One-step radiosynthesis and initial evaluation of a small molecule PET tracer for PD-L1 imaging

Miao, Yinxing; Lv, Gaochao; Chen, Yinfei; Qiu, Ling; Xie, Minhao; Lin, Jianguo

doi:10.1016/j.bmcl.2020.127572

Cited by 27 publications

(79 citation statements)

References 27 publications

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“…[15] mAb Df-Nivolumab 89 Zr PET 3.75 nM [16][17][18] mAb Df-Pembrolizumab 89 Zr PET n.a. [19,20] Keytruda 64 Cu 89 Zr PET n.a. [21,22] N-sucDf-Pembrolizumab 89 Zr PET n.a.…”

Section: Class Substance Namementioning

confidence: 99%

Development of Radiotracers for Imaging of the PD-1/PD-L1 Axis

2022

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Immune checkpoint inhibitor (ICI) therapy has emerged as a major treatment option for a variety of cancers. Among the immune checkpoints addressed, the programmed death receptor 1 (PD-1) and its ligand PD-L1 are the key targets for an ICI. PD-L1 has especially been proven to be a reproducible biomarker allowing for therapy decisions and monitoring therapy success. However, the expression of PD-L1 is not only heterogeneous among and within tumor lesions, but the expression is very dynamic and changes over time. Immunohistochemistry, which is the standard diagnostic tool, can only inadequately address these challenges. On the other hand, molecular imaging techniques such as positron emission tomography (PET) and single-photon emission computed tomography (SPECT) provide the advantage of a whole-body scan and therefore fully address the issue of the heterogeneous expression of checkpoints over time. Here, we provide an overview of existing PET, SPECT, and optical imaging (OI) (radio)tracers for the imaging of the upregulation levels of PD-1 and PD-L1. We summarize the preclinical and clinical data of the different molecule classes of radiotracers and discuss their respective advantages and disadvantages. At the end, we show possible future directions for developing new radiotracers for the imaging of PD-1/PD-L1 status in cancer patients.

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“…[15] mAb Df-Nivolumab 89 Zr PET 3.75 nM [16][17][18] mAb Df-Pembrolizumab 89 Zr PET n.a. [19,20] Keytruda 64 Cu 89 Zr PET n.a. [21,22] N-sucDf-Pembrolizumab 89 Zr PET n.a.…”

Section: Class Substance Namementioning

confidence: 99%

Development of Radiotracers for Imaging of the PD-1/PD-L1 Axis

2022

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“…Miao et al reported the radiosynthesis of the small molecule PD-L1 inhibitor [ 18 F]LN via 18 F- 19 F isotope exchange reaction [55]. [ 18 F]LN was achieved with a high radiochemical purity above 95%.…”

Section: Pd-1/pd-l1 Targeting Radiotracersmentioning

confidence: 99%

“…Some radiotracers targeting other diseases have also been developed including a purinergic receptor P2X7 antagonist [ 18 F]F-PTTP for the detection of inflammation [78], [ 99m Tc]Tc-GlcNAc-PEI (N-acetylglucosamine (GlcNAc) conjugated polyethylenimine (PEI)) specifically interacts with desmin and vimentin expressed on activated hepatic stellate cells (HSCs) for assessing liver fibrosis [79], [ 18 F] FPGal based on isotonicamide for the imaging of asialoglycoprotein receptor (ASGPR) related liver disease [80], and [ 68 Ga]Ga-HZ20 for the quantitative analysis of angiotensin Mi [48], Yu [51] Feng [49], Gao [52] Ma Xing [54] Miao [55], Huang [56] Jiang [57], Huang [58] Yang [ converting enzyme 2 (ACE2) expression in novel coronavirus sensitive organs [81].…”

Section: Imaging Agents For Other Diseasesmentioning

confidence: 99%

Current status and future perspective of radiopharmaceuticals in China

Ji¹,

Li²,

Sui³

et al. 2021

Eur J Nucl Med Mol Imaging

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“…Finally, another [ 18 F]labeled small molecule inhibitor, [ 18 F]LN, was designed in 2020 by Yinxing et al [79] to evaluate PET imaging in both PD-L1 transfected (A375-hPD-L1) and non-transfected (A375) melanoma-bearing mice. Authors observed that tumor uptake (1.96 ± 0.27 %ID/g) reached the maximum at 15 min in the positive group, being 2.2-fold higher than in the negative (0.89 ± 0.31 %ID/g) or the blocked (1.07 ± 0.26 %ID/g) group.…”

Section: Radiolabeled Small Moleculesmentioning

confidence: 99%

Molecular Imaging in Immunotherapy: A Systematic Review

Liberini¹,

Laudicella²,

Capozza³

et al. 2021

Preprint

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Immunotherapy is an effective therapeutic option for several cancers. In the last years, the introduction of checkpoint inhibitors (ICIs) has shifted the therapeutic landscape in oncology and improved patient prognosis in a variety of neoplastic diseases. However, to date, the selection of the best patients eligible for these therapies, as well as the response assessment is still challenging. Patients are mainly stratified using immunohistochemical analysis of the expression of anti-gens on biopsy specimens, such as PD-L1 and PD-1, on tumor cells, on peritumoral immune cells, and/or in the tumor microenvironment (TME). Recently, the use and development of imaging biomarkers able to assess in-vivo cancer-related processes are becoming more important. Today, positron emission tomography (PET) with 2-deoxy-2-[18F]fluoro-D-glucose ([18F]FDG) is used routinely to evaluate tumor metabolism, and also to predict and monitor response to immunotherapy. Although highly sensitive, FDG-PET, in general, is rather unspecific. Novel radiopharmaceuticals (immuno-PET radiotracers) able to identify specific immune system targets are under investigation in pre-clinical and clinical settings. In this review, we will provide an overview of the main new immuno-PET radiotracers in development. We will also review the main players (immune cells, tumor cells, and molecular targets) involved in immunotherapy. Furthermore, we report current applications and the evidence of using [18F]FDG PET in immunotherapy, including the use of artificial intelligence (AI).

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One-step radiosynthesis and initial evaluation of a small molecule PET tracer for PD-L1 imaging

Cited by 27 publications

References 27 publications

Development of Radiotracers for Imaging of the PD-1/PD-L1 Axis

Development of Radiotracers for Imaging of the PD-1/PD-L1 Axis

Current status and future perspective of radiopharmaceuticals in China

Molecular Imaging in Immunotherapy: A Systematic Review

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