The Performance of FDA-Approved PET Imaging Agents in the Detection of Prostate Cancer

Abstract

Positron emission tomography (PET) incorporated with X-ray computed tomography (PET/CT) or magnetic resonance imaging (PET/MRI) is increasingly being used as a diagnostic tool for prostate cancer (PCa). In this review, we describe and evaluate the clinical performance of some Food and Drug Administration (FDA)-approved agents used for visualizing PCa: [18F]FDG, [11C]choline, [18F]FACBC, [68Ga]Ga-PSMA-11, [18F]DCFPyL, and [18F]-NaF. We carried out a comprehensive literature search based on articles published from 1 January 2010 to 1 March 2022. We selected English language articles associated with the discovery, preclinical study, clinical study, and diagnostic performance of the imaging agents for the evaluation. Prostate-specific membrane antigen (PSMA)-targeted imaging agents demonstrated superior diagnostic performance in both primary and recurrent PCa, compared with [11C]choline and [18F]FACBC, both of which target dividing cells and are used especially in patients with low prostate-specific antigen (PSA) values. When compared to [18F]-NaF (which is suitable for the detection of bone metastases), PSMA-targeted agents were also capable of detecting lesions in the lymph nodes, soft tissues, and bone. However, a limitation of PSMA-targeted imaging was the heterogeneity of PSMA expression in PCa, and consequently, a combination of two PET tracers was proposed to overcome this obstacle. The preliminary studies indicated that the use of PSMA-targeted scanning is more cost efficient than conventional imaging modalities for high-risk PCa patients. Furthering the development of imaging agents that target PCa-associated receptors and molecules could improve PET-based diagnosis of PCa.

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“…Also, another radiotracer, 64 Cu-DOTA-AE105, is designed to target the human urokinase-type plasminogen activator receptor (uPAR) expressed in cancer cells. It is used to improve prostate cancer diagnosis, diagnose aggressive cancers, and determine cancer aggressiveness [33][34][35].…”

Preclinical Evaluation of a Novel High-Affinity Radioligand [99mTc]Tc-BQ0413 Targeting Prostate-Specific Membrane Antigen (PSMA)

“…Interest has grown in molecular imaging using positron emission tomography (PET) and single-photon emission computed tomography (SPECT) for the diagnosis of prostate cancer [2]. Several radiolabeled imaging probes have been approved for the visualization of prostate cancer [3]. Among the cellular mechanisms and molecular targets that can be used for diagnostic imaging in prostate cancer patients are cell division, including upregulated metabolic activity and the synthesis of cell components; osteoblastic activity in bone metastases; and numerous extracellular antigens and receptors, e.g., androgen receptor, prostate-specific membrane antigen (PSMA), gastrin-releasing peptide receptor (GRPR), urokinase-type plasminogen activator (uPA), prostate stem cell antigen (PSCA), six transmembrane epithelial antigen of prostate (STEAP1), and CD46 [4].…”