The utility of radiolabeled PSMA ligands for tumor imaging

Shahrokhi, Pejman; Farahani, Arezou Masteri; Tamaddondar, Mohammad; Rezazadeh, Farzaneh

doi:10.1111/cbdd.13946

Cited by 4 publications

(2 citation statements)

References 179 publications

(170 reference statements)

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“…Small ureabased pseudo-peptide inhibitors are the most commonly studied type of PSMA-targeting radioligands for both diagnostic and therapeutic applications. Several studies have focused on optimising the molecular design of such tracers, resulting in novel compounds with improved targeting properties [5][6][7]. Consequently, numerous clinical studies of PSMA-targeting radioligands for imaging and radioligand therapy with promising results are also ongoing [8]: [ 68 Ga]Ga-PSMA-11 and [ 18 F]F-DCFPyL for positron emission tomography (PET) imaging of PSMA-positive lesions, and the theranostic pair [ 68 Ga]Ga-PSMA-617/[ 177 Lu]Lu-PSMA-617 for treatment of progressive PSMA-positive metastatic castration-resistant PCa are three PSMA-binding radioligands approved by the Food and Drug Administration (FDA) [9][10][11][12].…”

Section: Introductionmentioning

confidence: 99%

Preclinical Characterisation of PSMA/GRPR-Targeting Heterodimer [68Ga]Ga-BQ7812 for PET Diagnostic Imaging of Prostate Cancer: A Step towards Clinical Translation

Lundmark

Abouzayed

Rinne

et al. 2023

Cancers

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The development of radioligands targeting prostate-specific membrane antigen (PSMA) and gastrin-releasing peptide receptor (GRPR) has shown promising results for the imaging and therapy of prostate cancer. However, studies have shown that tumors and metastases can express such targets heterogeneously. To overcome this issue and to improve protein binding, radioligands with the ability to bind both PSMA and GRPR have been developed. Herein, we present the preclinical characterization of [68Ga]Ga-BQ7812; a PSMA/GRPR-targeting radioligand for the diagnostic PET imaging of prostate cancer. This study aimed to evaluate [68Ga]Ga-BQ7812 to promote the translation of such imaging probes into the clinic. [68Ga]Ga-BQ7812 demonstrated rapid and specific binding to both targets in a PSMA/GRPR-expressing PC3-pip cell line. Results from the biodistribution study in PC3-pip xenografted mice showed specific binding to both targets, with the highest activity uptake at 1 h pi in tumor (PSMA+/GRPR+, 10.4 ± 1.0% IA/g), kidneys (PSMA+, 45 ± 16% IA/g), and pancreas (GRPR+, 5.6 ± 0.7% IA/g). At 3h pi, increased tumour-to-organ ratios could be seen due to higher retention in the tumor compared with other PSMA or GRPR-expressing organs. These results, together with low toxicity and an acceptable estimated dosimetry profile (total effective dose = 0.0083 mSv/MBq), support the clinical translation of [68Ga]Ga-BQ7812 and represent a step towards its first clinical trial.

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Section: Introductionmentioning

confidence: 99%

Preclinical Characterisation of PSMA/GRPR-Targeting Heterodimer [68Ga]Ga-BQ7812 for PET Diagnostic Imaging of Prostate Cancer: A Step towards Clinical Translation

Lundmark

Abouzayed

Rinne

et al. 2023

Cancers

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“…Action of PSMA-Targeted Theranostic Agent Ga-PSMA-11, 18 F-PSMA-11, 18 F-PSMA-1007, 18 F-rhPSMA 7.3, 68 Ga-PSMA-617, 68 Cu-PSMA-I&T, 44 Sc-PSMA-617 등이 전임상 및 임상 연구에 활발히 적용되기 시작하였다. 34 2. Therapeutic Performance 시 비례해서 높아졌다(73% for <0.5 ng/mL vs. 75% for 0.5 to <1.0 ng/mL vs. 83% for 1.0 to <2.0 ng/mL vs. 91% for 2.0 to <5.0 ng/mL vs. 96% for ≥5.0 ng/ mL).…”

mentioning

confidence: 99%

An Update of Prostate-Specific Membrane Antigen Theranostics in Prostate Cancer

Hong¹

2022

Korean J Urol Oncol

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Theranostics is a new term which involves the integration of therapy and diagnosis in a single platform. Prostate-specific membrane antigen (PSMA) has emerged to be a novel promising target for both diagnostic imaging and therapeutics of prostate cancer. During the past decade, radiotracers targeting the PSMA for positron emission tomography (PET) have been developed. These PET tracers are small molecular inhibitors that bind the extracellular domain of PSMA. With the recent approval of radioisotope labeled PSMA PET for clinical use, the field of PSMA theranostics has come under the spotlight. Can the preliminary efficacy and safety data on PSMA theranostics may change the prostate cancer landscape? In this review, we will focus on the history of development, approval of drug, and diagnostic and therapeutic performance of PSMA PET in patients with prostate cancer.

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Radiolabeled vitamins as the potential diagnostic probes for targeted tumor imaging

Shahrokhi

Farahani

Tamaddondar

2022

Bioorganic Chemistry

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The utility of radiolabeled PSMA ligands for tumor imaging

Abstract: Prostate-specific membrane antigen (PSMA) as an excellent target for molecular imaging of cancer is a 750-amino

Cited by 4 publications

References 179 publications

Preclinical Characterisation of PSMA/GRPR-Targeting Heterodimer [68Ga]Ga-BQ7812 for PET Diagnostic Imaging of Prostate Cancer: A Step towards Clinical Translation

Preclinical Characterisation of PSMA/GRPR-Targeting Heterodimer [68Ga]Ga-BQ7812 for PET Diagnostic Imaging of Prostate Cancer: A Step towards Clinical Translation

An Update of Prostate-Specific Membrane Antigen Theranostics in Prostate Cancer

Radiolabeled vitamins as the potential diagnostic probes for targeted tumor imaging

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