PSMA Theranostics: Review of the Current Status of PSMA-Targeted Imaging and Radioligand Therapy

Jones, Wallace; Griffiths, Kelly; Barata, Pedro C.; Fletcher, Sean A.

doi:10.3390/cancers12061367

Cited by 93 publications

(96 citation statements)

References 84 publications

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“…Similarly, improved detection and sensitivity could be achieved using bimodal agents [ 238 ]. Besides, the clinical success for radiolabeled somatostatin analogs both with diagnostic and therapeutic radionuclides paved the way for new promising peptide derivatives, such as bombesin, neurotensin, or CXCR4 ligands, and, in a similar way, PSMA ligands, for cancer theranostics [ 49 , 233 , 239 , 240 ].…”

Section: Future Prospectsmentioning

confidence: 99%

Overview of Radiolabeled Somatostatin Analogs for Cancer Imaging and Therapy

et al. 2020

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Identified in 1973, somatostatin (SST) is a cyclic hormone peptide with a short biological half-life. Somatostatin receptors (SSTRs) are widely expressed in the whole body, with five subtypes described. The interaction between SST and its receptors leads to the internalization of the ligand–receptor complex and triggers different cellular signaling pathways. Interestingly, the expression of SSTRs is significantly enhanced in many solid tumors, especially gastro-entero-pancreatic neuroendocrine tumors (GEP-NET). Thus, somatostatin analogs (SSAs) have been developed to improve the stability of the endogenous ligand and so extend its half-life. Radiolabeled analogs have been developed with several radioelements such as indium-111, technetium-99 m, and recently gallium-68, fluorine-18, and copper-64, to visualize the distribution of receptor overexpression in tumors. Internal metabolic radiotherapy is also used as a therapeutic strategy (e.g., using yttrium-90, lutetium-177, and actinium-225). With some radiopharmaceuticals now used in clinical practice, somatostatin analogs developed for imaging and therapy are an example of the concept of personalized medicine with a theranostic approach. Here, we review the development of these analogs, from the well-established and authorized ones to the most recently developed radiotracers, which have better pharmacokinetic properties and demonstrate increased efficacy and safety, as well as the search for new clinical indications.

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Section: Future Prospectsmentioning

confidence: 99%

Overview of Radiolabeled Somatostatin Analogs for Cancer Imaging and Therapy

et al. 2020

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“…There are multiple molecules being explored for PSMA radioligand therapy (RLT), including alpha- and beta-emitting radioisotopes, bispecific T cell engagers or docetaxel nanoparticles. 41 …”

Section: Emerging Therapiesmentioning

confidence: 99%

Volume matters and intensification is needed: emerging trends in the management of advanced prostate cancer

Sheng¹,

Barata²,

Alameddine³

et al. 2021

DIC

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Significant changes in the management of patients with de novo metastatic prostate cancer have led to the use of novel oral agents and docetaxel-based chemotherapy earlier in the natural history of their disease. Our main challenge is the lack of prospective randomized data comparing these regimens. It is clear that treatment intensification is needed. Yet, the heterogeneity of this patient population coupled with the lack of understanding of the specific biology for a given individual makes treatment selection challenging. The aim of this narrative review is to discuss the importance of defining advanced disease by volume, the necessity for treatment intensification, and the current and future landscape of metastatic hormone-sensitive prostate cancer management.

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“…PSMA has a large extracellular domain, which can be recognized by antibodies, their fragments, small molecules, nanobodies, and aptamers [28,29]. Additionally, PSMA internalizes the bound targeting molecules and any payload attached to them, making it an excellent molecular target for both diagnostic imaging and targeted therapy, applying a theragnostic approach [24,[30][31][32]. Many small molecules and antibodies targeting PSMA have been developed, labeled with βemitters ( 177 Lu, 161 Tb, 131 I, 90 Y, 67 Cu, 47 Sc), and studied in preclinical and clinical studies [33][34][35][36].…”

Section: Introductionmentioning

confidence: 99%

Preclinical and Clinical Status of PSMA-Targeted Alpha Therapy for Metastatic Castration-Resistant Prostate Cancer

Juzeniene

Stenberg

Bruland

et al. 2021

Cancers

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Bone, lymph node, and visceral metastases are frequent in castrate-resistant prostate cancer patients. Since such patients have only a few months’ survival benefit from standard therapies, there is an urgent need for new personalized therapies. The prostate-specific membrane antigen (PSMA) is overexpressed in prostate cancer and is a molecular target for imaging diagnostics and targeted radionuclide therapy (theragnostics). PSMA-targeted α therapies (PSMA-TAT) may deliver potent and local radiation more selectively to cancer cells than PSMA-targeted β- therapies. In this review, we summarize both the recent preclinical and clinical advances made in the development of PSMA-TAT, as well as the availability of therapeutic α-emitting radionuclides, the development of small molecules and antibodies targeting PSMA. Lastly, we discuss the potentials, limitations, and future perspectives of PSMA-TAT.

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PSMA Theranostics: Review of the Current Status of PSMA-Targeted Imaging and Radioligand Therapy

Cited by 93 publications

References 84 publications

Overview of Radiolabeled Somatostatin Analogs for Cancer Imaging and Therapy

Overview of Radiolabeled Somatostatin Analogs for Cancer Imaging and Therapy

Volume matters and intensification is needed: emerging trends in the management of advanced prostate cancer

Preclinical and Clinical Status of PSMA-Targeted Alpha Therapy for Metastatic Castration-Resistant Prostate Cancer

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