In Vivo Evaluation of a Bombesin Analogue Labeled with Ga-68 and Co-55/57

Purpose The purpose of this study was to apply an analogue of bombesin, NOTA-AMBA, labeled with Co-55 or Ga-68, for preclinical imaging of prostate cancer. Procedures The peptide NOTA-AMBA was labeled with Ga-68 or Co-55 by microwave irradiation. Biodistribution in xenograft mice (PC3) was performed...

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Veröffentlicht in:Molecular imaging and biology 2016-06, Vol.18 (3), p.368-376
Hauptverfasser: Dam, Johan Hygum, Olsen, Birgitte Brinkmann, Baun, Christina, Høilund-Carlsen, Poul-Flemming, Thisgaard, Helge
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container_end_page 376
container_issue 3
container_start_page 368
container_title Molecular imaging and biology
container_volume 18
creator Dam, Johan Hygum
Olsen, Birgitte Brinkmann
Baun, Christina
Høilund-Carlsen, Poul-Flemming
Thisgaard, Helge
description Purpose The purpose of this study was to apply an analogue of bombesin, NOTA-AMBA, labeled with Co-55 or Ga-68, for preclinical imaging of prostate cancer. Procedures The peptide NOTA-AMBA was labeled with Ga-68 or Co-55 by microwave irradiation. Biodistribution in xenograft mice (PC3) was performed at 1, 4, and 24 h (only cobalt at 24 h) using a fixed amount of peptide. Four weeks post-inoculation, xenograft mice were positron emission tomography/X-ray computed tomography scanned after tail vein injection of [ 68 Ga]NOTA-AMBA or [ 55 Co]NOTA-AMBA. Results Labeling with Ga-68 and Co-55/57 was achieved in yields greater than 90 %. A radiochemical purity (RCP) of 95 and 90 % were obtained for Ga-68 and Co-55, respectively. Both radiopeptides showed high uptake in the intestines, stomach, pancreas, and in the tumor ([ 68 Ga]NOTA-AMBA, 10.3 %ID/g at 1 h to 6.4 %ID/g at 4 h; [ 57 Co]NOTA-AMBA, 8.2 %ID/g at 1 h to 5.3%ID/g at 24 h). Normal tissue cleared over time improving tumor-to-background ratios. Conclusions NOTA-AMBA was labeled in high yields and RCP with Ga-68 and Co-55/57. High tumor uptake in a subcutaneous mouse prostate cancer model was observed. At 24 h, [ 55/57 Co]NOTA-AMBA showed better tumor-to-organ ratios than [ 68 Ga]NOTA-AMBA at both 1 and 4 h post-injection. Hence, for imaging, [ 55 Co]NOTA-AMBA was found to be superior compared to [ 68 Ga]NOTA-AMBA.
doi_str_mv 10.1007/s11307-015-0911-z
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Procedures The peptide NOTA-AMBA was labeled with Ga-68 or Co-55 by microwave irradiation. Biodistribution in xenograft mice (PC3) was performed at 1, 4, and 24 h (only cobalt at 24 h) using a fixed amount of peptide. Four weeks post-inoculation, xenograft mice were positron emission tomography/X-ray computed tomography scanned after tail vein injection of [ 68 Ga]NOTA-AMBA or [ 55 Co]NOTA-AMBA. Results Labeling with Ga-68 and Co-55/57 was achieved in yields greater than 90 %. A radiochemical purity (RCP) of 95 and 90 % were obtained for Ga-68 and Co-55, respectively. Both radiopeptides showed high uptake in the intestines, stomach, pancreas, and in the tumor ([ 68 Ga]NOTA-AMBA, 10.3 %ID/g at 1 h to 6.4 %ID/g at 4 h; [ 57 Co]NOTA-AMBA, 8.2 %ID/g at 1 h to 5.3%ID/g at 24 h). Normal tissue cleared over time improving tumor-to-background ratios. Conclusions NOTA-AMBA was labeled in high yields and RCP with Ga-68 and Co-55/57. High tumor uptake in a subcutaneous mouse prostate cancer model was observed. At 24 h, [ 55/57 Co]NOTA-AMBA showed better tumor-to-organ ratios than [ 68 Ga]NOTA-AMBA at both 1 and 4 h post-injection. Hence, for imaging, [ 55 Co]NOTA-AMBA was found to be superior compared to [ 68 Ga]NOTA-AMBA.</description><identifier>ISSN: 1536-1632</identifier><identifier>EISSN: 1860-2002</identifier><identifier>DOI: 10.1007/s11307-015-0911-z</identifier><identifier>PMID: 26561028</identifier><language>eng</language><publisher>New York: Springer US</publisher><subject>Animals ; Binding, Competitive ; Bombesin - analogs &amp; derivatives ; Cell Line, Tumor ; Chromatography, High Pressure Liquid ; Cobalt Radioisotopes - chemistry ; Gallium Radioisotopes - chemistry ; Humans ; Imaging ; Inhibitory Concentration 50 ; Male ; Medicine ; Medicine &amp; Public Health ; Mice, SCID ; Peptides - blood ; Peptides - chemistry ; Positron-Emission Tomography ; Protein Stability ; Radiology ; Radiopharmaceuticals - chemistry ; Research Article ; Tissue Distribution ; Tomography, X-Ray Computed ; Xenograft Model Antitumor Assays</subject><ispartof>Molecular imaging and biology, 2016-06, Vol.18 (3), p.368-376</ispartof><rights>World Molecular Imaging Society 2015</rights><rights>World Molecular Imaging Society 2016</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c405t-96d917771f0ccc041757ffc61449c66760d9ceeedef2547ad287e5001ab810dc3</citedby><cites>FETCH-LOGICAL-c405t-96d917771f0ccc041757ffc61449c66760d9ceeedef2547ad287e5001ab810dc3</cites><orcidid>0000-0001-6577-7011</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1007/s11307-015-0911-z$$EPDF$$P50$$Gspringer$$H</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1007/s11307-015-0911-z$$EHTML$$P50$$Gspringer$$H</linktohtml><link.rule.ids>314,780,784,27924,27925,41488,42557,51319</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/26561028$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Dam, Johan Hygum</creatorcontrib><creatorcontrib>Olsen, Birgitte Brinkmann</creatorcontrib><creatorcontrib>Baun, Christina</creatorcontrib><creatorcontrib>Høilund-Carlsen, Poul-Flemming</creatorcontrib><creatorcontrib>Thisgaard, Helge</creatorcontrib><title>In Vivo Evaluation of a Bombesin Analogue Labeled with Ga-68 and Co-55/57</title><title>Molecular imaging and biology</title><addtitle>Mol Imaging Biol</addtitle><addtitle>Mol Imaging Biol</addtitle><description>Purpose The purpose of this study was to apply an analogue of bombesin, NOTA-AMBA, labeled with Co-55 or Ga-68, for preclinical imaging of prostate cancer. Procedures The peptide NOTA-AMBA was labeled with Ga-68 or Co-55 by microwave irradiation. Biodistribution in xenograft mice (PC3) was performed at 1, 4, and 24 h (only cobalt at 24 h) using a fixed amount of peptide. Four weeks post-inoculation, xenograft mice were positron emission tomography/X-ray computed tomography scanned after tail vein injection of [ 68 Ga]NOTA-AMBA or [ 55 Co]NOTA-AMBA. Results Labeling with Ga-68 and Co-55/57 was achieved in yields greater than 90 %. A radiochemical purity (RCP) of 95 and 90 % were obtained for Ga-68 and Co-55, respectively. Both radiopeptides showed high uptake in the intestines, stomach, pancreas, and in the tumor ([ 68 Ga]NOTA-AMBA, 10.3 %ID/g at 1 h to 6.4 %ID/g at 4 h; [ 57 Co]NOTA-AMBA, 8.2 %ID/g at 1 h to 5.3%ID/g at 24 h). Normal tissue cleared over time improving tumor-to-background ratios. Conclusions NOTA-AMBA was labeled in high yields and RCP with Ga-68 and Co-55/57. High tumor uptake in a subcutaneous mouse prostate cancer model was observed. At 24 h, [ 55/57 Co]NOTA-AMBA showed better tumor-to-organ ratios than [ 68 Ga]NOTA-AMBA at both 1 and 4 h post-injection. 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Procedures The peptide NOTA-AMBA was labeled with Ga-68 or Co-55 by microwave irradiation. Biodistribution in xenograft mice (PC3) was performed at 1, 4, and 24 h (only cobalt at 24 h) using a fixed amount of peptide. Four weeks post-inoculation, xenograft mice were positron emission tomography/X-ray computed tomography scanned after tail vein injection of [ 68 Ga]NOTA-AMBA or [ 55 Co]NOTA-AMBA. Results Labeling with Ga-68 and Co-55/57 was achieved in yields greater than 90 %. A radiochemical purity (RCP) of 95 and 90 % were obtained for Ga-68 and Co-55, respectively. Both radiopeptides showed high uptake in the intestines, stomach, pancreas, and in the tumor ([ 68 Ga]NOTA-AMBA, 10.3 %ID/g at 1 h to 6.4 %ID/g at 4 h; [ 57 Co]NOTA-AMBA, 8.2 %ID/g at 1 h to 5.3%ID/g at 24 h). Normal tissue cleared over time improving tumor-to-background ratios. Conclusions NOTA-AMBA was labeled in high yields and RCP with Ga-68 and Co-55/57. High tumor uptake in a subcutaneous mouse prostate cancer model was observed. At 24 h, [ 55/57 Co]NOTA-AMBA showed better tumor-to-organ ratios than [ 68 Ga]NOTA-AMBA at both 1 and 4 h post-injection. Hence, for imaging, [ 55 Co]NOTA-AMBA was found to be superior compared to [ 68 Ga]NOTA-AMBA.</abstract><cop>New York</cop><pub>Springer US</pub><pmid>26561028</pmid><doi>10.1007/s11307-015-0911-z</doi><tpages>9</tpages><orcidid>https://orcid.org/0000-0001-6577-7011</orcidid></addata></record>
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subjects Animals
Binding, Competitive
Bombesin - analogs & derivatives
Cell Line, Tumor
Chromatography, High Pressure Liquid
Cobalt Radioisotopes - chemistry
Gallium Radioisotopes - chemistry
Humans
Imaging
Inhibitory Concentration 50
Male
Medicine
Medicine & Public Health
Mice, SCID
Peptides - blood
Peptides - chemistry
Positron-Emission Tomography
Protein Stability
Radiology
Radiopharmaceuticals - chemistry
Research Article
Tissue Distribution
Tomography, X-Ray Computed
Xenograft Model Antitumor Assays
title In Vivo Evaluation of a Bombesin Analogue Labeled with Ga-68 and Co-55/57
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