Radiolabeled enzyme inhibitors and binding agents targeting PSMA: Effective theranostic tools for imaging and therapy of prostate cancer

Pillai, M.R.A.; Nanabala, Raviteja; Joy, Ajith; Sasikumar, Arun; Knapp, F. F.

doi:10.1016/j.nucmedbio.2016.08.006

Cited by 65 publications

(35 citation statements)

References 197 publications

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“…Due to such favorable findings, 18 F-DCFPyL was further evaluated in several clinical studies and is still a popular imaging agent in the United States. [98][99][100][101][102] In 2014, Bayer Healthcare developed an 18 F-labeled ligand, called BAY 1075553. 103 BAY 1075553 is a 9:1 mixture of the two stereoisomers (2S,4S)-and (2R,4S)-2-[ 18 F]fluoro-4-phosphonomethyl-pentanedioic acid that could be synthesized by nucleophilic radiofluorination of the precursor.…”

Section: Carbon-11mentioning

confidence: 99%

Targeting prostate cancer: Prostate‐specific membrane antigen based diagnosis and therapy

Wüstemann

Haberkorn

Babich

et al. 2018

Medicinal Research Reviews

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The high incidence rates of prostate cancer (PCa) raise demand for improved therapeutic strategies. Prostate tumors specifically express the prostate-specific membrane antigen (PSMA), a membrane-bound protease. As PSMA is highly overexpressed on malignant prostate tumor cells and as its expression rate correlates with the aggressiveness of the disease, this tumor-associated biomarker provides the possibility to develop new strategies for diagnostics and therapy of PCa. Major advances have been made in PSMA targeting, ranging from immunotherapeutic approaches to therapeutic small molecules. This review elaborates the diversity of PSMA targeting agents while focusing on the radioactively labeled tracers for diagnosis and endoradiotherapy. A variety of radionuclides have been shown to either enable precise diagnosis or efficiently treat the tumor with minimal effects to nontargeted organs. Most small molecules with affinity for PSMA are based on either a phosphonate or a urea-based binding motif. Based on these pharmacophores, major effort has been made to identify modifications to achieve ideal pharmacokinetics while retaining the specific targeting of the PSMA binding pocket. Several tracers have now shown excellent clinical usability in particular for molecular imaging and therapy as proven by the efficiency of theranostic approaches in current studies. The archetypal expression profile of PSMA may be exploited for the treatment with alpha emitters to break radioresistance and thus to bring the power of systemic therapy to higher levels.

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Section: Carbon-11mentioning

confidence: 99%

Targeting prostate cancer: Prostate‐specific membrane antigen based diagnosis and therapy

Wüstemann

Haberkorn

Babich

et al. 2018

Medicinal Research Reviews

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show abstract

“…These compounds based on lysine-glutamate-urea derivatives, first developed as inhibitors of the enzymatic activity of PSMA, have been labelled by a variety of radionuclides for PET imaging and radionuclide therapy for theranostic approaches in prostate cancer patients. A variety of closely related compounds are under investigation [29]. Retrospective studies have suggested a high sensitivity of PET using 68 Ga-PSMA ligands in early restaging of prostate cancer but, as with other PET tracers, their value in primary tumour staging is yet to be determined, especially in patients with high-risk disease [30, 31].…”

Section: Psma and Somatostatin Receptor Imaging And Therapy: High Thrmentioning

confidence: 99%

Highlights lecture EANM 2016: “Embracing molecular imaging and multi-modal imaging: a smart move for nuclear medicine towards personalized medicine”

Aboagye

Kraeber-Bodéré

2017

Eur J Nucl Med Mol Imaging

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The 2016 EANM Congress took place in Barcelona, Spain, from 15 to 19 October under the leadership of Prof. Wim Oyen, chair of the EANM Scientific Committee. With more than 6,000 participants, this congress was the most important European event in nuclear medicine, bringing together a multidisciplinary community involved in the different fields of nuclear medicine. There were over 600 oral and 1,200 poster or e-Poster presentations with an overwhelming focus on development and application of imaging for personalized care, which is timely for the community. Beyond FDG PET, major highlights included progress in the use of PSMA and SSTR receptor-targeted radiopharmaceuticals and associated theranostics in oncology. Innovations in radiopharmaceuticals for imaging pathologies of the brain and cardiovascular system, as well as infection and inflammation, were also highlighted. In the areas of physics and instrumentation, multimodality imaging and radiomics were highlighted as promising areas of research.

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“…In 2018, refined advances in prostate‐specific membrane antigen (PSMA)‐targeted PET/CT imaging techniques using various positron emission radioisotopes for early detection of PCa, management of metastatic castration‐resistant prostate cancer (mCRPC), and their applications in detection of recurrent disease by guided biopsy and surgery were published. There are also recent reports that exclusively cover clinical translation of PSMA‐targeted 68 Ga and 177 Lu radioisotopes for detection and therapy of PCa in humans . However, a comprehensive analysis exhaustively describing various diagnostic methodologies using targeted molecular imaging techniques is yet to be compiled.…”

Section: Introductionmentioning

confidence: 99%

“…There are also recent reports that exclusively cover clinical translation of PSMA-targeted 68 Ga and 177 Lu radioisotopes for detection and therapy of PCa in humans. [17][18][19] However, a comprehensive analysis exhaustively describing various diagnostic methodologies using targeted molecular imaging techniques is yet to be compiled.…”

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confidence: 99%

Comparison of prostate‐specific membrane antigen ligands in clinical translation research for diagnosis of prostate cancer

et al. 2019

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Background Prostate‐specific membrane antigen (PSMA), overexpressed on prostate cancer (PCa), is a well‐characterized cell surface protein to selectively diagnose PCa. PSMA's unique characteristics and its 1000‐fold higher expression in PCa compared with other tissues renders it as a suitable biomarker for detection of PCa in its early stage. In this report, we critically analyze and recommend the requirements needed for the development of variety of PSMA‐targeted molecular imaging agents based on antibodies, small molecule ligands, peptides, and aptamers. The targeting moieties are either conjugated to radionuclear isotopes or near‐infrared agents for efficient diagnosis of PCa. Recent findings From the analysis, it was found that several small molecule–derived PCa imaging agents are approved for clinical trials in Europe and the United States, and few are already in the clinical use for diagnosis of PCa. Even though 111In‐labeled capromab pendetide was approved by the Food and Drug Administration (FDA) and other engineered antibodies are available for detection of PCa, but high production cost, low shelf life (less than 1 month at 4°C), possibility of human immuno reactions, and low blood clearance rate necessitated a need for developing new imaging agents, which are serum stable, cost‐effective, and possesses longer shelf life (6 months), have fast clearance rate from nontargeted tissues during the diagnosis process. It is found that small molecule ligand‐derived imaging agents possesses most of the desired properties expected for an ideal diagnostic agent when compared with other targeting moieties. Conclusion This report discusses in detail the homing moieties used in the development of targeted diagnostic tools for detection of PCa. The merits and demerits of monoclonal antibodies, small molecule ligands, peptides, and aptamers for imaging of PCa and intraoperative guided surgery are extensively analyzed. Among all, urea‐based ligands were found to be most successful in preclinical and clinical trials and show a major promise for future commercialization.

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Radiolabeled enzyme inhibitors and binding agents targeting PSMA: Effective theranostic tools for imaging and therapy of prostate cancer

Cited by 65 publications

References 197 publications

Targeting prostate cancer: Prostate‐specific membrane antigen based diagnosis and therapy

Targeting prostate cancer: Prostate‐specific membrane antigen based diagnosis and therapy

Highlights lecture EANM 2016: “Embracing molecular imaging and multi-modal imaging: a smart move for nuclear medicine towards personalized medicine”

Comparison of prostate‐specific membrane antigen ligands in clinical translation research for diagnosis of prostate cancer

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