68Ga- and 177Lu-Labeled PSMA I&T: Optimization of a PSMA-Targeted Theranostic Concept and First Proof-of-Concept Human Studies
Martina Weineisen
1
,
M. Schottelius
1
,
Jakub Simecek
2
,
Richard P. Baum
3
,
AKIN YILDIZ
4
,
Seval Beykan
5, 6
,
Harshad R. Kulkarni
3
,
Michael Lassmann
5, 6
,
Ingo Klette
3
,
Matthias Eiber
7
,
Markus Schwaiger
7
,
Hans Jürgen Wester
1
3
Theranostics Center for Molecular Radiotherapy and Molecular Imaging (PET/CT), Zentralklinik Bad Berka, Bad Berka, Germany.
|
4
Department of Nuclear Medicine, Medstar Hospital Cancer Center, Antalya, Turkey.
|
6
and.
Publication type: Journal Article
Publication date: 2015-06-18
scimago Q1
SJR: 2.224
CiteScore: 12.6
Impact factor: —
ISSN: 01615505, 2159662X
PubMed ID:
26089548
Radiology, Nuclear Medicine and imaging
Abstract
On the basis of the high and consistent expression of prostate-specific membrane antigen (PSMA) in metastatic prostate cancer (PC), the goal of this study was the development, preclinical evaluation, and first proof-of-concept investigation of a PSMA inhibitor for imaging and therapy (PSMA I&T) for (68)Ga-based PET and (177)Lu-based endoradiotherapeutic treatment in patients with metastatic and castration-resistant disease.PSMA I&T was synthesized in a combined solid phase and solution chemistry strategy. The PSMA affinity of (nat)Ga-/(nat)Lu-PSMA I&T was determined in a competitive binding assay using LNCaP cells. Internalization kinetics of (68)Ga- and (177)Lu-PSMA I&T were investigated using the same cell line, and biodistribution studies were performed in LNCaP tumor-bearing CD-1 nu/nu mice. Initial human PET imaging studies using (68)Ga-PSMA I&T, as well as endoradiotherapeutic treatment of 2 patients with metastatic PC using (177)Lu-PSMA I&T, were performed.PSMA I&T and its cold gallium and lutetium analog revealed nanomolar affinity toward PSMA. The DOTAGA (1,4,7,10-tetraazacyclododecane-1-(glutamic acid)-4,7,10-triacetic acid) conjugate PSMA I&T allowed fast and high-yield labeling with (68)Ga(III) and (177)Lu(III). Uptake of (68)Ga-/(177)Lu-PSMA I&T in LNCaP tumor cells is highly efficient and PSMA-specific, as demonstrated by competition studies both in vitro and in vivo. Tumor targeting and tracer kinetics in vivo were fast, with the highest uptake in tumor xenografts and kidneys (both PSMA-specific). First-in-human (68)Ga-PSMA I&T PET imaging allowed high-contrast detection of bone lesions, lymph node, and liver metastases. Endoradiotherapy with (177)Lu-PSMA I&T in 2 patients was found to be effective and safe with no detectable side effects.(68)Ga-PSMA I&T shows potential for high-contrast PET imaging of metastatic PC, whereas its (177)Lu-labeled counterpart exhibits suitable targeting and retention characteristics for successful endoradiotherapeutic treatment. Prospective studies on larger cohorts of patients are warranted and planned.
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Weineisen M. et al. 68Ga- and 177Lu-Labeled PSMA I&T: Optimization of a PSMA-Targeted Theranostic Concept and First Proof-of-Concept Human Studies // Journal of Nuclear Medicine. 2015. Vol. 56. No. 8. pp. 1169-1176.
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Weineisen M., Schottelius M., Simecek J., Baum R. P., YILDIZ A., Beykan S., Kulkarni H. R., Lassmann M., Klette I., Eiber M., Schwaiger M., Wester H. J. 68Ga- and 177Lu-Labeled PSMA I&T: Optimization of a PSMA-Targeted Theranostic Concept and First Proof-of-Concept Human Studies // Journal of Nuclear Medicine. 2015. Vol. 56. No. 8. pp. 1169-1176.
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TY - JOUR
DO - 10.2967/jnumed.115.158550
UR - https://doi.org/10.2967/jnumed.115.158550
TI - 68Ga- and 177Lu-Labeled PSMA I&T: Optimization of a PSMA-Targeted Theranostic Concept and First Proof-of-Concept Human Studies
T2 - Journal of Nuclear Medicine
AU - Weineisen, Martina
AU - Schottelius, M.
AU - Simecek, Jakub
AU - Baum, Richard P.
AU - YILDIZ, AKIN
AU - Beykan, Seval
AU - Kulkarni, Harshad R.
AU - Lassmann, Michael
AU - Klette, Ingo
AU - Eiber, Matthias
AU - Schwaiger, Markus
AU - Wester, Hans Jürgen
PY - 2015
DA - 2015/06/18
PB - Society of Nuclear Medicine
SP - 1169-1176
IS - 8
VL - 56
PMID - 26089548
SN - 0161-5505
SN - 2159-662X
ER -
Cite this
BibTex (up to 50 authors)
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@article{2015_Weineisen,
author = {Martina Weineisen and M. Schottelius and Jakub Simecek and Richard P. Baum and AKIN YILDIZ and Seval Beykan and Harshad R. Kulkarni and Michael Lassmann and Ingo Klette and Matthias Eiber and Markus Schwaiger and Hans Jürgen Wester},
title = {68Ga- and 177Lu-Labeled PSMA I&T: Optimization of a PSMA-Targeted Theranostic Concept and First Proof-of-Concept Human Studies},
journal = {Journal of Nuclear Medicine},
year = {2015},
volume = {56},
publisher = {Society of Nuclear Medicine},
month = {jun},
url = {https://doi.org/10.2967/jnumed.115.158550},
number = {8},
pages = {1169--1176},
doi = {10.2967/jnumed.115.158550}
}
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MLA
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Weineisen, Martina, et al. “68Ga- and 177Lu-Labeled PSMA I&T: Optimization of a PSMA-Targeted Theranostic Concept and First Proof-of-Concept Human Studies.” Journal of Nuclear Medicine, vol. 56, no. 8, Jun. 2015, pp. 1169-1176. https://doi.org/10.2967/jnumed.115.158550.