Initial experience with 18F-fluoroethylcholine PET/CT in staging and monitoring therapy response of advanced renal cell carcinoma

Middendorp, Marcus; Maute, Luise; Sauter, Bruno; Vogl, Thomas J.; Grünwald, Frank

doi:10.1007/s12149-010-0375-9

Cited by 27 publications

(15 citation statements)

References 18 publications

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“…The ease, relative low cost, noninvasive and high sensitivity of BLI allow rapid screening of large chemical libraries in very small quantities and subsequent SAR studies. Currently, human PET/CT imaging has been used to monitor tumor progression, evaluation, and response to therapy (44-46). PET imaging has also been used for pre-clinical studies for evaluation of the efficacy of different HDACi in small animal models.…”

Section: Discussionmentioning

confidence: 99%

Syntheses and Discovery of a Novel Class of Cinnamic Hydroxamates as Histone Deacetylase Inhibitors by Multimodality Molecular Imaging in Living Subjects

Chan

Smith

et al. 2014

Cancer Research

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Histone deacetylases (HDAC) that regulate gene expression are being explored as cancer therapeutic targets. In this study, we focused on HDAC6 based on its ability to inhibit cancerous Hsp90 chaperone activities by disrupting Hsp90/p23 interactions. To identify novel HDAC6 inhibitors, we used a dual-luciferase reporter system in cell culture and living mice by bioluminescence imaging (BLI). On the basis of existing knowledge, a library of hydrazone compounds was generated for screening by coupling cinnamic hydroxamates with aldehydes and ketones. Potency and selectivity were determined by in vitro HDAC profiling assays, with further evaluation to inhibit Hsp90(α/β)/p23 interactions by BLI. In this manner, we identified compound 1A12 as a dose-dependent inhibitor of Hsp90(α/β)/p23 interactions, UKE-1 myeloid cell proliferation, p21waf1 upregulation, and acetylated histone H3 levels. 1A12 was efficacious in tumor xenografts expressing Hsp90(α)/p23 reporters relative to carrier control–treated mice as determined by BLI. Small animal 18F-FDG PET/CT imaging on the same cohort showed that 1A12 also inhibited glucose metabolism relative to control subjects. Ex vivo analyses of tumor lysates showed that 1A12 administration upregulated acetylated-H3 by approximately 3.5-fold. Taken together, our results describe the discovery and initial preclinical validation of a novel selective HDAC inhibitor.

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Section: Discussionmentioning

confidence: 99%

Syntheses and Discovery of a Novel Class of Cinnamic Hydroxamates as Histone Deacetylase Inhibitors by Multimodality Molecular Imaging in Living Subjects

Chan

Smith

et al. 2014

Cancer Research

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“…Horn et al compared 18 F-FLT and 18 F-FDG for early measurement of response to sunitinib treatment in 20 patients with metastatic RCC and demonstrated that while FLT-PET could be used to identify response as early as 1 week after the start of treatment, 18 F-FDG PET was more effective at a later time point of 3–4 weeks, suggesting that inhibition of VEGF signaling with sunitinib exerts an early effect on tumor proliferation, which is then followed by a reduction in tumor metabolism [24]. Two groups have reported the utility of 18 F-fluoroethylcholine PET [25] and 11 C-acetate PET [26] for staging and monitoring of the response of advanced RCC to therapy. Furthermore, one preliminary report has demonstrated that anti-3- 18 F-FACBC PET showed better conspicuity for papillary RCC than for clear cell RCC [27].…”

Section: Kidney Cancermentioning

confidence: 99%

Update on advances in molecular PET in urological oncology

et al. 2016

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Integrated positron emission tomography/computed tomography (PET/CT) with 2-[18F]fluoro-2-deoxy-D-glucose (18F-FDG) has emerged as a powerful tool for the combined metabolic and anatomic evaluation of many cancers. In urological oncology, however, the use of 18F-FDG has been limited by a generally low tumor uptake, and physiological excretion of FDG through the urinary system. 18F-FDG PET/CT is useful when applied to specific indications in selected patients with urological malignancy. New radiotracers and positron emission tomography/magnetic resonance imaging (PET/MRI) are expected to further improve the performance of PET in uro-oncology.

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“…44 Other novel PET radiotracers To date, several other novel radiotracers have been evaluated for RCC imaging. These include anti-1-amino-3-18 Ffluorocyclobutane-1-carboxylic acid (anti-18 F-FACBC), 46 18 F-fluoroethylcholine, 47 and 18 F-fluoromisonidazole ( 18 F-FMISO). 48 Similar to the case of 89 Zr-bevacizumab and small molecules against PSMA, these tracers have been studied in only a handful of patients and their role in imaging the indeterminate renal mass remains in question.…”

Section: Zr-bevacizumabmentioning

confidence: 99%

Nuclear imaging of renal tumours: a step towards improved risk stratification

2015

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Patients presenting with a clinically localized renal mass should ideally be managed with a risk-adapted approach that incorporates data regarding the metastatic potential of a given tumour. Unfortunately, currently available anatomical imaging techniques are unable to reliably distinguish between the various types of renal tumours, which include both benign and malignant histologies. Nuclear imaging offers a potential noninvasive means to characterize clinically localized renal tumours. A number of nuclear imaging tests are currently under investigation for this purpose and might one day be incorporated into patient care.

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Initial experience with 18F-fluoroethylcholine PET/CT in staging and monitoring therapy response of advanced renal cell carcinoma

Abstract: In this small sample more than half of the RCC metastases were evident in baseline FEC PET. Monitoring therapy, FEC PET showed heterogeneous results in the first case with PD and was consistent with ceCT in the second one displaying PR.

Cited by 27 publications

References 18 publications

Syntheses and Discovery of a Novel Class of Cinnamic Hydroxamates as Histone Deacetylase Inhibitors by Multimodality Molecular Imaging in Living Subjects

Syntheses and Discovery of a Novel Class of Cinnamic Hydroxamates as Histone Deacetylase Inhibitors by Multimodality Molecular Imaging in Living Subjects

Update on advances in molecular PET in urological oncology

Nuclear imaging of renal tumours: a step towards improved risk stratification

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