Update on Preclinical Development and Clinical Translation of Cholecystokinin-2 Receptor Targeting Radiopharmaceuticals

The cholecystokinin-2 receptor (CCK2R) has been a target of interest for molecular imaging and targeted radionuclide therapy for two decades. However, so far CCK2R targeted imaging and therapy has not been introduced in clinical practice. Within this review the recent radiopharmaceutical development...

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Autores principales: Elisabeth von Guggenberg, Petra Kolenc, Christof Rottenburger, Renata Mikołajczak, Alicja Hubalewska-Dydejczyk
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Publicado: MDPI AG 2021
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Acceso en línea:https://doaj.org/article/39929c74eb0f41469615cdf0f02b4031
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spelling oai:doaj.org-article:39929c74eb0f41469615cdf0f02b40312021-11-25T17:03:52ZUpdate on Preclinical Development and Clinical Translation of Cholecystokinin-2 Receptor Targeting Radiopharmaceuticals10.3390/cancers132257762072-6694https://doaj.org/article/39929c74eb0f41469615cdf0f02b40312021-11-01T00:00:00Zhttps://www.mdpi.com/2072-6694/13/22/5776https://doaj.org/toc/2072-6694The cholecystokinin-2 receptor (CCK2R) has been a target of interest for molecular imaging and targeted radionuclide therapy for two decades. However, so far CCK2R targeted imaging and therapy has not been introduced in clinical practice. Within this review the recent radiopharmaceutical development of CCK2R targeting compounds and the ongoing clinical trials are presented. Currently, new gastrin derivatives as well as nonpeptidic substances are being developed to improve the properties for clinical use. A team of specialists from the field of radiopharmacy and nuclear medicine reviewed the available literature and summarized their own experiences in the development and clinical testing of CCK2R targeting radiopharmaceuticals. The recent clinical trials with novel radiolabeled minigastrin analogs demonstrate the potential for both applications, imaging as well as targeted radiotherapy, and reinforce the clinical applicability within a theranostic concept. The intense efforts in optimizing CCK2R targeting radiopharmaceuticals has led to new substances for clinical use, as shown in first imaging studies in patients with advanced medullary thyroid cancer. The first clinical results suggest that the wider clinical implication of CCK2R-targeted radiopharmaceuticals is reasonable.Elisabeth von GuggenbergPetra KolencChristof RottenburgerRenata MikołajczakAlicja Hubalewska-DydejczykMDPI AGarticlecholecystokinin-2 receptoragonistantagonisttumor targetingmolecular imagingtargeted radiotherapyNeoplasms. Tumors. Oncology. Including cancer and carcinogensRC254-282ENCancers, Vol 13, Iss 5776, p 5776 (2021)
institution DOAJ
collection DOAJ
language EN
topic cholecystokinin-2 receptor
agonist
antagonist
tumor targeting
molecular imaging
targeted radiotherapy
Neoplasms. Tumors. Oncology. Including cancer and carcinogens
RC254-282
spellingShingle cholecystokinin-2 receptor
agonist
antagonist
tumor targeting
molecular imaging
targeted radiotherapy
Neoplasms. Tumors. Oncology. Including cancer and carcinogens
RC254-282
Elisabeth von Guggenberg
Petra Kolenc
Christof Rottenburger
Renata Mikołajczak
Alicja Hubalewska-Dydejczyk
Update on Preclinical Development and Clinical Translation of Cholecystokinin-2 Receptor Targeting Radiopharmaceuticals
description The cholecystokinin-2 receptor (CCK2R) has been a target of interest for molecular imaging and targeted radionuclide therapy for two decades. However, so far CCK2R targeted imaging and therapy has not been introduced in clinical practice. Within this review the recent radiopharmaceutical development of CCK2R targeting compounds and the ongoing clinical trials are presented. Currently, new gastrin derivatives as well as nonpeptidic substances are being developed to improve the properties for clinical use. A team of specialists from the field of radiopharmacy and nuclear medicine reviewed the available literature and summarized their own experiences in the development and clinical testing of CCK2R targeting radiopharmaceuticals. The recent clinical trials with novel radiolabeled minigastrin analogs demonstrate the potential for both applications, imaging as well as targeted radiotherapy, and reinforce the clinical applicability within a theranostic concept. The intense efforts in optimizing CCK2R targeting radiopharmaceuticals has led to new substances for clinical use, as shown in first imaging studies in patients with advanced medullary thyroid cancer. The first clinical results suggest that the wider clinical implication of CCK2R-targeted radiopharmaceuticals is reasonable.
format article
author Elisabeth von Guggenberg
Petra Kolenc
Christof Rottenburger
Renata Mikołajczak
Alicja Hubalewska-Dydejczyk
author_facet Elisabeth von Guggenberg
Petra Kolenc
Christof Rottenburger
Renata Mikołajczak
Alicja Hubalewska-Dydejczyk
author_sort Elisabeth von Guggenberg
title Update on Preclinical Development and Clinical Translation of Cholecystokinin-2 Receptor Targeting Radiopharmaceuticals
title_short Update on Preclinical Development and Clinical Translation of Cholecystokinin-2 Receptor Targeting Radiopharmaceuticals
title_full Update on Preclinical Development and Clinical Translation of Cholecystokinin-2 Receptor Targeting Radiopharmaceuticals
title_fullStr Update on Preclinical Development and Clinical Translation of Cholecystokinin-2 Receptor Targeting Radiopharmaceuticals
title_full_unstemmed Update on Preclinical Development and Clinical Translation of Cholecystokinin-2 Receptor Targeting Radiopharmaceuticals
title_sort update on preclinical development and clinical translation of cholecystokinin-2 receptor targeting radiopharmaceuticals
publisher MDPI AG
publishDate 2021
url https://doaj.org/article/39929c74eb0f41469615cdf0f02b4031
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