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29 results on '"Laverman, Peter"'

1. Imaging and photodynamic therapy of prostate cancer using a theranostic PSMA-targeting ligand

Author

Urologie Onderzoek, Derks, Yvonne H W, Schilham, Melline G M, Rijpkema, Mark, Smeets, Esther M M, Amatdjais-Groenen, Helene I V, Kip, Annemarie, van Lith, Sanne A M, van de Kamp, Jill, Sedelaar, J P Michiel, Somford, Diederik M, Simons, Michiel, Laverman, Peter, Gotthardt, Martin, Löwik, Dennis W P M, Heskamp, Sandra, Lütje, Susanne, Urologie Onderzoek, Derks, Yvonne H W, Schilham, Melline G M, Rijpkema, Mark, Smeets, Esther M M, Amatdjais-Groenen, Helene I V, Kip, Annemarie, van Lith, Sanne A M, van de Kamp, Jill, Sedelaar, J P Michiel, Somford, Diederik M, Simons, Michiel, Laverman, Peter, Gotthardt, Martin, Löwik, Dennis W P M, Heskamp, Sandra, and Lütje, Susanne

Published
2023

2. Highlight selection of radiochemistry and radiopharmacy developments by editorial board

Author

Bernardes, Emerson, Caravan, Peter, van Dam, Michael, Winnie, Deuther-Conrad, Ellis, Beverly, Shozo, Furumoto, Guillet, Benjamin, Ya-Yao, Huang, Jia, Hongmei, Laverman, Peter, Li, Zijing, Liu, Zhaofei, Lodi, Filippo, Miao, Yubin, Perk, Lars, Schirrmacher, Ralf, Vercoullie, Johnny, Yang, Hua, Yang, Min, Yang, Xing, Zhang, Junbo, Zhang, Ming-Rong, Zhu, Hua, Bernardes, Emerson, Caravan, Peter, van Dam, Michael, Winnie, Deuther-Conrad, Ellis, Beverly, Shozo, Furumoto, Guillet, Benjamin, Ya-Yao, Huang, Jia, Hongmei, Laverman, Peter, Li, Zijing, Liu, Zhaofei, Lodi, Filippo, Miao, Yubin, Perk, Lars, Schirrmacher, Ralf, Vercoullie, Johnny, Yang, Hua, Yang, Min, Yang, Xing, Zhang, Junbo, Zhang, Ming-Rong, and Zhu, Hua

Abstract

Background: The Editorial Board of EJNMMI Radiopharmacy and Chemistry releases a biyearly highlight commentary to update the readership on trends in the field of radiopharmaceutical development. Results: This commentary of highlights has resulted in 23 different topics selected by each member of the Editorial Board addressing a variety of aspects ranging from novel radiochemistry to first in man application of novel radiopharmaceuticals and also a contribution in relation to MRI-agents is included. Conclusion: Trends in (radio)chemistry and radiopharmacy are highlighted demonstrating the progress in the research field being the scope of EJNMMI Radiopharmacy and Chemistry.

Published
2022

3. Degradation and excretion of poly(2-oxazoline) based hemostatic materials

Author

Boerman, Marcel A., Roozen, Edwin A., Franssen, Gerben M., Bender, Johan C.M.E., Hoogenboom, Richard, Leeuwenburgh, Sander C.G., Laverman, Peter, van Hest, Jan C.M., van Goor, Harry, Félix Lanao, Rosa P., Boerman, Marcel A., Roozen, Edwin A., Franssen, Gerben M., Bender, Johan C.M.E., Hoogenboom, Richard, Leeuwenburgh, Sander C.G., Laverman, Peter, van Hest, Jan C.M., van Goor, Harry, and Félix Lanao, Rosa P.

Abstract

Poly(2-oxazoline) copolymers with hydroxyl groups and activated NHS ester moieties (NHS-POx) have recently been applied successfully in hemostatic devices [5]. An important requirement for clinical application of these polymers is to determine their clearance rate. In this study, we tested this for two NHS-POx variants with different polarities: NHS-POx 1 and 2. As degradation studies showed that the copolymers remained intact (except for the NHS ester), the carboxylic acid variants of these two polymers (P1 (NHS-POx 1) and P2 (NHS-POx 2)) were synthesized containing suitable chelators (DTPA and DOTA) for radiolabeling. To investigate the excretion pathway and potential accumulation of the polymers in specific organs, P1 and 2 were labeled with radioactive 111Indium (multiday imaging, t1/2 = 2.8 d) or 68Gallium (imaging within hours, t1/2 = 68 min) and intravenously injected in Wistar rats. The excretion of these radiolabeled polymers was studied by SPECT/CT, PET/CT and biodistribution using y-counting. The major part of the degradation products were renally excreted leaving only a small quantity of polymer present in kidneys after 7 days (%ID/g: 3.1 ± 1.1 (SPECT/CT) and 9.5 ± 0.6 (γ-counter) for P1 and%ID/g: 2.2 ± 0.5 (γ-counter) for P2. A prolonged study (14 days) on P2 demonstrated slow clearance from the kidneys. PET/CT measurements on 68Gallium labeled P2 revealed that the majority of the polymer was cleared within 10 min. No accumulation of the degradation products was observed in other organs than the kidneys. We demonstrated that the hemostatic NHS-POx polymers can indeed be effectively and timely cleared from the body. Statement of Significance: Synthetic polymers such as poly(2-oxazoline)s (POx) are of increasing interest in the biomedical field, e.g. because of their tunable structure. Recently, we have demonstrated in a pig model that side chain functionalized POx can be successfully used to stop

Published
2020

4. Imaging fibroblast activation protein to monitor therapeutic effects of neutralizing interleukin-22 in collagen-induced arthritis

Author

Afd Pharmaceutics, Pharmaceutics, van der Geest, Tessa, Roeleveld, Debbie M, Walgreen, Birgitte, Helsen, Monique M, Nayak, Tapan K, Klein, Christian, Hegen, Martin, Storm, Gert, Metselaar, Josbert M, van den Berg, Wim B, van der Kraan, Peter M, Laverman, Peter, Boerman, Otto C, Koenders, Marije I, Afd Pharmaceutics, Pharmaceutics, van der Geest, Tessa, Roeleveld, Debbie M, Walgreen, Birgitte, Helsen, Monique M, Nayak, Tapan K, Klein, Christian, Hegen, Martin, Storm, Gert, Metselaar, Josbert M, van den Berg, Wim B, van der Kraan, Peter M, Laverman, Peter, Boerman, Otto C, and Koenders, Marije I

Published
2018

5. Imaging fibroblast activation protein to monitor therapeutic effects of neutralizing interleukin-22 in collagen-induced arthritis

Author

Afd Pharmaceutics, Pharmaceutics, van der Geest, Tessa, Roeleveld, Debbie M, Walgreen, Birgitte, Helsen, Monique M, Nayak, Tapan K, Klein, Christian, Hegen, Martin, Storm, Gert, Metselaar, Josbert M, van den Berg, Wim B, van der Kraan, Peter M, Laverman, Peter, Boerman, Otto C, Koenders, Marije I, Afd Pharmaceutics, Pharmaceutics, van der Geest, Tessa, Roeleveld, Debbie M, Walgreen, Birgitte, Helsen, Monique M, Nayak, Tapan K, Klein, Christian, Hegen, Martin, Storm, Gert, Metselaar, Josbert M, van den Berg, Wim B, van der Kraan, Peter M, Laverman, Peter, Boerman, Otto C, and Koenders, Marije I

Published
2018

6. Imaging fibroblast activation protein to monitor therapeutic effects of neutralizing interleukin-22 in collagen-induced arthritis

Author

Afd Pharmaceutics, Pharmaceutics, van der Geest, Tessa, Roeleveld, Debbie M, Walgreen, Birgitte, Helsen, Monique M, Nayak, Tapan K, Klein, Christian, Hegen, Martin, Storm, Gert, Metselaar, Josbert M, van den Berg, Wim B, van der Kraan, Peter M, Laverman, Peter, Boerman, Otto C, Koenders, Marije I, Afd Pharmaceutics, Pharmaceutics, van der Geest, Tessa, Roeleveld, Debbie M, Walgreen, Birgitte, Helsen, Monique M, Nayak, Tapan K, Klein, Christian, Hegen, Martin, Storm, Gert, Metselaar, Josbert M, van den Berg, Wim B, van der Kraan, Peter M, Laverman, Peter, Boerman, Otto C, and Koenders, Marije I

Published
2018

7. Liposomal treatment of experimental arthritis can be monitored noninvasively with a radiolabeled anti-fibroblast activation protein antibody

Author

Pharmaceutics, Afd Pharmaceutics, Van Der Geest, Tessa, Laverman, Peter, Gerrits, Danny, Walgreen, Birgitte, Helsen, Monique, Klein, Christian, Nayak, Tapan K., Storm, G, Metselaar, Josbert M., Koenders, Marije I., Boerman, Otto C., Pharmaceutics, Afd Pharmaceutics, Van Der Geest, Tessa, Laverman, Peter, Gerrits, Danny, Walgreen, Birgitte, Helsen, Monique, Klein, Christian, Nayak, Tapan K., Storm, G, Metselaar, Josbert M., Koenders, Marije I., and Boerman, Otto C.

Published
2017

8. Liposomal treatment of experimental arthritis can be monitored noninvasively with a radiolabeled anti-fibroblast activation protein antibody

Author

Pharmaceutics, Afd Pharmaceutics, Van Der Geest, Tessa, Laverman, Peter, Gerrits, Danny, Walgreen, Birgitte, Helsen, Monique, Klein, Christian, Nayak, Tapan K., Storm, G, Metselaar, Josbert M., Koenders, Marije I., Boerman, Otto C., Pharmaceutics, Afd Pharmaceutics, Van Der Geest, Tessa, Laverman, Peter, Gerrits, Danny, Walgreen, Birgitte, Helsen, Monique, Klein, Christian, Nayak, Tapan K., Storm, G, Metselaar, Josbert M., Koenders, Marije I., and Boerman, Otto C.

Published
2017

9. Liposomal treatment of experimental arthritis can be monitored noninvasively with a radiolabeled anti-fibroblast activation protein antibody

Author

Pharmaceutics, Afd Pharmaceutics, Van Der Geest, Tessa, Laverman, Peter, Gerrits, Danny, Walgreen, Birgitte, Helsen, Monique, Klein, Christian, Nayak, Tapan K., Storm, G, Metselaar, Josbert M., Koenders, Marije I., Boerman, Otto C., Pharmaceutics, Afd Pharmaceutics, Van Der Geest, Tessa, Laverman, Peter, Gerrits, Danny, Walgreen, Birgitte, Helsen, Monique, Klein, Christian, Nayak, Tapan K., Storm, G, Metselaar, Josbert M., Koenders, Marije I., and Boerman, Otto C.

Published
2017

10. Radionuclide imaging of liposomal drug delivery

Author

Sub General Pharmaceutics, Sub Drug targeting, Pharmaceutics, van der Geest, Tessa, Laverman, Peter, Metselaar, Josbert M., Storm, G, Boerman, Otto C., Sub General Pharmaceutics, Sub Drug targeting, Pharmaceutics, van der Geest, Tessa, Laverman, Peter, Metselaar, Josbert M., Storm, G, and Boerman, Otto C.

Published
2016

11. Radionuclide imaging of liposomal drug delivery

Author

Sub General Pharmaceutics, Sub Drug targeting, Pharmaceutics, van der Geest, Tessa, Laverman, Peter, Metselaar, Josbert M., Storm, G, Boerman, Otto C., Sub General Pharmaceutics, Sub Drug targeting, Pharmaceutics, van der Geest, Tessa, Laverman, Peter, Metselaar, Josbert M., Storm, G, and Boerman, Otto C.

Published
2016

12. Radionuclide imaging of liposomal drug delivery

Author

Sub General Pharmaceutics, Sub Drug targeting, Pharmaceutics, van der Geest, Tessa, Laverman, Peter, Metselaar, Josbert M., Storm, G, Boerman, Otto C., Sub General Pharmaceutics, Sub Drug targeting, Pharmaceutics, van der Geest, Tessa, Laverman, Peter, Metselaar, Josbert M., Storm, G, and Boerman, Otto C.

Published
2016

13. Superoxide dismutase enzymosomes: carrier capacity optimization, in vivo behaviour and therapeutic activity

Author

Sub Drug targeting, Pharmaceutics, Corvo, M Luísa, Marinho, H Susana, Marcelino, Paulo, Lopes, Rui M, Vale, Carlos A, Marques, Claúdia R, Martins, Luísa C D, Laverman, Peter, Storm, G, Martins, M Bárbara A F, Sub Drug targeting, Pharmaceutics, Corvo, M Luísa, Marinho, H Susana, Marcelino, Paulo, Lopes, Rui M, Vale, Carlos A, Marques, Claúdia R, Martins, Luísa C D, Laverman, Peter, Storm, G, and Martins, M Bárbara A F

Published
2015

14. Biodistribution and translational pharmacokinetic modeling of a human recombinant alkaline phosphatase

Author

Pharmacology, Sub Experimental pharmacology, Peters, Esther, Stevens, Jasper, Arend, Jacques, Guan, Zheng, Raaben, Willem, Laverman, Peter, Elsas, Andrea van, Masereeuw, R., Pickkers, Peter, Pharmacology, Sub Experimental pharmacology, Peters, Esther, Stevens, Jasper, Arend, Jacques, Guan, Zheng, Raaben, Willem, Laverman, Peter, Elsas, Andrea van, Masereeuw, R., and Pickkers, Peter

Published
2015

15. Comparison of three remote radiolabelling methods for long-circulating liposomes

Author

Pharmaceutics, Sub General Pharmaceutics, Sub Drug targeting, Van Der Geest, Tessa, Laverman, Peter, Gerrits, Danny, Franssen, Gerben M., Metselaar, Josbert M., Storm, G, Boerman, Otto C., Pharmaceutics, Sub General Pharmaceutics, Sub Drug targeting, Van Der Geest, Tessa, Laverman, Peter, Gerrits, Danny, Franssen, Gerben M., Metselaar, Josbert M., Storm, G, and Boerman, Otto C.

Published
2015

16. [18]F FDG PET/CT imaging to monitor the therapeutic effect of liposome-encapsulated prednisolone in experimental rheumatoid arthritis

Author

Pharmaceutics, Sub General Pharmaceutics, Sub Drug targeting, Van Der Geest, Tessa, Metselaar, Josbert M., Gerrits, Danny, Van Lent, Peter L., Storm, G, Laverman, Peter, Boerman, Otto C., Pharmaceutics, Sub General Pharmaceutics, Sub Drug targeting, Van Der Geest, Tessa, Metselaar, Josbert M., Gerrits, Danny, Van Lent, Peter L., Storm, G, Laverman, Peter, and Boerman, Otto C.

Published
2015

17. Distribution of technetium-99m PEG-liposomes during oligofructose-induced laminitis development in horses

Author

Pharmaceutics, Sub General Pharmaceutics, Sub Drug targeting, Underwood, Claire, Pollitt, Christopher C., Metselaar, Josbert M., Laverman, Peter, van Bloois, Louis, van den Hoven, Jolanda M., Storm, G, van Eps, Andrew W., Pharmaceutics, Sub General Pharmaceutics, Sub Drug targeting, Underwood, Claire, Pollitt, Christopher C., Metselaar, Josbert M., Laverman, Peter, van Bloois, Louis, van den Hoven, Jolanda M., Storm, G, and van Eps, Andrew W.

Published
2015

18. Comparison of three remote radiolabelling methods for long-circulating liposomes

Author

Pharmaceutics, Sub General Pharmaceutics, Sub Drug targeting, Van Der Geest, Tessa, Laverman, Peter, Gerrits, Danny, Franssen, Gerben M., Metselaar, Josbert M., Storm, G, Boerman, Otto C., Pharmaceutics, Sub General Pharmaceutics, Sub Drug targeting, Van Der Geest, Tessa, Laverman, Peter, Gerrits, Danny, Franssen, Gerben M., Metselaar, Josbert M., Storm, G, and Boerman, Otto C.

Published
2015

19. [18]F FDG PET/CT imaging to monitor the therapeutic effect of liposome-encapsulated prednisolone in experimental rheumatoid arthritis

Author

Pharmaceutics, Sub General Pharmaceutics, Sub Drug targeting, Van Der Geest, Tessa, Metselaar, Josbert M., Gerrits, Danny, Van Lent, Peter L., Storm, G, Laverman, Peter, Boerman, Otto C., Pharmaceutics, Sub General Pharmaceutics, Sub Drug targeting, Van Der Geest, Tessa, Metselaar, Josbert M., Gerrits, Danny, Van Lent, Peter L., Storm, G, Laverman, Peter, and Boerman, Otto C.

Published
2015

20. Distribution of technetium-99m PEG-liposomes during oligofructose-induced laminitis development in horses

Author

Pharmaceutics, Sub General Pharmaceutics, Sub Drug targeting, Underwood, Claire, Pollitt, Christopher C., Metselaar, Josbert M., Laverman, Peter, van Bloois, Louis, van den Hoven, Jolanda M., Storm, G, van Eps, Andrew W., Pharmaceutics, Sub General Pharmaceutics, Sub Drug targeting, Underwood, Claire, Pollitt, Christopher C., Metselaar, Josbert M., Laverman, Peter, van Bloois, Louis, van den Hoven, Jolanda M., Storm, G, and van Eps, Andrew W.

Published
2015

21. Superoxide dismutase enzymosomes: carrier capacity optimization, in vivo behaviour and therapeutic activity

Author

Sub Drug targeting, Pharmaceutics, Corvo, M Luísa, Marinho, H Susana, Marcelino, Paulo, Lopes, Rui M, Vale, Carlos A, Marques, Claúdia R, Martins, Luísa C D, Laverman, Peter, Storm, G, Martins, M Bárbara A F, Sub Drug targeting, Pharmaceutics, Corvo, M Luísa, Marinho, H Susana, Marcelino, Paulo, Lopes, Rui M, Vale, Carlos A, Marques, Claúdia R, Martins, Luísa C D, Laverman, Peter, Storm, G, and Martins, M Bárbara A F

Published
2015

22. Biodistribution and translational pharmacokinetic modeling of a human recombinant alkaline phosphatase

Author

Pharmacology, Sub Experimental pharmacology, Peters, Esther, Stevens, Jasper, Arend, Jacques, Guan, Zheng, Raaben, Willem, Laverman, Peter, Elsas, Andrea van, Masereeuw, R., Pickkers, Peter, Pharmacology, Sub Experimental pharmacology, Peters, Esther, Stevens, Jasper, Arend, Jacques, Guan, Zheng, Raaben, Willem, Laverman, Peter, Elsas, Andrea van, Masereeuw, R., and Pickkers, Peter

Published
2015

23. Biodistribution and translational pharmacokinetic modeling of a human recombinant alkaline phosphatase

Author

Pharmacology, Sub Experimental pharmacology, Peters, Esther, Stevens, Jasper, Arend, Jacques, Guan, Zheng, Raaben, Willem, Laverman, Peter, Elsas, Andrea van, Masereeuw, R., Pickkers, Peter, Pharmacology, Sub Experimental pharmacology, Peters, Esther, Stevens, Jasper, Arend, Jacques, Guan, Zheng, Raaben, Willem, Laverman, Peter, Elsas, Andrea van, Masereeuw, R., and Pickkers, Peter

Published
2015

24. [18]F FDG PET/CT imaging to monitor the therapeutic effect of liposome-encapsulated prednisolone in experimental rheumatoid arthritis

Author

Pharmaceutics, Sub General Pharmaceutics, Sub Drug targeting, Van Der Geest, Tessa, Metselaar, Josbert M., Gerrits, Danny, Van Lent, Peter L., Storm, G, Laverman, Peter, Boerman, Otto C., Pharmaceutics, Sub General Pharmaceutics, Sub Drug targeting, Van Der Geest, Tessa, Metselaar, Josbert M., Gerrits, Danny, Van Lent, Peter L., Storm, G, Laverman, Peter, and Boerman, Otto C.

Published
2015

25. Distribution of technetium-99m PEG-liposomes during oligofructose-induced laminitis development in horses

Author

Pharmaceutics, Sub General Pharmaceutics, Sub Drug targeting, Underwood, Claire, Pollitt, Christopher C., Metselaar, Josbert M., Laverman, Peter, van Bloois, Louis, van den Hoven, Jolanda M., Storm, G, van Eps, Andrew W., Pharmaceutics, Sub General Pharmaceutics, Sub Drug targeting, Underwood, Claire, Pollitt, Christopher C., Metselaar, Josbert M., Laverman, Peter, van Bloois, Louis, van den Hoven, Jolanda M., Storm, G, and van Eps, Andrew W.

Published
2015

26. Comparison of three remote radiolabelling methods for long-circulating liposomes

Author

Pharmaceutics, Sub General Pharmaceutics, Sub Drug targeting, Van Der Geest, Tessa, Laverman, Peter, Gerrits, Danny, Franssen, Gerben M., Metselaar, Josbert M., Storm, G, Boerman, Otto C., Pharmaceutics, Sub General Pharmaceutics, Sub Drug targeting, Van Der Geest, Tessa, Laverman, Peter, Gerrits, Danny, Franssen, Gerben M., Metselaar, Josbert M., Storm, G, and Boerman, Otto C.

Published
2015

27. Superoxide dismutase enzymosomes: carrier capacity optimization, in vivo behaviour and therapeutic activity

Author

Sub Drug targeting, Pharmaceutics, Corvo, M Luísa, Marinho, H Susana, Marcelino, Paulo, Lopes, Rui M, Vale, Carlos A, Marques, Claúdia R, Martins, Luísa C D, Laverman, Peter, Storm, G, Martins, M Bárbara A F, Sub Drug targeting, Pharmaceutics, Corvo, M Luísa, Marinho, H Susana, Marcelino, Paulo, Lopes, Rui M, Vale, Carlos A, Marques, Claúdia R, Martins, Luísa C D, Laverman, Peter, Storm, G, and Martins, M Bárbara A F

Published
2015

28. Imaging of Human Epidermal Growth Factor Receptor Type 2 Expression with 18F-Labeled Affibody Molecule ZHER2:2395 in a Mouse Model for Ovarian Cancer

Author

Heskamp, Sandra, Laverman, Peter, Rosik, Daniel, Boschetti, Frederic, van der Graaf, Winette T A, Oyen, Wim J G, van Laarhoven, Hanneke W M, Tolmachev, Vladimir, Boerman, Otto C, Heskamp, Sandra, Laverman, Peter, Rosik, Daniel, Boschetti, Frederic, van der Graaf, Winette T A, Oyen, Wim J G, van Laarhoven, Hanneke W M, Tolmachev, Vladimir, and Boerman, Otto C

Abstract

Affibody molecules are small (7 kDa) proteins with subnanomolar targeting affinity. Previous SPECT studies in xenografts have shown that the Affibody molecule 111In-DOTA-ZHER2:2395 can discriminate between high and low human epidermal growth factor receptor type 2 (HER2)–expressing tumors, indicating that radiolabeled Affibody molecules have potential for patient selection for HER2-targeted therapy. Compared with SPECT, PET with positron-emitting radionuclides, such as 18F, may improve imaging of HER2 expression because of higher sensitivity and improved quantification of PET. The aim of the present study was to determine whether the 18F-labeled NOTA-conjugated Affibody molecule ZHER2:2395 is a suitable agent for imaging of HER2 expression. The tumor-targeting properties of 18F-labeled ZHER2:2395 were compared with 111In- and 68Ga-labeled ZHER2:2395 in mice with HER2-expressing SK-OV-3 xenografts. Methods: ZHER2:2395 was conjugated with NOTA and radiolabeled with 18F, 68Ga, and 111In. Radiolabeling with 18F was based on the complexation of Al18F by NOTA. The 50% inhibitory concentration values for NOTA-ZHER2:2395 labeled with 19F, 69Ga, and 115In were determined in a competitive cell-binding assay using SK-OV-3 cells. Mice bearing subcutaneous SK-OV-3 xenografts were injected intravenously with radiolabeled NOTA-ZHER2:2395. One and 4 h after injection, PET/CT or SPECT/CT images were acquired, and the biodistribution was determined by ex vivo measurement. Results: The 50% inhibitory concentration values for 19F-, 69Ga-, and 115In-NOTA-ZHER2:2395 were 5.0, 6.3, and 5.3 nM, respectively. One hour after injection, tumor uptake was 4.4 ± 0.8 percentage injected dose per gram (%ID/g), 5.6 ± 1.6 %ID/g, and 7.1 ± 1.4 %ID/g for 18F-, 68Ga-, and 111In-NOTA-ZHER2:2395, respectively, and the respective tumor-to-blood ratios were 7.4 ± 1.8, 8.0 ± 1.3, and 4.8 ± 1.3. Tumor uptake was specific, because uptake could be blocked efficiently by coinjection of an excess of unlabeled ZH

Published
2012
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29. Imaging of Human Epidermal Growth Factor Receptor Type 2 Expression with (18)F-Labeled Affibody Molecule Z(HER2:2395) in a Mouse Model for Ovarian Cancer

Author

Heskamp, Sandra, Laverman, Peter, Rosik, Daniel, Boschetti, Frederic, van der Graaf, Winette T. A., Oyen, Wim J. G., van Laarhoven, Hanneke W. M., Tolmachev, Vladimir, Boerman, Otto C., Heskamp, Sandra, Laverman, Peter, Rosik, Daniel, Boschetti, Frederic, van der Graaf, Winette T. A., Oyen, Wim J. G., van Laarhoven, Hanneke W. M., Tolmachev, Vladimir, and Boerman, Otto C.

Abstract

Affibody molecules are small (7 kDa) proteins with subnanomolar targeting affinity. Previous SPECT studies in xenografts have shown that the Affibody molecule (111)In-DOTA-Z(HER2:2395) can discriminate between high and low human epidermal growth factor receptor type 2 (HER2)-expressing tumors, indicating that radiolabeled Affibody molecules have potential for patient selection for HER2-targeted therapy. Compared with SPECT, PET with positron-emitting radionuclides, such as (18)F, may improve imaging of HER2 expression because of higher sensitivity and improved quantification of PET. The aim of the present study was to determine whether the (18)F-labeled NOTA-conjugated Affibody molecule Z(HER2:2395) is a suitable agent for imaging of HER2 expression. The tumor-targeting properties of (18)F-labeled Z(HER2:2395) were compared with (111)In- and (68)Ga-labeled Z(HER2:2395) in mice with HER2-expressing SK-OV-3 xenografts. Methods: Z(HER2:2395) was conjugated with NOTA and radiolabeled with (18)F, (68)Ga, and (111)In. Radiolabeling with (18)F was based on the complexation of Al(18)F by NOTA. The 50% inhibitory concentration values for NOTA-Z(HER2:2395) labeled with (19)F, (69)Ga, and (115)In were determined in a competitive cell-binding assay using SK-OV-3 cells. Mice bearing subcutaneous SK-OV-3 xenografts were injected intravenously with radiolabeled NOTA-Z(HER2:2395). One and 4 h after injection, PET/CT or SPECT/CT images were acquired, and the biodistribution was determined by ex vivo measurement. Results: The 50% inhibitory concentration values for (19)F-, (69)Ga-, and (115)In-NOTA-Z(HER2:2395) were 5.0, 6.3, and 5.3 nM, respectively. One hour after injection, tumor uptake was 4.4 +/- 0.8 percentage injected dose per gram (% ID/g), 5.6 +/- 1.6 % ID/g, and 7.1 +/- 1.4 % ID/g for (18)F-, (68)Ga-, and (111)In-NOTA-Z(HER2:2395), respectively, and the respective tumor-to-blood ratios were 7.4 +/- 1.8, 8.0 +/- 1.3, and 4.8 +/- 1.3. Tumor uptake was specific, because uptake, QC 20120206

Published
2012
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