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Lutetium-177-Labeled Prostate-Specific Membrane Antigen-617 for Molecular Imaging and Targeted Radioligand Therapy of Prostate Cancer

Prostate-specific membrane antigen (PSMA) represents a promising target for PSMA-overexpressing diseases, especially prostate cancer-a common type of cancer among men worldwide. In response to the challenges in tackling prostate cancers, several promising PSMA inhibitors from a variety of molecular...

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Detalles Bibliográficos
Autores principales: Ritawidya, Rien, Wongso, Hendris, Effendi, Nurmaya, Pujiyanto, Anung, Lestari, Wening, Setiawan, Herlan, Humani, Titis Sekar
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Tabriz University of Medical Sciences 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10676551/
https://www.ncbi.nlm.nih.gov/pubmed/38022814
http://dx.doi.org/10.34172/apb.2023.079
Descripción
Sumario:Prostate-specific membrane antigen (PSMA) represents a promising target for PSMA-overexpressing diseases, especially prostate cancer-a common type of cancer among men worldwide. In response to the challenges in tackling prostate cancers, several promising PSMA inhibitors from a variety of molecular scaffolds (e.g., phosphorous-, thiol-, and urea-based molecules) have been developed. In addition, PSMA inhibitors bearing macrocyclic chelators have attracted interest due to their favorable pharmacokinetic properties. Recently, conjugating a small PSMA molecule inhibitor-bearing 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) chelator, as exemplified by [(177)Lu]Lu-PSMA-617 could serve as a molecular imaging probe and targeted radioligand therapy (TRT) of metastatic castration resistant prostate cancer (mCRPC). Hence, studies related to mCRPC have drawn global attention. In this review, the recent development of PSMA ligand-617-labeled with (177)Lu for the management of mCRPC is presented. Its molecular mechanism of action, safety, efficacy, and future direction are also described.