An improved radiolabelled RNA aptamer molecule for HER2 imaging in cancers

Varmira, Kambiz; Hosseinimehr, Seyed Jalal; Noaparast, Zohreh; Abedi, Seyed Mohammad

doi:10.3109/1061186x.2013.839688

Cited by 41 publications

(15 citation statements)

References 27 publications

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“…Although preclinical studies were successful [45,46,47,48,49], only a few clinical studies have been reported and results were disappointing since radiotracer uptake in tumors was absent or low [50,51]. Also, radiolabeled HER2-targeting RNA aptamers were synthesized for targeting HER2-positive BC lesions [52]. These studies are still in a preclinical setting and their advantage to HER2-targeting antibodies, affibodies, and nanobodies remains to be established.…”

Section: Human Epidermal Growth Factor Receptor 2 (Her2)-targeted mentioning

confidence: 99%

Review: Receptor Targeted Nuclear Imaging of Breast Cancer

Dalm

Verzijlbergen

Jong

2017

IJMS

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Receptor targeted nuclear imaging directed against molecular markers overexpressed on breast cancer (BC) cells offers a sensitive and specific method for BC imaging. Currently, a few targets such as estrogen receptor (ER), progesterone receptor (PR), human epidermal growth factor receptor 2 (HER2), somatostatin receptor (SSTR), and the gastrin releasing peptide receptor (GRPR) are being investigated for this purpose. Expression of these targets is BC subtype dependent and information that can be gained from lesion visualization is dependent on the target; ER-targeting radiotracers, e.g., can be used to monitor response to anti-estrogen treatment. Here we give an overview of the studies currently under investigation for receptor targeted nuclear imaging of BC. Main findings of imaging studies are summarized and (potential) purposes of lesion visualization by targeting these molecular markers are discussed. Since BC is a very heterogeneous disease and molecular target expression can vary per subtype, but also during disease progression or under influence of treatment, radiotracers for selected imaging purposes should be chosen carefully.

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Section: Human Epidermal Growth Factor Receptor 2 (Her2)-targeted mentioning

confidence: 99%

Review: Receptor Targeted Nuclear Imaging of Breast Cancer

Dalm

Verzijlbergen

Jong

2017

IJMS

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“…An increasing accumulation of radiolabelled aptamer in time (up to 5 h p.i.) has been often observed with other aptamers [19,20,[47][48][49].…”

Section: Tumour Uptakementioning

confidence: 99%

“…Several aptamers targeting HER2 have been reported [11][12][13][14][15][16][17][18]. So far, only one of these aptamers has been radiolabelled (with 99mTc) and its biodistribution was evaluated ex vivo [19,20].…”

Section: Introductionmentioning

confidence: 99%

Biodistribution of Novel 68Ga-Radiolabelled HER2 Aptamers in Mice

Gijs¹,

Becker

Plenevaux

et al. 2016

J Nucl Med Radiat Ther

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“…A modified RNA aptamer with HER2-specific targeting was labeled with 99m Tc and allowed SPECT imaging of HER2 expression (26,27). Another group used 64 Cu-WT4340 for PET imaging of HER2 messenger RNA and also demonstrated its successful use for evaluating the therapeutic efficacy of doxorubicin therapy in immunocompromised mice carrying human HER2-positive BC xenografts (28).…”

Section: Preclinical Settingmentioning

confidence: 99%

Imaging Diagnostic and Therapeutic Targets: Human Epidermal Growth Factor Receptor 2

et al. 2016

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Since the approval of trastuzumab, a humanized monoclonal antibody against the extracellular domain of human epidermal growth factor receptor 2 (HER2), 3 other HER2-targeting agents have gained regulatory approval: lapatinib, pertuzumab, and trastuzumab-emtansine. These agents have revolutionized the management of HER2-positive breast cancer, highlighting the concept that targeted therapies are successful when patients exhibit tumor-selective expression of a molecular target-in this case, HER2. However, response prediction and innate or acquired resistance remain serious concerns. Predictive biomarkers of a response-which could help in the selection of patients who might benefit from a selected targeted therapy-are currently lacking. Molecular imaging with anti-HER2 probes allows the noninvasive, whole-body assessment of HER2 tumor burden and has the potential to improve patient selection, optimize the dose and schedule, and rationalize assessment of the response to anti-HER2 therapies. Furthermore, unlike biopsy-based HER2 assessment, this approach can reveal inter-or intratumoral heterogeneity as well as variations in HER2 expression over time. This review summarizes the available literature and the current status of molecular imaging as a tool for the assessment of HER2 (target) expression or the prediction of an early treatment response in early and advanced HER2-positive breast cancer. Human epidermal growth factor receptor 2 (HER2) is overexpressed in several cancers, including breast, gastric, ovary, prostate, bladder, and lung cancers, and is a proven therapeutic target in the first 2 tumor types (1,2). In breast cancer (BC), in particular, HER2 overexpression is found in 15%-25% of patients and is associated with a clinically aggressive course. Successful targeting of HER2 with a range of anti-HER2 drugs has resulted in markedly improved patient outcomes in both advanced and early disease settings (3).However, the presence of a target (in this case, HER2) does not always guarantee benefit from matched targeted therapies because downstream signaling resistance or escape can occur. In HER2-overexpressing BC, it has been estimated that about 50% of patients with metastases do not benefit from anti-HER2 therapies (4), and not a single biomarker for identifying nonresponding patients has yet been validated (5).Furthermore, there is increasing evidence of temporal and spatial heterogeneity in BC HER2 overexpression. Patients with negative test results at diagnosis can have positive test results later in the disease course and vice versa, a fact that explains why biopsy of metastatic disease is a strong recommendation of many clinical treatment guidelines (6). Heterogeneity in biomarker expression at metastatic sites is only beginning to be recognized, with growing appreciation for molecular imaging.This article focuses on HER2-positive BC and provides a comprehensive overview of the present and future roles of molecular imaging in improving target mapping, predicting benefit from chemotherapy with or without ...

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An improved radiolabelled RNA aptamer molecule for HER2 imaging in cancers

Cited by 41 publications

References 27 publications

Review: Receptor Targeted Nuclear Imaging of Breast Cancer

Review: Receptor Targeted Nuclear Imaging of Breast Cancer

Biodistribution of Novel 68Ga-Radiolabelled HER2 Aptamers in Mice

Imaging Diagnostic and Therapeutic Targets: Human Epidermal Growth Factor Receptor 2

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