Simple new method for labelling of PSMA-11 with 68Ga in NaHCO3

Urbanová, Kamila; Seifert, Dirk; Vinšová, Hana; Vlk, Martin; Lebeda, O.

doi:10.1016/j.apradiso.2021.109692

Cited by 7 publications

(4 citation statements)

References 24 publications

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“…Recent cancer statistics reported by the American Cancer Society in 2020 show that prostate cancer (PCa) is a leading cause of cancer-related death in men . Prostate-specific membrane antigen (PSMA) is a type II transmembrane protein enzyme, which hydrolyzes N -acetyl-aspartylglutamate and folyl-poly-γ-glutamates. − It is highly expressed in poorly differentiated, metastatic, and castration-resistant prostate cancer; therefore, PSMA is a favorable target for molecular imaging and radionuclide therapy of prostate cancer (Figure ). ,− Two PSMA-targeting imaging agents, [ 68 Ga]Ga-PSMA-11 (Locametz, gallium Ga-68 gozetotide) and [ 18 F]DCFPyL (PYLARIFY, piflufolastat F18), were approved by the FDA in the past two years. , Importantly, for radionuclide therapy of prostate cancer, [ 177 Lu]Lu-PSMA-617 (Pluvicto, lutetium Lu-177 vipivotide tetraxetan) was also approved by the FDA in March 2022. ,, It is now available as a radionuclide therapeutic agent for the treatment of advanced prostate cancer.…”

Section: Introductionmentioning

confidence: 99%

New PSMA-Targeting Ligands: Transformation from Diagnosis (Ga-68) to Radionuclide Therapy (Lu-177)

Zha¹,

Choi²,

et al. 2022

J. Med. Chem.

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Prostate-specific membrane antigen (PSMA) is a promising target for the diagnosis and radionuclide therapy of prostate cancer. This study reports conversion of a previously reported 68Ga-imaging agent, [68Ga]Ga-P16-093, to a Lu-177 radionuclide therapeutic agent. Substitution of the HBED-CC metal chelating group with DOTA(GA)2 led to P17-087 (4) and P17-088 (7). Both agents showed excellent PSMA binding affinity (IC50 = 10–30 nM) comparable to that of recently FDA-approved [177Lu]Lu-PSMA-617 (Pluvicto). Biodistribution studies in PSMA expressing tumor bearing mice showed that [177Lu]Lu-4 exhibited very high tumor uptake and a fast blood clearance similar to those of [177Lu]Lu-PSMA-617. Conversely, [177Lu]Lu-7, containing an albumin binder, extended its blood half-life and exhibited significantly higher uptake and longer tumor residence time than [177Lu]Lu-4 and [177Lu]Lu-PSMA-617. The switch from chelator HBED-CC to DOTA(GA)2 and the switch from the imaging isotope gallium-68 to the therapeutic isotope lutetium-177 have successfully transformed a PSMA-targeting agent from diagnosis to promising radionuclide therapeutic agents.

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Section: Introductionmentioning

confidence: 99%

New PSMA-Targeting Ligands: Transformation from Diagnosis (Ga-68) to Radionuclide Therapy (Lu-177)

Zha¹,

Choi²,

et al. 2022

J. Med. Chem.

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“…In the method based on labeling the radionuclide with NaHCO 3 , it is directly labeled with an aqueous solution of PSMA11, which provides quantitative labeling within 5 min at laboratory temperature 21 . The final product pH was adjusted to 7 with phosphate buffer.…”

Section: Discussionmentioning

confidence: 99%

Comparison of three different methods in [⁶⁸Ga]Ga‐PSMA11 radiolabeling

Yüksel

Uğur

2022

Labelled Comp Radiopharmac

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In this study, quality control parameters such as radiochemical yield, radiochemical purity, and in vitro stability of gallium (68Ga)‐prostate‐specific membrane antigen‐11 ([68Ga]Ga‐PSMA11) radiopharmaceutical obtained in a research laboratory with three different synthesis algorithms were evaluated and compared. Gallium (68Ga) chloride precursor to be used in labeling in all three methods was obtained by using ITG brand 68Ge/68Ga generator. The first method for the [68Ga]Ga‐PSMA11 radiopharmaceutical was performed with the automated synthesis module, which is widely used in clinical practice. Its radiochemical yield, quality assurance, and stability met expectations. Radiolabeling success, suitability of quality control parameters, and in vitro stability of [68Ga]Ga‐PSMA11 radiopharmaceutical performed with ANMI kit were examined. The final product showed success in 68Ga‐complexation kinetics. All quality control criteria performed met the expectation for clinical applications. Direct cold labeling of PSMA11 ligand with sodium bicarbonate buffer was examined. Results were similar to the ANMI kit. Considering that all three methods are successful in radiochemical labeling, labeling with NaHCO3 buffer shows the labeling preference when we choose the cheap, practical, and easy labeling option.

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“…In a recent work, Urbanová et al designed a new automated labeling method of PSMA-11 that minimizes chemicals use and purification steps, providing quantitative labeling yields at room temperature. They tested and demonstrated that labeling the PSMA-11 ligand with 68 Ga in 0.1 M NaHCO 3 (in a pH range between 7.2 and 9.0) using an SPE reversed-phase mixed-mode cation exchanger cartridge was rapid, simple, and reproducible, avoiding heating and more complex purification steps [ 82 ].…”

Section: Main Technological Strategies and Examples Of Imaging Agents Developed For Improving Diagnostic Efficiencymentioning

confidence: 99%

The Pharmaceutical Technology Approach on Imaging Innovations from Italian Research

et al. 2021

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Many modern therapeutic approaches are based on precise diagnostic evidence, where imaging procedures play an essential role. To date, in the diagnostic field, a plethora of agents have been investigated to increase the selectivity and sensitivity of diagnosis. However, the most common drawbacks of conventional imaging agents reside in their non-specificity, short imaging time, instability, and toxicity. Moreover, routinely used diagnostic agents have low molecular weights and consequently a rapid clearance and renal excretion, and this represents a limitation if long-lasting imaging analyses are to be conducted. Thus, the development of new agents for in vivo diagnostics requires not only a deep knowledge of the physical principles of the imaging techniques and of the physiopathological aspects of the disease but also of the relative pharmaceutical and biopharmaceutical requirements. In this scenario, skills in pharmaceutical technology have become highly indispensable in order to respond to these needs. This review specifically aims to collect examples of newly developed diagnostic agents connoting the importance of an appropriate formulation study for the realization of effective products. Within the context of pharmaceutical technology research in Italy, several groups have developed and patented promising agents for fluorescence and radioactive imaging, the most relevant of which are described hereafter.

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Simple new method for labelling of PSMA-11 with 68Ga in NaHCO3

Cited by 7 publications

References 24 publications

New PSMA-Targeting Ligands: Transformation from Diagnosis (Ga-68) to Radionuclide Therapy (Lu-177)

New PSMA-Targeting Ligands: Transformation from Diagnosis (Ga-68) to Radionuclide Therapy (Lu-177)

Comparison of three different methods in [⁶⁸Ga]Ga‐PSMA11 radiolabeling

The Pharmaceutical Technology Approach on Imaging Innovations from Italian Research

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Simple new method for labelling of PSMA-11 with 68Ga in NaHCO3

Cited by 7 publications

References 24 publications

New PSMA-Targeting Ligands: Transformation from Diagnosis (Ga-68) to Radionuclide Therapy (Lu-177)

New PSMA-Targeting Ligands: Transformation from Diagnosis (Ga-68) to Radionuclide Therapy (Lu-177)

Comparison of three different methods in [68Ga]Ga‐PSMA11 radiolabeling

The Pharmaceutical Technology Approach on Imaging Innovations from Italian Research

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Comparison of three different methods in [⁶⁸Ga]Ga‐PSMA11 radiolabeling