An efficient radiosynthesis of [18F]fluoromisonidazole

Lim, Jean-Luc; Berridge, Marc S.

doi:10.1016/0969-8043(93)90110-v

Cited by 103 publications

(63 citation statements)

References 15 publications

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“…was produced by the nucleophilic fluorination of 1-(2 0 -nitro-1 0 -imidazolyl)-2-O-tetrahydropyranyl-3-O-toluenesulphonylpropandiole followed by acidic hydrolysis of the protecting group, as described by Lim and Berridge (1993).…”

Section: Radiolabelled Tracermentioning

confidence: 99%

Evaluation of hypoxia in an experimental rat tumour model by [18F]Fluoromisonidazole PET and immunohistochemistry

et al. 2004

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This study aimed to evaluate tumour hypoxia by comparing [ 18 F]Fluoromisonidazole uptake measured using positron emission tomography ([ 18 F]FMISO-PET) with immunohistochemical (IHC) staining techniques. Syngeneic rhabdomyosarcoma (R1) tumour pieces were transplanted subcutaneously in the flanks of WAG/Rij rats. Tumours were analysed at volumes between 0.9 and 7.3 cm 3 . Hypoxic volumes were defined using a 3D region of interest on 2 h postinjection [ 18 F]FMISO-PET images, applying different thresholds (1.2 -3.0). Monoclonal antibodies to pimonidazole (PIMO) and carbonic anhydrase IX (CA IX), exogenous and endogenous markers of hypoxia, respectively, were used for IHC staining. Marker-positive fractions were microscopically measured for each tumour, and hypoxic volumes were calculated. A heterogeneous distribution of hypoxia was observed both with histology and

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Section: Radiolabelled Tracermentioning

confidence: 99%

Evaluation of hypoxia in an experimental rat tumour model by [18F]Fluoromisonidazole PET and immunohistochemistry

et al. 2004

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“…The radiosynthesis of [ 18 F]FMISO was carried out at the Paul Scherrer Institute according to the two-step procedure reported by Lim and Berridge (15). PET experiments were undertaken using the 16-module variant of the NanoPET tomograph (Oxford Positron Systems; Weston-on-the-Green, United Kingdom) with performance characteristics as reported elsewhere (16).…”

Section: Methodsmentioning

confidence: 99%

Ionizing Radiation Antagonizes Tumor Hypoxia Induced by Antiangiogenic Treatment

Riesterer

Honer

Jochum

et al. 2006

Clinical Cancer Research

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Purpose: The combined treatment modality of ionizing radiation with inhibitors of angiogenesis is effective despite the supposition that inhibition of angiogenesis might increase tumor hypoxia and thereby negatively affect radiation sensitivity. To directly assess this still controversial issue, we analyzed treatment-dependent alterations of tumor oxygenation in response to inhibition of angiogenesis alone, ionizing radiation, and combined treatment. Experimental Design: Serial measurements with high-resolution [18 F]fluoromisonidazole positron emission tomography and immunohistochemical detection of the endogenous hypoxia marker glucose transporter-1 were done to determine tumor hypoxia in a murine mammary carcinoma allograft model. Results: Inhibition of angiogenesis with the clinically relevant vascular endothelial growth factor receptor tyrosine kinase inhibitor PTK787/ZK222584 reduced microvessel density but had only minimal effects on tumor growth, tumor cell apoptosis, and proliferation. However, PTK787/ ZK222584 treatment increased overall and local tumor hypoxia as revealed by extended expression of the hypoxia marker glucose transporter-1and increased uptake of [ 18 F]fluoromisonidazole. Fractionated irradiation induced a strong growth delay, which was associated with enhanced apoptosis and reduced proliferation of tumor cells but only minor effects on microvessel density and allograft oxygenation. Combined treatment with fractionated irradiation resulted in extended tumor growth delay and tumor cell apoptosis but no increase in tumor hypoxia. Conclusions:These results show that irradiation antagonizes the increase of hypoxia by vascular endothelial growth factor receptor tyrosine kinase inhibition and abrogates the potential negative effect on tumor hypoxia.Thus, the risk of treatment-induced hypoxia by inhibitors of angiogenesis exists but is kept minimal when combined with a cytotoxic treatment modality.Hypoxia reduces the radiosensitivity of tumor cells. Cells irradiated in normoxic conditions are twice to thrice more radiosensitive than cells irradiated under severe hypoxia. Thus, a putative reduction of oxygen delivery in result to inhibition of angiogenesis and destruction of the tumor vasculature could render the tumor more radioresistant and as such would be of major clinical concern (ref. 1 and references therein). Chronic and acute hypoxia result from diffusion-limited processes and intermittent blood flow due to an imbalance of rapid tumor growth, insufficient tumor angiogenesis, and supply of oxygen. This can not only directly reduce the efficacy of chemotherapy and radiotherapy but also cause the selection of more aggressive and even highly angiogenic tumor cell populations, which are also potentially resistant to inhibitors of angiogenesis (2).Various classes of angiogenesis inhibitors exist. They either directly target the microvascular endothelial cell and in particular its endothelial growth factors and corresponding receptors or indirectly block the tumor stress response to ...

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“…18 F-FMISO was prepared as described previously (26). The dPET acquisition was initiated concurrent to the intravenous bolus injection of 389 6 15 MBq of 18 F-FMISO.…”

Section: Pet/ct Imagingmentioning

confidence: 99%

Multiparametric Imaging of Tumor Hypoxia and Perfusion with¹⁸F-Fluoromisonidazole Dynamic PET in Head and Neck Cancer

et al. 2017

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Tumor hypoxia and perfusion are independent prognostic indicators of patient outcome. We developed the methodology for and investigated the utility of multiparametric imaging of tumor hypoxia and perfusion with 18 F-fluoromisonidazole ( 18 F-FMISO) dynamic PET (dPET) in head and neck cancer. Methods: One hundred twenty head and neck cancer patients underwent 0-to 30-min 18 F-FMISO dPET in a customized immobilization mask, followed by 10-min static acquisitions starting at 93 6 6 and 160 6 13 min after injection. A total of 248 lesions ($2 cm 3 ) were analyzed. Voxelwise pharmacokinetic modeling was conducted using an irreversible 1-plasma 2-tissuecompartment model to calculate surrogate biomarkers of tumor hypoxia (k 3 ), perfusion (K 1 ), and 18 F-FMISO distribution volume. The analysis was repeated with truncated dPET datasets. Results: Substantial inter-and intratumor heterogeneity was observed for all investigated metrics. Equilibration between the blood and unbound 18 F-FMISO was rapid in all tumors. 18 F-FMISO distribution volume deviated from the expected value of unity, causing discrepancy between k 3 maps and total 18 F-FMISO uptake and reducing the dynamic range of total 18 F-FMISO uptake for quantifying the degree of hypoxia. Both positive and negative trends between hypoxia and perfusion were observed in individual lesions. All investigated metrics were reproducible when calculated from a truncated 20-min dataset. Conclusion: 18 F-FMISO dPET provides the data necessary to generate parametric maps of tumor hypoxia, perfusion, and radiotracer distribution volume. These data clarify the ambiguity in interpreting 18 F-FMISO uptake and improve the characterization of lesions. We show total acquisition times can be reduced to 20 min, facilitating the translation of 18 F-FMISO dPET into the clinic.

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An efficient radiosynthesis of [18F]fluoromisonidazole

Cited by 103 publications

References 15 publications

Evaluation of hypoxia in an experimental rat tumour model by [18F]Fluoromisonidazole PET and immunohistochemistry

Evaluation of hypoxia in an experimental rat tumour model by [18F]Fluoromisonidazole PET and immunohistochemistry

Ionizing Radiation Antagonizes Tumor Hypoxia Induced by Antiangiogenic Treatment

Multiparametric Imaging of Tumor Hypoxia and Perfusion with¹⁸F-Fluoromisonidazole Dynamic PET in Head and Neck Cancer

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An efficient radiosynthesis of [18F]fluoromisonidazole

Cited by 103 publications

References 15 publications

Evaluation of hypoxia in an experimental rat tumour model by [18F]Fluoromisonidazole PET and immunohistochemistry

Evaluation of hypoxia in an experimental rat tumour model by [18F]Fluoromisonidazole PET and immunohistochemistry

Ionizing Radiation Antagonizes Tumor Hypoxia Induced by Antiangiogenic Treatment

Multiparametric Imaging of Tumor Hypoxia and Perfusion with18F-Fluoromisonidazole Dynamic PET in Head and Neck Cancer

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Multiparametric Imaging of Tumor Hypoxia and Perfusion with¹⁸F-Fluoromisonidazole Dynamic PET in Head and Neck Cancer