The Rise of PSMA Ligands for Diagnosis and Therapy of Prostate Cancer

The prostate-specific membrane antigen (PSMA) has received increased consideration during the past few years as an excellent target for both imaging and therapy of prostate cancer. After many years of outstanding preclinical research, the first significant step forward in clinical use was achieved i...

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Veröffentlicht in:Journal of Nuclear Medicine 2016-10, Vol.57 (Suppl 3), p.79S-89S
Hauptverfasser: Afshar-Oromieh, Ali, Babich, John W, Kratochwil, Clemens, Giesel, Frederik L, Eisenhut, Michael, Kopka, Klaus, Haberkorn, Uwe
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container_end_page 89S
container_issue Suppl 3
container_start_page 79S
container_title Journal of Nuclear Medicine
container_volume 57
creator Afshar-Oromieh, Ali
Babich, John W
Kratochwil, Clemens
Giesel, Frederik L
Eisenhut, Michael
Kopka, Klaus
Haberkorn, Uwe
description The prostate-specific membrane antigen (PSMA) has received increased consideration during the past few years as an excellent target for both imaging and therapy of prostate cancer. After many years of outstanding preclinical research, the first significant step forward in clinical use was achieved in 2008 with the first human experience with the small-molecule PSMA inhibitors I-MIP-1972 and I-MIP-1095. A clinical breakthrough followed in 2011 with Ga-PSMA-11 for PET imaging and I-MIP-1095 for endoradiotherapy of metastatic prostate cancer. Since then, PET/CT with Ga-PSMA-11 has rapidly spread worldwide, and endoradiotherapy with PSMA ligands has been conducted at increasing numbers of centers. Ga-PSMA-11 is currently the subject of multicenter studies in different countries. Since 2013, I-related PSMA therapy has been replaced by Lu-labeled ligands, such as PSMA-617, which is also the subject of multicenter studies. Alternative PSMA ligands for both imaging and therapy are available. Among them is Tc-MIP-1404, which has recently entered a phase 3 clinical trial. This article focuses on the highlights of the development and clinical application of PSMA ligands.
doi_str_mv 10.2967/jnumed.115.170720
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subjects Antigens, Surface - metabolism
Dipeptides - pharmacokinetics
Dipeptides - therapeutic use
Evidence-Based Medicine
Glutamate Carboxypeptidase II - antagonists & inhibitors
Glutamate Carboxypeptidase II - metabolism
Heterocyclic Compounds, 1-Ring - pharmacokinetics
Heterocyclic Compounds, 1-Ring - therapeutic use
Humans
Image Enhancement
Male
Molecular Diagnostic Techniques
Molecular Targeted Therapy
Organotechnetium Compounds - pharmacokinetics
Organotechnetium Compounds - therapeutic use
Positron-Emission Tomography
Prostatic Neoplasms - diagnostic imaging
Prostatic Neoplasms - metabolism
Prostatic Neoplasms - radiotherapy
Radiopharmaceuticals
title The Rise of PSMA Ligands for Diagnosis and Therapy of Prostate Cancer
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