Production, applications and status of zirconium-89 immunoPET agents

Jalilian, Amir Reza; Osso, João Alberto

doi:10.1007/s10967-017-5358-z

Cited by 15 publications

(8 citation statements)

References 78 publications

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“…[30,31] Copper-64 and its other isotopes ( 60 Cu, 61 Cu, 62 Cu, 67 Cu) have been shown to complex to many chelating agents with high stability, including to a number of derivatised cyclam macrocycles, and have been used in many radiopharmaceutical applications. [30][31][32][33][34] While copper-64 and the other copper isotopes are mostly used for diagnostic purposes, copper-67 (t1/2 = 61.8 h) emits beta (β -) particles of 580 keV (100%) (penetration range of 2.1 mm) with gamma rays of 92 and 184 keV being useful for therapeutic applications. Copper-64 and copper-67 together form a theranostic isotope pair that can be used for diagnosis and therapy.…”

Section: Introductionmentioning

confidence: 99%

Towards the Development of a Targeted Albumin-Binding Radioligand for Theranostic Applications: Synthesis, Radiolabelling and Preliminary In Vivo Studies

Driver

Ebenhan²,

Zeevaart³

et al. 2020

Preprint

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GluCAB is a newly synthesised macrocyclic radioligand designed to bind <i>in vivo</i> to albumin (HSA) for the purpose of development as a dual-targeting oncological theranostic agent. Subsequent to its synthesis and <sup>64</sup>Cu-radiolabelling, this radioligand has show a prolonged circulation time in healthy mice but with appropriate systemic clearance within 24 h. This radioligand meets the criteria to be further investigated for tumour targeting and uptake.

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Section: Introductionmentioning

confidence: 99%

Towards the Development of a Targeted Albumin-Binding Radioligand for Theranostic Applications: Synthesis, Radiolabelling and Preliminary In Vivo Studies

Driver

Ebenhan²,

Zeevaart³

et al. 2020

Preprint

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“…89 Zr immunoPET continues to drive research and development in the field of the application of mAbs in PET molecular imaging [ 33 ] and has shown great potential in cancer imaging [ 34 ]. Although 89 Zr-immunoPET is a highly attractive technique to measure tumour-associated antigens as well as the in vivo distribution of mAbs, it has to be mentioned that it is restrained by a few limitations.…”

Section: Resultsmentioning

confidence: 99%

MT1-MMP as a PET Imaging Biomarker for Pancreas Cancer Management

Morcillo

Lucas

Oteo

et al. 2018

Contrast Media & Molecular Imaging

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Pancreatic ductal adenocarcinoma (PDAC) continues to be one of the deadliest cancers for which optimal diagnostic tools are still greatly needed. Identification of PDAC-specific molecular markers would be extremely useful to improve disease diagnosis and follow-up. MT1-MMP has long been involved in pancreatic cancer, especially in tumour invasion and metastasis. In this study, we aim to ascertain the suitability of MT1-MMP as a biomarker for positron emission tomography (PET) imaging. Two probes were assessed and compared for this purpose, an MT1-MMP-specific binding peptide (MT1-AF7p) and a specific antibody (LEM2/15), labelled, respectively, with 68Ga and with 89Zr. PET imaging with both probes was conducted in patient-derived xenograft (PDX), subcutaneous and orthotopic, PDAC mouse models, and in a cancer cell line (CAPAN-2)-derived xenograft (CDX) model. Both radiolabelled tracers were successful in identifying, by means of PET imaging techniques, tumour tissues expressing MT1-MMP although they did so at different uptake levels. The 89Zr-DFO-LEM2/15 probe showed greater specific activity compared to the 68Ga-labelled peptide. The mean value of tumour uptake for the 89Zr-DFO-LEM2/15 probe (5.67 ± 1.11%ID/g, n=28) was 25–30 times higher than that of the 68Ga-DOTA-AF7p ones. Tumour/blood ratios (1.13 ± 0.51 and 1.44 ± 0.43 at 5 and 7 days of 89Zr-DFO-LEM2/15 after injection) were higher than those estimated for 68Ga-DOTA-AF7p probes (of approximately tumour/blood ratio = 0.5 at 90 min after injection). Our findings strongly point out that (i) the in vivo detection of MT1-MMP by PET imaging is a promising strategy for PDAC diagnosis and (ii) labelled LEM2/15 antibody is a better candidate than MT1-AF7p for PDAC detection.

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“…Immuno-positron emission tomography is an imaging technique that, using radio-labeled monoclonal antibodies, allows tracking and quantifying their distribution in the body, and can be applied to imaging of human malignancies. Zirconium-89 has a primary role in immunoPET being used in most of the diagnoses based on radioactive antibodies [59]. Its favorable characteristics are a half-life of 3.3 days which allows a manageable production and distribution, and the favorable decay mode where the unavoidable gamma rays have energies well distinguishable from PET photons.…”

Section: The Radionuclides Used In Nuclear Medicinementioning

confidence: 99%