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10.08.2019 | Original Article | Ausgabe 12/2019

European Journal of Nuclear Medicine and Molecular Imaging 12/2019

177Lu-labeled low-molecular-weight agents for PSMA-targeted radiopharmaceutical therapy

European Journal of Nuclear Medicine and Molecular Imaging > Ausgabe 12/2019
Sangeeta Ray Banerjee, Vivek Kumar, Ala Lisok, Jian Chen, Il Minn, Mary Brummet, Srikanth Boinapally, Michael Cole, Ethel Ngen, Bryan Wharram, Cory Brayton, Robert F. Hobbs, Martin G. Pomper
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Electronic supplementary material

The online version of this article (https://​doi.​org/​10.​1007/​s00259-019-04434-0) contains supplementary material, which is available to authorized users.
This article is part of the Topical Collection on Oncology – Genitourinary

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To develop a prostate-specific membrane antigen (PSMA)-targeted radiotherapeutic for metastatic castration-resistant prostate cancer (mCRPC) with optimized efficacy and minimized toxicity employing the β-particle radiation of 177Lu.


We synthesized 14 new PSMA-targeted, 177Lu-labeled radioligands (177Lu-L1–177Lu-L14) using different chelating agents and linkers. We evaluated them in vitro using human prostate cancer PSMA(+) PC3 PIP and PSMA(−) PC3 flu cells and in corresponding flank tumor models. Efficacy and toxicity after 8 weeks were evaluated at a single administration of 111 MBq for 177Lu-L1, 177Lu-L3, 177Lu-L5 and 177Lu-PSMA-617. Efficacy of 177Lu-L1 was further investigated using different doses, and long-term toxicity was determined in healthy immunocompetent mice.


Radioligands were produced in high radiochemical yield and purity. Cell uptake and internalization indicated specific uptake only in PSMA(+) PC3 cells. 177Lu-L1, 177Lu-L3 and 177Lu-L5 demonstrated comparable uptake to 177Lu-PSMA-617 and 177Lu-PSMA-I&T in PSMA-expressing tumors up to 72 h post-injection. 177Lu-L1, 177Lu-L3 and 177Lu-L5 also demonstrated efficient tumor regression at 8 weeks. 177Lu-L1 enabled the highest survival rate. Necropsy studies of the treated group at 8 weeks revealed subacute damage to lacrimal glands and testes. No radiation nephropathy was observed 1 year post-treatment in healthy mice receiving 111 MBq of 177Lu-L1, most likely related to the fast renal clearance of this agent.


177Lu-L1 is a viable clinical candidate for radionuclide therapy of PSMA-expressing malignancies because of its high tumor-targeting ability and low off-target radiotoxic effects.

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