas ; Madsen, Jacob ; Rasmussen, Thomas ; Hasbak, Philip ; Kastrup, Jens ; Brandt-Larsen, Malene ; Follin, Bjarke ; Pharao Hammelev, Karsten

Angiogenesis is part of the healing process following an ischemic injury and is vital for the post-ischemic repair of the myocardium. Therefore, it is of particular interest to be able to noninvasively monitor angiogenesis. This might, not only permit risk stratification of patients following myocardial infarction, but could also facilitate development and improvement of new therapies directed towards stimulation of the angiogenic response. During angiogenesis endothelial cells must adhere to one another to form new microvessels. αvβ3 integrin has been found to be highly expressed in activated endothelial cells and has been identified as a critical modulator of angiogenesis. 68Ga-NODAGA-E[c(RGDyK)]2 (RGD) has recently been developed by us as an angiogenesis positron-emission-tomography (PET) ligand targeted towards αvβ3 integrin. In the present study, we induced myocardial infarction in Göttingen minipigs. Successful infarction was documented by 82Rubidium-dipyridamole stress PET and computed tomography. RGD uptake was demonstrated in the infarcted myocardium one week and one month after induction of infarction by RGD-PET. In conclusion, we demonstrated angiogenesis by noninvasive imaging using RGD-PET in minipigs hearts, which resemble human hearts. The perspectives are very intriguing and might permit the evaluation of new treatment strategies targeted towards increasing the angiogenetic response, e.g., stem-cell treatment.

100 Deals associated with 68Ga-NODAGA-E[c(RGDyK)]2

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Myocardial Ischemia	Phase 2	Denmark	Rigshospitalet	01 Jan 2024
Acute myocardial infarction	Discovery	Denmark	Rigshospitalet	20 Feb 2018
Neurofibromatosis 2	Discovery	Denmark	Rigshospitalet	02 Jan 2018
Breast Cancer	Discovery	Denmark	Rigshospitalet	01 Nov 2016
Neoplasm Metastasis	Discovery	Denmark	Rigshospitalet	01 Nov 2016
Neuroendocrine Carcinoma	Discovery	Denmark	Rigshospitalet	01 Nov 2016
Ovarian Cancer	Discovery	Denmark	Rigshospitalet	01 Nov 2016

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