In Vivo Monitoring of the Antiangiogenic Effect of Neurotensin Receptor-Mediated Radiotherapy by Small-Animal Positron Emission Tomography: A Pilot Study
The neurotensin receptor (NTS1) has emerged as an interesting target for molecular imaging and radiotherapy of NTS-positive tumors due to the overexpression in a range of tumors. The aim of this study was to develop a 177Lu-labeled NTS1 radioligand, its application for radiotherapy in a preclinical...
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MDPI AG
2014-04-01
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| Series: | Pharmaceuticals |
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| Online Access: | http://www.mdpi.com/1424-8247/7/4/464 |
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| author | Simone Maschauer Tina Ruckdeschel Philipp Tripal Roland Haubner Jürgen Einsiedel Harald Hübner Peter Gmeiner Torsten Kuwert Olaf Prante |
| author_facet | Simone Maschauer Tina Ruckdeschel Philipp Tripal Roland Haubner Jürgen Einsiedel Harald Hübner Peter Gmeiner Torsten Kuwert Olaf Prante |
| author_sort | Simone Maschauer |
| collection | DOAJ |
| description | The neurotensin receptor (NTS1) has emerged as an interesting target for molecular imaging and radiotherapy of NTS-positive tumors due to the overexpression in a range of tumors. The aim of this study was to develop a 177Lu-labeled NTS1 radioligand, its application for radiotherapy in a preclinical model and the imaging of therapy success by small-animal positron emission tomography (µPET) using [68Ga]DOTA-RGD as a specific tracer for imaging angiogenesis. The 177Lu-labeled peptide was subjected to studies on HT29-tumor-bearing nude mice in vivo, defining four groups of animals (single dose, two fractionated doses, four fractionated doses and sham-treated animals). Body weight and tumor diameters were determined three times per week. Up to day 28 after treatment, µPET studies were performed with [68Ga]DOTA-RGD. At days 7–10 after treatment with four fractionated doses of 11–14 MBq (each at days 0, 3, 6 and 10), the tumor growth was slightly decreased in comparison with untreated animals. Using a single high dose of 51 MBq, a significantly decreased tumor diameter of about 50% was observed with the beginning of treatment. Our preliminary PET imaging data suggested decreased tumor uptake values of [68Ga]DOTA-RGD in treated animals compared to controls at day 7 after treatment. This pilot study suggests that early PET imaging with [68Ga]DOTA-RGD in radiotherapy studies to monitor integrin expression could be a promising tool to predict therapy success in vivo. Further successive PET experiments are needed to confirm the significance and predictive value of RGD-PET for NTS-mediated radiotherapy. |
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| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-12-17T10:01:48Z |
| publishDate | 2014-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-dd0a545755b14bdda5acc42681b1c9292022-12-21T21:53:17ZengMDPI AGPharmaceuticals1424-82472014-04-017446448110.3390/ph7040464ph7040464In Vivo Monitoring of the Antiangiogenic Effect of Neurotensin Receptor-Mediated Radiotherapy by Small-Animal Positron Emission Tomography: A Pilot StudySimone Maschauer0Tina Ruckdeschel1Philipp Tripal2Roland Haubner3Jürgen Einsiedel4Harald Hübner5Peter Gmeiner6Torsten Kuwert7Olaf Prante8Department of Nuclear Medicine, Laboratory of Molecular Imaging and Radiochemistry, Friedrich Alexander University, Schwabachanlage 6, 91054 Erlangen, GermanyDepartment of Nuclear Medicine, Laboratory of Molecular Imaging and Radiochemistry, Friedrich Alexander University, Schwabachanlage 6, 91054 Erlangen, GermanyDepartment of Nuclear Medicine, Laboratory of Molecular Imaging and Radiochemistry, Friedrich Alexander University, Schwabachanlage 6, 91054 Erlangen, GermanyDepartment of Nuclear Medicine, Innsbruck Medical University, Anichstr. 35, 6020 Innsbruck, AustriaDepartment of Chemistry and Pharmacy, Medicinal Chemistry, Emil Fischer Center, Friedrich Alexander University, Schuhstraße 19, 91052 Erlangen, GermanyDepartment of Chemistry and Pharmacy, Medicinal Chemistry, Emil Fischer Center, Friedrich Alexander University, Schuhstraße 19, 91052 Erlangen, GermanyDepartment of Chemistry and Pharmacy, Medicinal Chemistry, Emil Fischer Center, Friedrich Alexander University, Schuhstraße 19, 91052 Erlangen, GermanyDepartment of Nuclear Medicine, Laboratory of Molecular Imaging and Radiochemistry, Friedrich Alexander University, Schwabachanlage 6, 91054 Erlangen, GermanyDepartment of Nuclear Medicine, Laboratory of Molecular Imaging and Radiochemistry, Friedrich Alexander University, Schwabachanlage 6, 91054 Erlangen, GermanyThe neurotensin receptor (NTS1) has emerged as an interesting target for molecular imaging and radiotherapy of NTS-positive tumors due to the overexpression in a range of tumors. The aim of this study was to develop a 177Lu-labeled NTS1 radioligand, its application for radiotherapy in a preclinical model and the imaging of therapy success by small-animal positron emission tomography (µPET) using [68Ga]DOTA-RGD as a specific tracer for imaging angiogenesis. The 177Lu-labeled peptide was subjected to studies on HT29-tumor-bearing nude mice in vivo, defining four groups of animals (single dose, two fractionated doses, four fractionated doses and sham-treated animals). Body weight and tumor diameters were determined three times per week. Up to day 28 after treatment, µPET studies were performed with [68Ga]DOTA-RGD. At days 7–10 after treatment with four fractionated doses of 11–14 MBq (each at days 0, 3, 6 and 10), the tumor growth was slightly decreased in comparison with untreated animals. Using a single high dose of 51 MBq, a significantly decreased tumor diameter of about 50% was observed with the beginning of treatment. Our preliminary PET imaging data suggested decreased tumor uptake values of [68Ga]DOTA-RGD in treated animals compared to controls at day 7 after treatment. This pilot study suggests that early PET imaging with [68Ga]DOTA-RGD in radiotherapy studies to monitor integrin expression could be a promising tool to predict therapy success in vivo. Further successive PET experiments are needed to confirm the significance and predictive value of RGD-PET for NTS-mediated radiotherapy.http://www.mdpi.com/1424-8247/7/4/464neurotensin receptorpositron emission tomographyradiotherapylutetium-177RGD peptideangiogenesis |
| spellingShingle | Simone Maschauer Tina Ruckdeschel Philipp Tripal Roland Haubner Jürgen Einsiedel Harald Hübner Peter Gmeiner Torsten Kuwert Olaf Prante In Vivo Monitoring of the Antiangiogenic Effect of Neurotensin Receptor-Mediated Radiotherapy by Small-Animal Positron Emission Tomography: A Pilot Study Pharmaceuticals neurotensin receptor positron emission tomography radiotherapy lutetium-177 RGD peptide angiogenesis |
| title | In Vivo Monitoring of the Antiangiogenic Effect of Neurotensin Receptor-Mediated Radiotherapy by Small-Animal Positron Emission Tomography: A Pilot Study |
| title_full | In Vivo Monitoring of the Antiangiogenic Effect of Neurotensin Receptor-Mediated Radiotherapy by Small-Animal Positron Emission Tomography: A Pilot Study |
| title_fullStr | In Vivo Monitoring of the Antiangiogenic Effect of Neurotensin Receptor-Mediated Radiotherapy by Small-Animal Positron Emission Tomography: A Pilot Study |
| title_full_unstemmed | In Vivo Monitoring of the Antiangiogenic Effect of Neurotensin Receptor-Mediated Radiotherapy by Small-Animal Positron Emission Tomography: A Pilot Study |
| title_short | In Vivo Monitoring of the Antiangiogenic Effect of Neurotensin Receptor-Mediated Radiotherapy by Small-Animal Positron Emission Tomography: A Pilot Study |
| title_sort | in vivo monitoring of the antiangiogenic effect of neurotensin receptor mediated radiotherapy by small animal positron emission tomography a pilot study |
| topic | neurotensin receptor positron emission tomography radiotherapy lutetium-177 RGD peptide angiogenesis |
| url | http://www.mdpi.com/1424-8247/7/4/464 |
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