Prostate-Specific Membrane Antigen Ligands for Imaging and Therapy
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Prostate-Specific Membrane Antigen Ligands for Imaging and Therapy : J Nucl Med. / Eiber, M.; Fendler, W. P.; Rowe, S. P.; Calais, J.; Hofman, M. S.; Maurer, T.; Schwarzenboeck, S. M.; Kratowchil, C.; Herrmann, K.; Giesel, F. L.
In: J NUCL MED, Vol. 58, No. Suppl 2, 2017, p. 67s-76s.Research output: SCORING: Contribution to journal › SCORING: Journal article › Research
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TY - JOUR
T1 - Prostate-Specific Membrane Antigen Ligands for Imaging and Therapy
T2 - J Nucl Med
AU - Eiber, M.
AU - Fendler, W. P.
AU - Rowe, S. P.
AU - Calais, J.
AU - Hofman, M. S.
AU - Maurer, T.
AU - Schwarzenboeck, S. M.
AU - Kratowchil, C.
AU - Herrmann, K.
AU - Giesel, F. L.
N1 - 1535-5667 Eiber, Matthias Fendler, Wolfgang P Rowe, Steven P Calais, Jeremie Hofman, Michael S Maurer, Tobias Schwarzenboeck, Sarah M Kratowchil, Clemens Herrmann, Ken Giesel, Frederik L Journal Article Review United States J Nucl Med. 2017 Sep;58(Suppl 2):67S-76S. doi: 10.2967/jnumed.116.186767.
PY - 2017
Y1 - 2017
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 (68)Ga- and (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 castration-resistant 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 (68)Ga- and (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 castration-resistant 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 - Animals Antigens, Surface/metabolism Diagnostic Imaging/methods Glutamate Carboxypeptidase II/metabolism Humans Ligands Molecular Targeted Therapy/methods Neoplasms/diagnostic imaging/metabolism/radiotherapy imaging prostate cancer prostate-specific membr
U2 - 10.2967/jnumed.116.186767
DO - 10.2967/jnumed.116.186767
M3 - SCORING: Journal article
VL - 58
SP - 67s-76s
JO - J NUCL MED
JF - J NUCL MED
SN - 0161-5505
IS - Suppl 2
ER -
