Prostate-specific membrane antigen ligands for imaging and therapy

Matthias Eiber, Wolfgang P. Fendler, Steven Rowe, Jeremie Calais, Michael S. Hofman, Tobias Maurer, Sarah M. Schwarzenboeck, Clemens Kratowchil, Ken Herrmann, Frederik L. Giesel

Research output: Contribution to journalReview article

Abstract

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-urea- based PSMA ligands used for both imaging and radioligand therapy are the mainstays of the current success. For PET imaging, both 68Gaand 18F-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 177Lu-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 177Lu-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.

Original languageEnglish (US)
Pages (from-to)67S-76S
JournalJournal of Nuclear Medicine
Volume58
DOIs
StatePublished - Sep 1 2017

Fingerprint

Ligands
Prostatic Neoplasms
Therapeutics
Prostate-Specific Antigen
human glutamate carboxypeptidase II
Recurrence
Urea
Neoplasms
Cohort Studies
Retrospective Studies
Molecular Weight
Lymph Nodes
Safety

Keywords

  • Imaging
  • Prostate cancer
  • Prostate-specific membrane antigen
  • Therapy

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging

Cite this

Eiber, M., Fendler, W. P., Rowe, S., Calais, J., Hofman, M. S., Maurer, T., ... Giesel, F. L. (2017). Prostate-specific membrane antigen ligands for imaging and therapy. Journal of Nuclear Medicine, 58, 67S-76S. https://doi.org/10.2967/jnumed.116.186767

Prostate-specific membrane antigen ligands for imaging and therapy. / Eiber, Matthias; Fendler, Wolfgang P.; Rowe, Steven; Calais, Jeremie; Hofman, Michael S.; Maurer, Tobias; Schwarzenboeck, Sarah M.; Kratowchil, Clemens; Herrmann, Ken; Giesel, Frederik L.

In: Journal of Nuclear Medicine, Vol. 58, 01.09.2017, p. 67S-76S.

Research output: Contribution to journalReview article

Eiber, M, Fendler, WP, Rowe, S, Calais, J, Hofman, MS, Maurer, T, Schwarzenboeck, SM, Kratowchil, C, Herrmann, K & Giesel, FL 2017, 'Prostate-specific membrane antigen ligands for imaging and therapy', Journal of Nuclear Medicine, vol. 58, pp. 67S-76S. https://doi.org/10.2967/jnumed.116.186767
Eiber, Matthias ; Fendler, Wolfgang P. ; Rowe, Steven ; Calais, Jeremie ; Hofman, Michael S. ; Maurer, Tobias ; Schwarzenboeck, Sarah M. ; Kratowchil, Clemens ; Herrmann, Ken ; Giesel, Frederik L. / Prostate-specific membrane antigen ligands for imaging and therapy. In: Journal of Nuclear Medicine. 2017 ; Vol. 58. pp. 67S-76S.
@article{e72da54054a74402ac8f6364cd56bcf4,
title = "Prostate-specific membrane antigen ligands for imaging and therapy",
abstract = "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-urea- based PSMA ligands used for both imaging and radioligand therapy are the mainstays of the current success. For PET imaging, both 68Gaand 18F-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 177Lu-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 177Lu-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.",
keywords = "Imaging, Prostate cancer, Prostate-specific membrane antigen, Therapy",
author = "Matthias Eiber and Fendler, {Wolfgang P.} and Steven Rowe and Jeremie Calais and Hofman, {Michael S.} and Tobias Maurer and Schwarzenboeck, {Sarah M.} and Clemens Kratowchil and Ken Herrmann and Giesel, {Frederik L.}",
year = "2017",
month = "9",
day = "1",
doi = "10.2967/jnumed.116.186767",
language = "English (US)",
volume = "58",
pages = "67S--76S",
journal = "Journal of Nuclear Medicine",
issn = "0161-5505",
publisher = "Society of Nuclear Medicine Inc.",

}

TY - JOUR

T1 - Prostate-specific membrane antigen ligands for imaging and therapy

AU - Eiber, Matthias

AU - Fendler, Wolfgang P.

AU - Rowe, Steven

AU - Calais, Jeremie

AU - Hofman, Michael S.

AU - Maurer, Tobias

AU - Schwarzenboeck, Sarah M.

AU - Kratowchil, Clemens

AU - Herrmann, Ken

AU - Giesel, Frederik L.

PY - 2017/9/1

Y1 - 2017/9/1

N2 - 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-urea- based PSMA ligands used for both imaging and radioligand therapy are the mainstays of the current success. For PET imaging, both 68Gaand 18F-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 177Lu-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 177Lu-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.

AB - 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-urea- based PSMA ligands used for both imaging and radioligand therapy are the mainstays of the current success. For PET imaging, both 68Gaand 18F-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 177Lu-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 177Lu-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.

KW - Imaging

KW - Prostate cancer

KW - Prostate-specific membrane antigen

KW - Therapy

UR - http://www.scopus.com/inward/record.url?scp=85028887873&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=85028887873&partnerID=8YFLogxK

U2 - 10.2967/jnumed.116.186767

DO - 10.2967/jnumed.116.186767

M3 - Review article

VL - 58

SP - 67S-76S

JO - Journal of Nuclear Medicine

JF - Journal of Nuclear Medicine

SN - 0161-5505

ER -