IP Library Granted Patent US 12,521,454
Granted Patent B2
US 12,521,454 · App. 16/762,873 · Granted Jan 13, 2026

Patent

Inventors: Andreas Kjaer (Frederiksberg, DK); Jacob Madsen (Copenhagen, DK); Malene Brandt-Larsen (Copenhagen, DK); Jytte Oxboel (Copenhagen, DK)
Assignee: RIGSHOSPITALET
A61K51/0482
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Quick Facts
Patent No.
US 12,521,454
App. No.
16/762,873
Granted
Jan 13, 2026
Kind
B2
Abstract

There is provided two angiogenesis clinical PET tracers, namely 68Ga-NODAGA-E[c(RGDyK)]2 and 64Cu-NODAGA-E[c(RGDyK)]2 for imaging of neo-angiogenesis in humans.

Claims (10)

1 . A method of imaging tissue in a human for detecting progression of angiogenesis in cancer metastasis, said method comprising contacting with or administering to a tissue a compound of formula I,

and

imaging the tissue with a positron emission tomography (PET) imaging system, wherein said cancer metastasis is liver metastasis or lymph node metastasis having a tumor to liver ratio of at least 3.7.

2 . A method of diagnosing the presence of one or more angiogenesis related metastatic cancer diseases in a human comprising:

contacting or administering to a tissue a compound of formula I,

and

imaging the tissue with an imaging system, wherein the imaging includes PET imaging of liver metastases or lymph node metastases having a tumor to liver ratio of at least 3.7, and wherein the location of the compound corresponds to the location of the angiogenesis related metastatic cancer diseases in the human.

3 . The method of claim 2 , wherein the imaging system is a PET imaging system.

4 . A method of imaging tissue in a human for detecting progression of angiogenesis in cancer metastasis, said method comprising contacting with or administering to a tissue [ 64 Cu]NODAGA-E[c(RGDyK)] 2 , and imaging the tissue with an imaging system, wherein the imaging system is a PET imaging system, wherein said cancer metastasis is liver metastasis or lymph node metastasis having a tumor to liver ratio of at least 3.7.

5 . A method of diagnosing the presence of one or more angiogenesis related metastatic cancer diseases in a human comprising contacting or administering to a tissue [ 64 Cu]NODAGA-E[c(RGDyK)] 2 and imaging the tissue with a positron emission tomography (PET) imaging system, wherein the imaging includes imaging of liver metastases or lymph node metastases, and wherein the location of the compound corresponds to the location of the angiogenesis related metastatic cancer diseases in the human, and the metastases have a tumor to liver ratio of at least 3.7.

Assignments (2)
SECURITY INTEREST Recorded Mar 3, 2026
From: QUANTIPHI, INC.
To: CITIBANK, N.A.
Reel/Frame 075018/0042 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 18, 2021
From: KJAER, ANDREAS; MADSEN, JACOB; BRANDT-LARSEN, MALENE; OXBOEL, JYTTE
To: RIGSHOSPITALET
Reel/Frame 055311/0467 →
Priority Claims (1)
DK PA 2017 70845 · Nov 10, 2017 · national
Continuity (1)
Related Publication 20200282084A1 · Sep 10, 2020
References Cited (21)
US 20080267882A1 · Chen et al. · 2008 [cited by applicant]
Zhai et al. (Mol. Pharmaceutics 2015, 12, 2142-2150). [cited by examiner]
Sun et al. (Theranostics 2014, 4, 778-786). [cited by examiner]
Rasmussen et al. (Diagnostics 2016, 6, 1-4). [cited by examiner]
Cai et al. (Bio. Techniques 2005, 39, S14-S25). [cited by examiner]
Kikkawa et al. (Clin. Exper. Metastasis 2002, 19, 717-725). [cited by examiner]
Robertson et al. (Current Pharm. Design 2008, 14, 296-305). [cited by examiner]
International Search Report and Written Opinion from International Application No. PCT/DK2018/050293, mailed Feb. 6, 2019. [cited by applicant]
Chakraborty et al. “Toward realization of mix-and-use approach in Ga radiopharmacy; preparation, evaluation and preliminary clinical utilization of 68Ga-labeled NODAGA-coupled RGD peptide derivative.” Nuclear Medicine a… [cited by applicant]
Oxboel et al. “Comparison of two new angiogenesis PET tracers 68Ga-NODAGA-E(c[RGDyK])2 and Cu-NODAGA-E (c[RGDyK]) in vivo imaging studies in human xenograft tumors.” Nuclear Medicine and Biology (2014), vol. 41 pp. 259-… [cited by applicant]
Rasmussen et al. “Angiogenesis PET Tracer Uptake (68Ga-NODAGA-E(c[RGDyK]) in Induced Myocardial Infarction in Minipigs.” Diagnostics (2016) vol. 6, No. 2. Article 26. [cited by applicant]
ClinicalTrials.gov Identifier NCT02970786 Phase I Trial 68Ga-NODAGA-E(c[RGDyK]) Positron Emission Tomography for Imagining Angiogenesis in Primary and Metastasis Tumor Lesion in Humans. Nov. 22, 2016. [cited by applicant]
ClinicalTrials.gov Identifier NCT03271281: PET/CT Imaging of Angiogenesis in Patients with Neuroendocrine Tumors Using 68Ga-NODAGA-E(c[RGDyK]) Sep. 5, 2017. [cited by applicant]
Eo et al. “Angiogensis Imagining Using 68Ga-RGD PET/CT: Therapeutic Implications.” Seminars in Nuclear Medicine (2016), vol. 46, No. 5. pp. 419-427. [cited by applicant]
Laitinen et al. “Comparision of cyclic RGD peptides for axb3 integrin detection in a rat model of yocardial infarction.” Ejnmmi Research, (2013), vol. 3. No. 1. Article 38. [cited by applicant]
R. Haubner, et al., “[68Ga]NODAGA-RGD—Metabolic Stability, Biodistribution, and Dosimetry Data from Patients with Hepatocellular Carcinoma and Liver Cirrhosis”, Eur J Nucl Med Mol Imaging, DOI 10.1007/s00259-016-3396-3;… [cited by applicant]
P. A. Knetsch, et al., “[68Ga]NODAGA-RGD for Imaging αvβ3 Integrin Expression”, Eur J Nucl Med Mol Imaging, DOI 10.1007/s00259-011-1778-0; (2011) 38: pp. 1303-1312. [cited by applicant]
M. M. Clausen, et al., “First-In-Human Study of [68Ga]Ga-NODAGA-E[c(RGDyK]2 PET for Integrin αvβ3 Imaging in Patients with Breast Cancer and Neuroendocrine Neoplasms: Safety, Dosimetry and Tumor Imaging Ability”, Diagno… [cited by applicant]
M. M. Clausen, et al., “First-In-Human Study of [68Ga]Ga-NODAGA-E[c(RGDyK]2 PET for Integrin αvβ3 Imaging in Patients with Breast Cancer and Neuroendocrine Neoplasms: Safety, Dosimetry and Tumor Imaging Ability”, Diagno… [cited by applicant]
D. J. Kwekkeboom, et al., “Somatostatin Receptor Imaging”, Seminars in Nuclear Medicine, vol. XXXII, No. 2, Apr. 2002, pp. 84-91. [cited by applicant]
F. L. Giesel, et al., “68Ga-FAPI PET/CT: Biodistribution and Preliminary Dosimetry Estimate of 2 DOTA-Containing FAP-Targeting Agents in Patients with Various Cancers”, The Journal of Nuclear Medicine, vol. 60, No. 3, M… [cited by applicant]