Review of commonly used prostate specific PET tracers used in prostate cancer imaging in current clinical practice

Niaz, Muhammad Junaid; Sun, Michael; Skafida, Myrto; Niaz, Muhammad Obaid; Ivanidze, Jana; Osborne, Joseph R.; O’Dwyer, Elisabeth

doi:10.1016/j.clinimag.2021.06.006

Cited by 14 publications

(9 citation statements)

References 76 publications

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“…Computed tomography (CT) and bone scans have been the main imaging modalities used for the detection of metastases. Positron emission tomography (PET) imaging tracers, such as 11 C-Choline and 18 F-Fluciclovine, outperform FDG PET in the detection of nodal and osseous disease [ 2 ]. More recently, however, prostate-specific membrane antigen (PSMA)-based tracers have been found to be more accurate for the detection of prostate cancer [ 3 , 4 , 5 , 6 , 7 , 8 ].…”

Section: Introductionmentioning

confidence: 99%

Management of Patients with Recurrent and Metachronous Oligometastatic Prostate Cancer in the Era of PSMA PET

Sabbagh

Mohamad

Lichter

et al. 2022

Cancers

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Prostate-specific membrane antigen (PSMA) positron emission tomography (PET) scans have higher sensitivity and specificity for detecting lymph nodes or metastatic disease relative to conventional imaging in prostate cancer staging. Since its FDA approval and incorporation into treatment guidelines, the use of PSMA PET has increased in patients undergoing initial staging, those with recurrence after initial definitive treatment, and patients with metastatic disease. Although the early detection of metastatic lesions is changing disease management, it is unclear whether this impact on management translates into clinical benefit. This review will summarize evidence pertaining to the change in patient management due to PSMA PET use and will discuss the implications of PSMA PET on treatment decisions in prostate cancer, particularly in the settings of biochemical recurrence and metachronous oligometastatic disease.

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Section: Introductionmentioning

confidence: 99%

Management of Patients with Recurrent and Metachronous Oligometastatic Prostate Cancer in the Era of PSMA PET

Sabbagh

Mohamad

Lichter

et al. 2022

Cancers

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“…Without AR expression, the cells of tCRPC present low-to-zero prostate-specific membrane antigen (PSMA) [ 3 , 4 , 5 ]. Consequently, patients with NEPC cannot benefit from PSMA-targeted diagnosis and treatment options [ 6 , 7 , 8 ]. While the progression of NEPC is more aggressive, the lack of an understanding of its underlying biological mechanisms represents a challenge for the design of new therapies and diagnostic tools for the disease [ 9 , 10 ].…”

Section: Introductionmentioning

confidence: 99%

A Theranostic Small-Molecule Prodrug Conjugate for Neuroendocrine Prostate Cancer

et al. 2023

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After androgen deprivation therapy, a significant number of prostate cancer cases progress with a therapy-resistant neuroendocrine phenotype (NEPC). This represents a challenge for diagnosis and treatment. Based on our previously reported design of theranostic small-molecule prodrug conjugates (T-SMPDCs), herein we report a T-SMPDC tailored for targeted positron emission tomography (PET) imaging and chemotherapy of NEPC. The T-SMPDC is built upon a triazine core (TZ) to present three functionalities: (1) a chelating moiety (DOTA: 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) for PET imaging when labeled with 68Ga (t1/2 = 68 min) or other relevant radiometals; (2) an octreotide (Octr) that targets the somatostatin receptor 2 (SSTR2), which is overexpressed in the innervated tumor microenvironment (TME); and (3) fingolimod, FTY720—an antagonist of sphingosine kinase 1 that is an intracellular enzyme upregulated in NEPC. Polyethylene glycol (PEG) chains were incorporated via conventional conjugation methods or a click chemistry reaction forming a 1,4-disubstituted 1,2,3-triazole (Trz) linkage for the optimization of in vivo kinetics as necessary. The T-SMPDC, DOTA-PEG3-TZ(PEG4-Octr)-PEG2-Trz-PEG3-Val-Cit-pABOC-FTY720 (PEGn: PEG with n repeating ethyleneoxy units (n = 2, 3, or 4); Val: valine; Cit: citrulline; pABOC: p-amino-benzyloxycarbonyl), showed selective SSTR2 binding and mediated internalization of the molecule in SSTR2 high cells. Release of FTY720 was observed when the T-SMPDC was exposed to cathepsin B, and the released FTY720 exerted cytotoxicity in cells. In vivo PET imaging showed significantly higher accumulation (2.1 ± 0.3 %ID/g; p = 0.02) of [68Ga]Ga-DOTA-PEG3-TZ(PEG4-Octr)-PEG2-Trz-PEG3-Val-Cit-pABOC-FTY720 in SSTR2high prostate cancer xenografts than in the SSTR2low xenografts (1.5 ± 0.4 %ID/g) at 13 min post-injection (p.i.) with a rapid excretion through the kidneys. Taken together, these proof-of-concept results validate the design concept of the T-SMPDC, which may hold a great potential for targeted diagnosis and therapy of NEPC.

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“…Positron emission tomography (PET) has become a cornerstone of nuclear medicine for the detection of biological processes in a range of diseases from brain pathologies to cancer. − In nuclear medicine, the use of coordination complexes of radiometal ions plays a crucial role in the development of novel radiopharmaceuticals for diagnostic or therapeutic applications. Indeed, depending on the emissive properties of the radionuclides, these radiolabeled complexes find application as PET (β + emitters) or single-photon emission computed tomography (SPECT; γ-emitters) imaging agents as well as radiotherapeutics (β – , α emitters) …”

Section: Introductionmentioning

confidence: 99%

HNODThia: A Promising Chelator for the Development of ⁶⁴Cu Radiopharmaceuticals

et al. 2023

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Herein, we present the synthesis and coordination chemistry of copper(II) and zinc(II) complexes of two novel heterocyclic triazacyclononane (tacn)-based chelators (HNODThia and NODThia-AcNHEt). The chelator HNODThia was further derivatized to obtain a novel PSMA-based bioconjugate (NODThia-PSMA) and a bifunctional photoactivatable azamacrocyclic analogue, NODThia-PEG 3 -ArN 3 , for the development of copper-64 radiopharmaceuticals. 64Cu radiolabeling experiments were performed on the different metal-binding chelates, whereby quantitative radiochemical conversion (RCC) was obtained in less than 10 min at room temperature. The in vitro stability of NODThia-PSMA in human plasma was assessed by ligand-challenge and copper-exchange experiments. Next, we investigated the viability of the photoactivatable analog (NODThia-PEG 3 -ArN 3 ) for the light-induced photoradiosynthesis of radiolabeled proteins. One-pot photoconjugation reactions to human serum albumin (HSA) as a model protein and the clinically relevant monoclonal antibody formulation MetMAb were performed. [64Cu]Cu-7-azepin-HSA and [64Cu]Cu-7-azepin-onartuzumab were prepared in less than 15 min by irradiation at 395 nm, with radiochemical purities (RCP) of >95% and radiochemical yields (RCYs) of 42.7 ± 5.3 and 49.6%, respectively. Together, the results obtained here open the way for the development of highly stable 64Cu-radiopharmaceuticals by using aza-heterocyclic tacn-based chelators, and the method can easily be extended to the development of 67Cu radiopharmaceuticals for future applications in molecularly targeted radio(immuno)therapy.

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Review of commonly used prostate specific PET tracers used in prostate cancer imaging in current clinical practice

Cited by 14 publications

References 76 publications

Management of Patients with Recurrent and Metachronous Oligometastatic Prostate Cancer in the Era of PSMA PET

Management of Patients with Recurrent and Metachronous Oligometastatic Prostate Cancer in the Era of PSMA PET

A Theranostic Small-Molecule Prodrug Conjugate for Neuroendocrine Prostate Cancer

HNODThia: A Promising Chelator for the Development of ⁶⁴Cu Radiopharmaceuticals

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Review of commonly used prostate specific PET tracers used in prostate cancer imaging in current clinical practice

Cited by 14 publications

References 76 publications

Management of Patients with Recurrent and Metachronous Oligometastatic Prostate Cancer in the Era of PSMA PET

Management of Patients with Recurrent and Metachronous Oligometastatic Prostate Cancer in the Era of PSMA PET

A Theranostic Small-Molecule Prodrug Conjugate for Neuroendocrine Prostate Cancer

HNODThia: A Promising Chelator for the Development of 64Cu Radiopharmaceuticals

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Product

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HNODThia: A Promising Chelator for the Development of ⁶⁴Cu Radiopharmaceuticals