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PSMA-Targeting Imaging and Theranostic Agents—Current Status and Future Perspective

In the past two decades, extensive efforts have been made to develop agents targeting prostate-specific membrane antigen (PSMA) for prostate cancer imaging and therapy. To date, represented by two recent approvals of [(68)Ga]Ga-PSMA-11 and [(18)F]F-DCFPyL by the United States Food and Drug Administr...

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Autores principales: Debnath, Sashi, Zhou, Ning, McLaughlin, Mark, Rice, Samuel, Pillai, Anil K., Hao, Guiyang, Sun, Xiankai
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8835702/
https://www.ncbi.nlm.nih.gov/pubmed/35163083
http://dx.doi.org/10.3390/ijms23031158
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author Debnath, Sashi
Zhou, Ning
McLaughlin, Mark
Rice, Samuel
Pillai, Anil K.
Hao, Guiyang
Sun, Xiankai
author_facet Debnath, Sashi
Zhou, Ning
McLaughlin, Mark
Rice, Samuel
Pillai, Anil K.
Hao, Guiyang
Sun, Xiankai
author_sort Debnath, Sashi
collection PubMed
description In the past two decades, extensive efforts have been made to develop agents targeting prostate-specific membrane antigen (PSMA) for prostate cancer imaging and therapy. To date, represented by two recent approvals of [(68)Ga]Ga-PSMA-11 and [(18)F]F-DCFPyL by the United States Food and Drug Administration (US-FDA) for positron emission tomography (PET) imaging to identify suspected metastases or recurrence in patients with prostate cancer, PSMA-targeting imaging and theranostic agents derived from small molecule PSMA inhibitors have advanced to clinical practice and trials of prostate cancer. The focus of current development of new PSMA-targeting agents has thus shifted to the improvement of in vivo pharmacokinetics and higher specific binding affinity with the aims to further increase the detection sensitivity and specificity and minimize the toxicity to non-target tissues, particularly the kidneys. The main strategies involve systematic chemical modifications of the linkage between the targeting moiety and imaging/therapy payloads. In addition to a summary of the development history of PSMA-targeting agents, this review provides an overview of current advances and future promise of PSMA-targeted imaging and theranostics with focuses on the structural determinants of the chemical modification towards the next generation of PSMA-targeting agents.
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spelling pubmed-88357022022-02-12 PSMA-Targeting Imaging and Theranostic Agents—Current Status and Future Perspective Debnath, Sashi Zhou, Ning McLaughlin, Mark Rice, Samuel Pillai, Anil K. Hao, Guiyang Sun, Xiankai Int J Mol Sci Review In the past two decades, extensive efforts have been made to develop agents targeting prostate-specific membrane antigen (PSMA) for prostate cancer imaging and therapy. To date, represented by two recent approvals of [(68)Ga]Ga-PSMA-11 and [(18)F]F-DCFPyL by the United States Food and Drug Administration (US-FDA) for positron emission tomography (PET) imaging to identify suspected metastases or recurrence in patients with prostate cancer, PSMA-targeting imaging and theranostic agents derived from small molecule PSMA inhibitors have advanced to clinical practice and trials of prostate cancer. The focus of current development of new PSMA-targeting agents has thus shifted to the improvement of in vivo pharmacokinetics and higher specific binding affinity with the aims to further increase the detection sensitivity and specificity and minimize the toxicity to non-target tissues, particularly the kidneys. The main strategies involve systematic chemical modifications of the linkage between the targeting moiety and imaging/therapy payloads. In addition to a summary of the development history of PSMA-targeting agents, this review provides an overview of current advances and future promise of PSMA-targeted imaging and theranostics with focuses on the structural determinants of the chemical modification towards the next generation of PSMA-targeting agents. MDPI 2022-01-21 /pmc/articles/PMC8835702/ /pubmed/35163083 http://dx.doi.org/10.3390/ijms23031158 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Debnath, Sashi
Zhou, Ning
McLaughlin, Mark
Rice, Samuel
Pillai, Anil K.
Hao, Guiyang
Sun, Xiankai
PSMA-Targeting Imaging and Theranostic Agents—Current Status and Future Perspective
title PSMA-Targeting Imaging and Theranostic Agents—Current Status and Future Perspective
title_full PSMA-Targeting Imaging and Theranostic Agents—Current Status and Future Perspective
title_fullStr PSMA-Targeting Imaging and Theranostic Agents—Current Status and Future Perspective
title_full_unstemmed PSMA-Targeting Imaging and Theranostic Agents—Current Status and Future Perspective
title_short PSMA-Targeting Imaging and Theranostic Agents—Current Status and Future Perspective
title_sort psma-targeting imaging and theranostic agents—current status and future perspective
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8835702/
https://www.ncbi.nlm.nih.gov/pubmed/35163083
http://dx.doi.org/10.3390/ijms23031158
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