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...

Full description

Saved in:
Bibliographic Details
Published in:Advanced pharmaceutical bulletin 2023-11, Vol.13 (4), p.701-711
Main Authors: Ritawidya, Rien, Wongso, Hendris, Effendi, Nurmaya, Pujiyanto, Anung, Lestari, Wening, Setiawan, Herlan, Humani, Titis Sekar
Format: Article
Language:English
Subjects:
Antigens
Biopsy
Cancer therapies
Disease
Ligands
lutetium-177
Metastasis
metastatic-castration resistant prostate cancer
Monoclonal antibodies
Nuclear medicine
Prostate cancer
psma-617
Radiation therapy
radioligand
Tomography
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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 [177Lu]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 177Lu for the management of mCRPC is presented. Its molecular mechanism of action, safety, efficacy, and future direction are also described.
ISSN:2228-5881
2251-7308
DOI:10.34172/apb.2023.079