Herlan Setiawan

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

Publisher: Maad Rayan Publishing Company

Date: 29-04-2023

DOI: 10.34172/APB.2023.079

Abstract: 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-N,N,N’’,N’’’-1,4,7,10-tetraacetic acid (DOTA) chelator, as exemplified by [177Lu]Lu-DOTA-PSMA-617 could serve as a molecular imaging probe and targeted radioligand therapy 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 177Lu for the management of mCRPC is presented. Its molecular mechanism of action, safety, efficacy, and future direction are also described.

Osaka Prefecture University

Location: Japan

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Badan Riset Dan Inovasi Nasional Republik Indonesia

Location: Indonesia

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Badan Tenaga Nuklir Nasional

Location: Indonesia

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