Prostate-Specific Membrane Antigen–Targeted Radiohalogenated PET and Therapeutic Agents for Prostate Cancer

Rowe, Steven P.; Drzezga, Alexander; Neumaier, Bernd; Dietlein, Markus; Gorin, Michael A.; Zalutsky, Michael R.; Pomper, Martin G.

doi:10.2967/jnumed.115.170175

Cited by 50 publications

(33 citation statements)

References 66 publications

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“…Recent reviews described in detail the history and different characteristics of a broad spectrum of PSMA ligands, which is beyond the scope of this review (59)(60)(61). Table 1 provides an overview of the most commonly used low-molecular-weight PSMA ligands.…”

Section: Comprehensive Overview Of Different Classes Of Psma Ligands mentioning

confidence: 99%

Prostate-Specific Membrane Antigen Ligands for Imaging and Therapy

et al. 2017

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The prostate-specific membrane antigen (PSMA) is highly expressed on most prostate cancer (PC) cells. Therefore, the targeting of PSMA has become increasingly important over the last decade. Glu-ureabased PSMA ligands used for both imaging and radioligand therapy are the mainstays of the current success. For PET imaging, both 68 Gaand 18 F-labeled agents have been successfully translated to clinical applications. Mainly retrospective cohort studies have shown a high value in the setting of biochemical recurrence, with high detection rates even in the presence of low prostate-specific antigen levels. Preliminary data indicated that radioguided surgery with PSMA ligands may help to further improve patient outcomes because it facilitates the removal of small tumor deposits that are otherwise difficult to detect. For primary PC, PSMA ligand PET imaging has been shown to be superior to cross-sectional imaging for the detection of metastatic lymph nodes. In addition, it promises to also provide intraprostatic tumor localization, especially when used in combination with multiparametric MRI. Increasing numbers of studies have reported considerable changes in management resulting from PSMA ligand PET imaging for both biochemical recurrence and primary disease. The use of 177 Lu-PSMA-based radioligand therapy has demonstrated a reasonable response, mainly as defined by a prostate-specific antigen response of more than 50%, comparable to other recently introduced agents. Especially given the high level of safety of 177 Lu-PSMA radioligand therapy, with only minimal grade 3 and 4 toxicities reported so far, it has the potential to expand options for metastatic castrationresistant PC. This review is intended to provide a comprehensive overview of the current literature on low-molecular-weight PSMA ligands for both PET imaging and therapeutic approaches, with a focus on agents that have been clinically adopted.

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Section: Comprehensive Overview Of Different Classes Of Psma Ligands mentioning

confidence: 99%

Prostate-Specific Membrane Antigen Ligands for Imaging and Therapy

et al. 2017

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“…Prostate-specific membrane antigen (PSMA) is overexpressed in most cases of prostate cancer and is potentially associated with metastasis and progression of prostate cancer (3). Clinical studies have increasingly confirmed that PSMA is a valuable target for both the diagnosis and the treatment of prostate cancer (4,5). Radiolabeled urea derivatives, including 18 F-DCFBC (6), 18 F-DCFPyL (7), 68 Ga-PSMA-HBED-CC (8), 99m Tc-MIP-1404 (9), 68 Ga/ 64 Cu-DKFZ-PSMA-617 (10)(11)(12), and 18 F-PSMA-1007 (13,14), have been reported to detect primary and metastatic prostate cancer lesions.…”

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Preclinical Evaluation and Pilot Clinical Study of Al¹⁸F-PSMA-BCH for Prostate Cancer PET Imaging

Liu

et al. 2019

J Nucl Med

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“…15,16 Indeed, multiple fluorinated compounds targeting PSMA have been developed. 17,18 Furthest along in clinical development is the 18 F-DCFPyL radiotracer, which was first described by Chen et al 19 This radiotracer has been examined in several studies in the context of imaging biochemically recurrent or metastatic PCa. 20–22 …”

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Prostate Specific Membrane Antigen Targeted ¹⁸ F-DCFPyL Positron Emission Tomography/Computerized Tomography for the Preoperative Staging of High Risk Prostate Cancer: Results of a Prospective, Phase II, Single Center Study

et al. 2018

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Purpose We prospectively evaluated the diagnostic performance of prostate specific membrane antigen targeted 18F-DCFPyL positron emission tomography/computerized tomography in the preoperative staging of men at high risk for harboring metastatic prostate cancer despite a negative conventional staging evaluation. Materials and Methods Men with clinically localized high or very high risk prostate cancer were imaged with 18F-DCFPyL positron emission tomography/computerized tomography before undergoing radical prostatectomy with standardized pelvic lymph node dissection. The scans were interpreted by 2 blinded nuclear medicine readers and assessed for interreader variability as well as diagnostic accuracy for pelvic lymph node staging. Surgical pathology served as the reference standard to which 18F-DCFPyL scan findings were compared. Results A total of 25 men contributed analyzable data to this study. Seven of these patients (28%) were found to have 1 or more positive lymph nodes on surgical pathology. Sites of radiotracer uptake were identified in the prostate of all imaged patients. The 2 readers identified the same number of prostatic lesions in 22 patients (88%), of whom all had at least 1 intraprostatic lesion in common between the 2 reads. Additionally, the readers assigned the same N stage to 46 of 50 individual lymph node packets (92%). Following reconciliation of the relatively few discordant imaging reads, 7 patients (28%) were found to have 1 or more sites of radiotracer uptake in the pelvis consistent with N1 disease, resulting in 71.4% sensitivity (95% CI 29.0–96.3) and 88.9% specificity (95% CI 65.3–98.6). Analysis at the level of individual nodal packets resulted in 66.7% sensitivity (95% CI 29.9–92.5) and 92.7% specificity (95% CI 80.1–98.5). Three men (12%) had evidence of M1a disease. Conclusions 18F-DCFPyL positron emission tomography/computerized tomography allowed for accurate detection of prostate cancer sites in men believed to have clinically localized disease based on conventional imaging. Our results support the need for a larger study to more precisely define the diagnostic accuracy of this novel molecular imaging test.

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Prostate-Specific Membrane Antigen–Targeted Radiohalogenated PET and Therapeutic Agents for Prostate Cancer

Cited by 50 publications

References 66 publications

Prostate-Specific Membrane Antigen Ligands for Imaging and Therapy

Prostate-Specific Membrane Antigen Ligands for Imaging and Therapy

Preclinical Evaluation and Pilot Clinical Study of Al¹⁸F-PSMA-BCH for Prostate Cancer PET Imaging

Prostate Specific Membrane Antigen Targeted ¹⁸ F-DCFPyL Positron Emission Tomography/Computerized Tomography for the Preoperative Staging of High Risk Prostate Cancer: Results of a Prospective, Phase II, Single Center Study

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Prostate-Specific Membrane Antigen–Targeted Radiohalogenated PET and Therapeutic Agents for Prostate Cancer

Cited by 50 publications

References 66 publications

Prostate-Specific Membrane Antigen Ligands for Imaging and Therapy

Prostate-Specific Membrane Antigen Ligands for Imaging and Therapy

Preclinical Evaluation and Pilot Clinical Study of Al18F-PSMA-BCH for Prostate Cancer PET Imaging

Prostate Specific Membrane Antigen Targeted 18 F-DCFPyL Positron Emission Tomography/Computerized Tomography for the Preoperative Staging of High Risk Prostate Cancer: Results of a Prospective, Phase II, Single Center Study

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Preclinical Evaluation and Pilot Clinical Study of Al¹⁸F-PSMA-BCH for Prostate Cancer PET Imaging

Prostate Specific Membrane Antigen Targeted ¹⁸ F-DCFPyL Positron Emission Tomography/Computerized Tomography for the Preoperative Staging of High Risk Prostate Cancer: Results of a Prospective, Phase II, Single Center Study