The positron emission tomography (PET) radioisotope zirconium-89 (89 Zr) is particularly suited for antibody imaging, ... 25 µg and 100 µg for each tracer. PET quantification showed [89 Zr] ...
Zirconium-89 has attracted huge interests and is used in tracing and quantification of slow biological processes and labeling of long half-live biomolecules such as monoclonal antibodies for pharmacokinetic studies and clinical trials. In this review, a concise introduction to targetry, irradiation data, separation and coordination chemistry …
Immuno-PET using desferrioxamine (DFO)-conjugated zirconium-89 ([89Zr]Zr4+)-labeled antibodies is a powerful tool used for preclinical and clinical molecular imaging. However, a comprehensive study evaluating the variables involved in DFO-conjugation and 89Zr-radiolabeling of antibodies, and their impact on the in vitro and in …
Immuno-PET using desferrioxamine (DFO)-conjugated zirconium-89 ([89 Zr]Zr 4+)-labeled antibodies is a powerful tool used for preclinical and clinical molecular imaging.However, a comprehensive study evaluating the variables involved in DFO-conjugation and 89 Zr-radiolabeling of antibodies, and their impact on the in vitro and in …
The positron emitter zirconium-89 (89Zr) has very attractive properties for positron emission tomography (PET) imaging of intact monoclonal antibodies (mAbs) using immuno-PET. ... Trace metal ions ...
Immuno-PET detection of LAG-3 expressing intratumoral lymphocytes using the zirconium-89 radiolabeled fully human anti-LAG-3 antibody REGN3767 [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2018; 2018 Apr 14-18; Chicago, IL. Philadelphia (PA): AACR; Cancer Res 2018;78(13 …
Objective: To investigate the imaging and biodistribution of a novel zirconium-89 (89 Zr)-labeled mouse anti-cd20 monoclonal antibody (mAb) in control and experimental autoimmune encephalomyelitis (EAE) mice following subcutaneous (s. c.) and intravenous (i.v.) administration. Background: Anti-cd20-mediated B-cell depletion using …
89 Zr is an emerging radionuclide that plays an essential role in immuno-positron emission tomography (PET) imaging. The long half-life of 89 Zr (t 1/2 = 3.3 days) is favorable for evaluating the in vivo distribution of monoclonal antibodies. Thus, the use of 89 Zr is promising for monitoring antibody-based cancer therapies. Immuno-PET combines …
Positron emission tomography (PET) imaging is used in drug development to noninvasively measure biodistribution and receptor occupancy. Ideally, PET tracers retain target binding and biodistribution properties of the investigated drug. Previously, we developed a zirconium-89 PET tracer based on a long-circulating glucagon-like peptide …
Metallic radionuclides conjugated to biological vectors via an appropriate chelator are employed in nuclear medicine for the diagnosis (imaging) and radiotherapy of diseases. For the application of radiolabeled antibodies using positron emission tomography (immunoPET), zirconium-89 has gained increasing interest over the last decades as its …
Zirconium-89 is an effective radionuclide for antibody-based positron emission tomography (PET) ... An improved chelator for 89 Zr 4+ could eliminate the release of osteophilic 89 Zr 4+ and lead to a safer PET tracer with reduced background radiation dose. Herein, we present an octadentate chelator 3,4,3-(LI-1,2-HOPO) (or …
Zirconium-89 (t 1/2 = 78.4 h) with a 23% positron decay branch and a maximum positron energy of 0.9 MeV is the preferred isotope for evaluation of radiopharmaceuticals with extended pharmacokinetics including large proteins, antibodies, and nanomaterials. Given its increasing commercial availability, zirconium-89 is supplanting copper-64, which ...
Molecular imaging is based on two important concepts of the "Tracer Principle" and the "Magic Bullet", which were developed respectively by George de Hevey and Paul Ehrlich. ... (64 Cu) and zirconium-89 (89 Zr) . Zirconium-89 (89 Zr) Early studies about 89 Zr and its radiochemistry were reported (in the 1960 s) by the National …
Abstract. The interest in zirconium-89 ( 89 Zr) as a positron-emitting radionuclide has grown considerably over the last decade due to its standardized production, long half-life of 78.2 h, favorable decay characteristics for positron emission tomography (PET) imaging and its successful use in a variety of clinical and preclinical …
A direct comparison between 89 Zr-bevacizumab and an irrelevant 89 Zr-labeled IgG revealed a significantly higher tumor uptake of 89 Zr-bevacizumab in nude mice with human ovarian SK-OV-3 tumors . Besides using 89 Zr-bevacizumab as PET tracer for noninvasive in vivo imaging of VEGF expression in the tumor microenvironment, …
Zirconium-89 is a β+-emitting radiometal with a relatively long physical half-life (t ½ = 3.27 days) that matches the biological half-life of antibodies and intact cells, allowing imaging at later time points not possible with …
Here, we aimed to develop an improved zirconium-89-labeled GLP-1RA with increased molar activity to increase the uptake in low receptor density tissues, such …
We assessed safety, imaging dose and timing, pharmacokinetics and immunogenicity of zirconium-89-labeled, CD8-specific, one-armed antibody positron emission tomography tracer …
Purpose: We evaluated the dosimetry of [(89)Zr]rituximab, an anti-CD20 immunoPET tracer to image B cell non-Hodgkin's lymphoma (NHL) using a humanized transgenic mouse model that expresses human CD20 transgenic mice (huCD20TM). Procedures: Rituximab was conjugated to desferrioxamine (Df) for radiolabeling of Zirconium-89. …
Purpose Tracking cells in vivo using imaging can provide non-invasive information to understand the pharmacology, efficacy, and safety of novel cell therapies. Zirconium-89 (t1/2 = 78.4 h) has recently been used to synthesize [89Zr]Zr(oxinate)4 for cell tracking using positron emission tomography (PET). This work presents an in vitro …
Biomedical Utility The importance of zirconium-89 in PET lies in its ability to facilitate the in vivo tracking of targeting vectors that require extended amounts of time to achieve optimal target-to-background contrast ratios. Over the last decade, the standardization of its production and commercial availability has paved the way for the …
Objectives: The aim of this study was to design a novel tracer targeting programmed cell death-ligand 2 (PD-L2) to dynamically monitor PD-L2 expression and perform preclinical screening to identify patients who may benefit from immune checkpoint inhibitor therapy (ICI) therapy. Methods: 89 Zr labelling of DFO-conjugated PD-L2 antibody (ATL2) was …
The objectives of the study are to determine the dosimetry and whole body distribution of the novel PET tracer, 89 Zr-VRC01, ... Zirconium-89 (half-life = 78.4 h, 23% positron emission) was then ...
The production of 89Zr, the bioconjugation strategies, and applications in (pre-)clinical studies of 89Zr-based immuno-PET in oncology will be discussed, and the ongoing development of new 89ZR-labeled antibodies directed against novel tumor targets is expected to expand applications in the medical imaging. Antibody based positron …
Zirconium-89 half-life of ca. 3.3 days matches the pharmacokinetics of antibodies (half-life of 3–4 days), thus rendering a more suitable isotope for antibody-based immuno-PET imaging with respect to other metallic radioisotopes such as copper-64 or yttrium-86 [4].An additional reason why zirconium-89 has been deemed in the past …
In recent years the field is focused on (89)Zr, a radiometal with near ideal physical and chemical properties for immuno-PET. In this review we will discuss the production of (89)Zr, the bioconjugation strategies, and applications in (pre-)clinical studies of (89)Zr-based immuno-PET in oncology. To date, (89)Zr-based PET imaging has been ...
The study will be executed in collaboration with TRACER B.V. ("TRACER"), a CRO specializing in molecular imaging techniques and fast in-human clinical trials. The project is performed under The TRACER Excellence Program (TEP). The study will be based on APAC that is coupled to zirconium-89 without altering the functionalities of …
The PET isotope zirconium-89 (89 Zr; t 1/2 =78.4 hours) is favorable for radiolabeling mAbs, as its physical half-life matches the time mAbs require for optimal target-to-background signals.47 Recently, a first-in-human PET imaging study with 89 Zr-labeled atezolizumab (anti-PD-L1) showed that tracer uptake appeared to be a predictor of ...
We herein demonstrate the zirconium-89 (Zr-89) conjugation and radiolabeling of IIIB6 in vitro and in vivo ... Representative maximum intensity projections (MIP) of a athymic nude mouse injected with 10.1 MBq [89 Zr]IIIB6. Following tracer injection, microPET/CT images were acquisited for 20 min at a 2 h, b 4 h, c 6 h and d 24 …
Purpose: Although lymphocyte activation gene-3 (LAG-3) directed therapies demonstrate promising clinical anti-cancer activity, only a subset of patients seems to benefit and predictive biomarkers are lacking. Here, we explored the potential use of the anti-LAG-3 antibody tracer [89 Zr]Zr-BI 754111 as a predictive imaging biomarker and …
Here we present the initial results from a first-in-human study to assess the feasibility of imaging with zirconium-89-labeled atezolizumab (anti-PD-L1), including ... a function of tracer exposure and target expression, was high in lymphoid tissues and at sites of inflammation. In tumors, uptake was generally high but heterogeneous, varying ...
A direct comparison between 89 Zr-bevacizumab and an irrelevant 89 Zr-labeled IgG revealed a significantly higher tumor uptake of 89 Zr-bevacizumab in nude mice with human ovarian SK-OV-3 tumors . Besides using 89 Zr-bevacizumab as PET tracer for noninvasive in vivo imaging of VEGF expression in the tumor microenvironment, …
Zirconium-89 is a residualizing, positron-emitting radionuclide whose physical half-life provides an excellent match for the pharmacokinetic profiles of many antibodies. …