Preliminary evaluation of a novel 18F-labeled PARP-1 ligand for PET imaging of PARP-1 expression in prostate cancer

Xu, Jinbin; Mpoy, Cedric; Chu, Wenhua; Kim, Sung Hoon; Li, Huifangjie; Rogers, Buck E.; Katzenellenbogen, John A.

doi:10.1016/j.nucmedbio.2018.08.003

Cited by 32 publications

(40 citation statements)

References 24 publications

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“…In microPET imaging study 18 F-WC-DW-F accumulated and remained in the target tumor (close to 4% ID/c.c. at 2-h post-injection) but readily washed out from other organs and tissue, except for the liver [36].…”

Section: Poly (Adp-ribose) Polymerase-1 (Parp-1)mentioning

confidence: 99%

Prognostic and Theranostic Applications of Positron Emission Tomography for a Personalized Approach to Metastatic Castration-Resistant Prostate Cancer

Filippi

Frantellizzi

Chiaravalloti

et al. 2021

IJMS

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Metastatic castration-resistant prostate cancer (mCRPC) represents a condition of progressive disease in spite of androgen deprivation therapy (ADT), with a broad spectrum of manifestations ranging from no symptoms to severe debilitation due to bone or visceral metastatization. The management of mCRPC has been profoundly modified by introducing novel therapeutic tools such as antiandrogen drugs (i.e., abiraterone acetate and enzalutamide), immunotherapy through sipuleucel-T, and targeted alpha therapy (TAT). This variety of approaches calls for unmet need of biomarkers suitable for patients’ pre-treatment selection and prognostic stratification. In this scenario, imaging with positron emission computed tomography (PET/CT) presents great and still unexplored potential to detect specific molecular and metabolic signatures, some of whom, such as the prostate specific membrane antigen (PSMA), can also be exploited as therapeutic targets, thus combining diagnosis and therapy in the so-called “theranostic” approach. In this review, we performed a web-based and desktop literature research to investigate the prognostic and theranostic potential of several PET imaging probes, such as 18F-FDG, 18F-choline and 68Ga-PSMA-11, also covering the emerging tracers still in a pre-clinical phase (e.g., PARP-inhibitors’ analogs and the radioligands binding to gastrin releasing peptide receptors/GRPR), highlighting their potential for defining personalized care pathways in mCRPC

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Section: Poly (Adp-ribose) Polymerase-1 (Parp-1)mentioning

confidence: 99%

Prognostic and Theranostic Applications of Positron Emission Tomography for a Personalized Approach to Metastatic Castration-Resistant Prostate Cancer

Filippi

Frantellizzi

Chiaravalloti

et al. 2021

IJMS

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“…The PET radionuclide 18 F (half-life/T 1/2 = 109.771 min) is one of the most favored diagnostic radionuclides in PARP imaging probes. 18 F conjugated PARPis like olaparib ( 18 F-Olaparib) [17], olaparib derivatives ( 18 F-20 [15], 18 F-PARPi [16]), and rucaparib derivatives ( 18 F-Fluorthanatrace ( 18 F-FTT) [25], 18 F-WC-DZ-F [26]) have been evaluated for imaging of PARP1 expression.…”

Section: Radio-fluorinated Parp Tracersmentioning

confidence: 99%

“…Apart from olaparib derivatives, a rucaparib derivative, 18 F-WC-DZ-F has been characterized in a subcutaneous prostate cancer model [ 26 ]. Structurally, it is an analogue of 18 F-FTT, which is currently in clinical trials.…”

Section: Imaging With Parp-addressing Tracersmentioning

confidence: 99%

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Advancements in PARP1 Targeted Nuclear Imaging and Theranostic Probes

Sankaranarayanan

Kossatz

Weber

et al. 2020

JCM

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The central paradigm of novel therapeutic approaches in cancer therapy is identifying and targeting molecular biomarkers. One such target is the nuclear DNA repair enzyme Poly-(ADP ribose) polymerase 1 (PARP1). Sensitivity to PARP inhibition in certain cancers such as gBRCAmut breast and ovarian cancers has led to its exploitation as a target. The overexpression of PARP1 in several types of cancer further evoked interest in its use as an imaging target. While PARP1-targeted inhibitors have fast developed and approved in this past decade, determination of PARP1 expression might help to predict the response to PARP inhibitor treatment. This has the potential of improving prognosis and moving towards tailored therapy options and/or dosages. This review summarizes the recent pre-clinical advancements in imaging and theranostic PARP1 targeted tracers. To assess PARP1 levels, several imaging probes with fluorescent or beta/gamma emitting radionuclides have been proposed and three have advanced to ongoing clinical evaluation. Apart from its diagnostic value in detection of primary tumors as well as metastases, this shall also help in delivering therapeutic radionuclides to PARP1 overexpressing tumors. Henceforth nuclear medicine has now advanced towards conjugating theranostic radionuclides to PARP1 inhibitors. This paves the way for a future of PARP1-targeted theranostics and personalized therapy.

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“…In clinical routine PET imaging of the somatostatin receptor (SSTR) in patients with neuroendocrine tumours (NETs) employing on [ 68 Ga]Ga-DOTA-peptides such as [ 68 Ga]Ga-DOTATOC or [ 68 Ga]Ga-DOTATATE is the gold standard [ 4 ]. Current guidelines recommend a preplacement of [ 111 In]In-DTPA-octreotide by [ 68 Ga]-labelled SSAs [ 5 ]. The theranostic pair with [ 177 Lu]Lu-DOTATOC or [ 177 Lu]Lu-DOTATATE as radiotracers for peptide receptor radionuclide therapy (PRRT) has been established [ 6 ].…”

mentioning

confidence: 99%

The battle on time, money and precision: Da[18F] id vs. [68Ga]liath

Sahnoun

Conen

Mottaghy

2020

Eur J Nucl Med Mol Imaging

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Preliminary evaluation of a novel 18F-labeled PARP-1 ligand for PET imaging of PARP-1 expression in prostate cancer

Abstract: We synthesized a novel PARP-1 radioligand, [F]WC-DZ-F. The preliminary evaluation of [F]WC-DZ-F indicates that it is a suitable PET imaging agent for measuring PARP-1 expression in prostate cancer and should be applicable to other types of cancers.

Cited by 32 publications

References 24 publications

Prognostic and Theranostic Applications of Positron Emission Tomography for a Personalized Approach to Metastatic Castration-Resistant Prostate Cancer

Prognostic and Theranostic Applications of Positron Emission Tomography for a Personalized Approach to Metastatic Castration-Resistant Prostate Cancer

Advancements in PARP1 Targeted Nuclear Imaging and Theranostic Probes

The battle on time, money and precision: Da[18F] id vs. [68Ga]liath

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