Tracers / [177Lu]Lu-PSMA-617

[177Lu]Lu-PSMA-617

Also written as 177Lu-PSMA-617; [177Lu]Lu-PSMA-617; [177Lu]Lu-PSMA617; [Lu-177]Lu-PSMA-617; Lu-177 PSMA-617; lutetium (177Lu) vipivotide tetraxetan; PSMA-617
Radionuclide
Lu-177 t½ 9585 min
Modality
Therapy
Production route
Stage
approved
Syntheses indexed
96

What it is

Compound class
PSMA-617 (DOTA-conjugated urea-based PSMA-targeting small molecule ligand)
Target / mechanism
Targets prostate-specific membrane antigen (PSMA); binding results in internalisation and delivery of β-radiation into PSMA-expressing cancer cells PMID 37284895
Clinical application
PSMA-targeted radioligand therapy for metastatic castration-resistant prostate cancer PMID 38725500
Theranostic pair
<a href="/tracers/ga68-psma11/">ga68-psma11</a>

Regulatory status

FDA
EMA (centralised)
Other approvals
Brand names

Clinical use

Typical injected activity
Uptake time

Reported in the literature. Not a dosing recommendation.

Published syntheses

ModuleCassettePurificationYield %RCP %Precursor / supplierSource
Modular-Lab PharmTracer
Eckert & Ziegler
vendor cassetteSPEDOTA-PSMA
ABX
27090254
2016 EJNMMI Res
177Lu-radiolabelling was performed using the cassette-based ModularLab PharmTracer® synthesizer (EZAG, Berlin, Germany)
Scintomics GRP / GRP-3V
Scintomics
vendor cassettenone>90 %92 %PSMA-617
ABX
27090254
2016 EJNMMI Res
Both kinds of synthesis was carried out with a Scintomics GRP synthesizer, sterile single use cassettes and the standard synthesis sequences for 68Ga-peptides respective therapeutic peptides. — The labelling to 177Lu-PSMA-617 was quantitative, there for the yield was >90 %
iPHASE MultiSyn
iPHASE Technologies
vendor cassettenone91 ± 4
yes
96.6 ± 0.7PSMA-617
ABX
33067810
2021 J Labelled Comp Radiopharm
iPHASE MultiSyn module — Formulated and sterile radiopharmaceuticals were obtained in 76 ± 3% (n = 20) and 91 ± 4% (n = 15) radiochemical yields after 17 and 20 min, respectively.
9931891883
2020 Nucl Med Biol
Elysia-Raytest
vendor cassettenone>96%
no
>95%PSMA-617 (vipovitide tetraxetan)
MedChemExpress
42287471
2026 EJNMMI Radiopharm Chem
Radiopharmaceutical [177Lu]Lu-PSMA-617 was synthetized by the Gaia&Luna module (Elysia Raytest, Germany). — The radiopharmaceutical was obtained with > 95% radiochemical purity and > 96% radiochemical yield.
40638023
2025 Ann Nucl Med
>95%PSMA-617
MedChemExpress
36145382
2022 Pharmaceuticals (Basel)
41026359
2025 Int J Clin Oncol
39293462
2024 Lancet
40580320
2025 Eur J Nucl Med Mol Imaging
Modular-Lab EAZY
Eckert & Ziegler
vendor cassetteSPE90.1 ± 0.8%>99% TLC, >98% HPLCPSMA-617
Gamma Servizi s.r.l., Pavia, Italy
29097938
2017 Contrast Media Mol Imaging
The ML Eazy system was also tested to prepare 90Y- and 177Lu-PSMA-617 — 90.1 ± 0.8% (n = 5), for yttrium-90 and lutetium-177, respectively, were achieved
Manual synthesisSPE72 ± 6%
no
>95%PSMA-617
MedChemExpress
42654126
2026 Pharmaceutics
PSMA-617 (10 mM in DMSO), sodium acetate (0.4 M, pH 5.5), 20% ascorbic acid solution, and approximately 185-370 MBq of 177Lu-LuCl3 ... were combined in a reaction vial, and incubated at 95 °C for 60 min. — The non-decay-corrected radiochemical yield was 72 ± 6%
Elysia-Raytest
vendor cassettenone>96%
no
>95%PSMA-617 (vipovitide tetraxetan)
MedChemExpress
42287471
2026 EJNMMI Radiopharm Chem
Radiopharmaceutical [177Lu]Lu-PSMA-617 was synthetized by the Gaia&Luna module (Elysia Raytest, Germany). — The radiopharmaceutical was obtained with > 95% radiochemical purity and > 96% radiochemical yield.
Kit-based preparation95.642287471
2026 EJNMMI Radiopharm Chem
reference product (Pluvicto®)
Manual synthesisDOTA-PSMA-617
ABX
42274762
2026 Eur J Nucl Med Mol Imaging
radiolabeling was performed in-house
Kit-based preparation
Novartis
Novartis
42201380
2026 Eur J Nucl Med Mol Imaging
[177Lu]Lu-PSMA-617 (Pluvicto™, Novartis) was administered intravenously
Manual synthesisSPE>95%>98%PSMA-617
Novartis
42159963
2026 EJNMMI Radiopharm Chem
In a 1.5 mL protein Eppendorf tube (LoBind®), approximately 37.0 MBq of 177LuCl3 in 0.25 M NaOAc buffer (pH 5.5, 100 µL) or 18.5 MBq of 212PbCl2 in 0.2 M NaOAc buffer (pH 5.5, 100 µL) was mixed with PSMA-617 (1.0 nmol, 1.0 µL). — isolated radiochemical yield of > 95% for [177Lu]Lu-PSMA-617
42138316
2026 Clin Transl Sci
42013849
2026 Cell Rep Med
41993992
2026 Front Endocrinol (Lausanne)
41856667
2026 J Nucl Med
41819830
2026 J Nucl Med
41771032
2026 Clin Nucl Med
41748296
2026 J Nucl Med
41679922
2026 J Nucl Med
Kit-based preparation41610875
2026 Nuklearmedizin
In-house preparations (using GMP-grade kits and in-house radiolabelling)
41489652
2026 Eur J Nucl Med Mol Imaging
41448174
2026 Med Phys
Manual synthesisPSMA-61741407974
2026 Eur J Nucl Med Mol Imaging
37–187 MBq of 177LuCl3 was mixed with 10 µL of 0.5 M NaOAc (pH = 5.5) and incubated with AP-01 or PSMA-617 (10–20 µg) at 90 °C for 20 min, respectively
Kit-based preparation
Novartis
PSMA-617
Novartis
40897948
2025 Mol Imaging Biol
[177Lu]Lu-PSMA-1-DOTA was labeled by 3D Imaging, LCC with clinical grade [177Lu]Lu-PSMA-617 (Pluvicto, Novartis) used as positive control for RLT.
40724999
2025 Int J Mol Sci
iPHASE MultiSyn
iPHASE Technologies
vendor cassette99 ± 5%
no
95.8 ± 1.6% (0h HPLC)PSMA-617
ABX
40696084
2025 EJNMMI Radiopharm Chem
This process was automated using an iPHASE MultiSyn radiochemistry module with sterile kits affording sterile and apyrogenic 177Lu-labeled radiopharmaceuticals in non-decay corrected yields > 95%. — yielding 99 ± 5%.
40638023
2025 Ann Nucl Med
Manual synthesisPSMA-617 precursor
MedChemExpress
40049746
2025 J Nucl Med
All radiopharmaceuticals were radiolabeled, formulated, and quality-controlled using optimized versions of previously described methods (15).
Manual synthesisSPE99.5 ± 0.5%>97%PSMA-617
Jenguro Ltd., Moscow, Russia
39771514
2024 Pharmaceutics
The synthesis was carried out in Eppendorf Safe-Lock tubes (1.5, 2.0, or 5 mL) at temperatures of 24.5 (RT), 50, 75, 82, and 95 °C with Eppendorf ThermoMixer® C (Hamburg, Germany). — a nearly quantitative reaction yield (99.5 ± 0.5%) may be observed after 10 min of incubation even at ambient temperature (RT, 24.5 °C)
Manual synthesis
CEM Corporation
98.1 ± 1.2%≥97.5%PSMA-617
Jenguro Ltd., Moscow, Russia
39771514
2024 Pharmaceutics
For microwave heating, the reaction was performed with a CEM Discover 908005 Microwave Synthesis System in Biotage® Microwave Reaction Vials (Uppsala, Sweden). — radiochemical yields of ~98% were achieved in 1 (98.1 ± 1.2%) and 5 (98.2 ± 1.1%) min at sodium acetate concentrations of 0.1 and 1.0 mol/L, respectively
39753366
2025 J Nucl Med
Manual synthesisover 90%above 95%PSMA-61739563828
2024 ACS Med Chem Lett
[177Lu]LuCl3, Na–Ac buffer (400 nM), pH = 5.0, 98 °C, 25 min. — radiochemical yield was over 90%
39207485
2024 Eur J Nucl Med Mol Imaging
Manual synthesisnone94.29 ± 0.01%94.29 ± 0.01%PSMA-61739083135
2024 EJNMMI Radiopharm Chem
177Lu-PSMA-617 was prepared by successively adding 177LuCl3 solution (5 µL, 40.7 MBq), PSMA-617 (0.22 mmol/L, 30 µL, 6.7 nmol; prepared in 0.5 M HAc-NaAc buffer, pH 5.2), and gentisic acid (65.00 mmol/L, 40 µL, 2600 nmol) in a reaction flask. — 177Lu-PSMA-61795 ℃5.015 min94.29 ± 0.01%94.29 ± 0.01%
38960712
2024 J Nucl Med
38855174
2024 Theranostics
38760451
2024 Sci Rep
Manual synthesisPSMA-61738725500
2024 Chem Sci
The corresponding DOTA conjugates were labeled with 177Lu (compound 18 and Pluvicto™)
Manual synthesisSPE90%greater than 95%PSMA-61738700450
2024 Adv Healthc Mater
PSMA-617 in water (25 μg per 25 μL) was added to 925 MBq of 177Lu in 250 μL 0.18 M ascorbic acid solution and the solution was shaken at 95 °C for 40 min — The isolated radiochemical yield after cartridge purification was 90%, with greater than 95% purity and molar activity was 41.68 MBq/nmol.
PSMA-61738577331
2024 Front Oncol
37861915
2023 Curr Oncol Rep
Manual synthesisPSMA-617 precursor
ABX
37797974
2023 J Nucl Med
Radiolabeling was performed as previously described
Manual synthesisHPLC+SPEPSMA-61737649602
2023 Theranostics
[177Lu]LuCl3 (~500 MBq in ~15 μL) was added to a solution of the DOTA-conjugated precursor (25 μg) in NaOAc buffer (0.5 mL, 0.1 M, pH 4.5). The mixture was incubated at 90 °C for 15 min
Manual synthesisPSMA-617
ABX
37284895
2023 Naunyn Schmiedebergs Arch Pharmacol
PSMA-617 (60 µg) mixed with 740 µl of gentensic solution (3 mg/ml dissolved in 0.4 M sodium acetate, pH = 4.6) was added to 163 µl of the 177LuCl3 solution. The buffered solution was heated for 20 min at 92 °C and diluted with saline to reach a final activity of 1 GBq/ml.
≥ 97%PSMA-61737246997
2023 Eur J Nucl Med Mol Imaging
36759199
2023 J Nucl Med
HPLCPSMA-61736168623
2022 Theranostics
Scintomics GRP / GRP-3V
Scintomics
vendor cassettenonePSMA-617
ABX
36166155
2022 EJNMMI Radiopharm Chem
[177Lu]Lu-PSMA-I&T and [177Lu]Lu-PSMA-617 was produced with a Scintomics GRP module
Manual synthesisnone≥ 98%PSMA-61735635566
2022 Eur J Nucl Med Mol Imaging
The radiolabeling of the PSMA ligands with lutetium-177 (no-carrier-added; in 0.04 M HCl; ITM Medical Isotopes GmbH, Germany) was performed under standard labeling conditions at pH 4.5 as previously reported
Manual synthesis>95%PSMA-617 precursor35086894
2022 J Nucl Med
177Lu labeling of PSMA ligands according to standard manual procedures resulted in a radiochemical purity of more than 95%
Manual synthesis>98>98PSMA-617
ABX
34932154
2022 Eur J Nucl Med Mol Imaging
For the biodistribution study, 18 µg PSMA ligand (15 nmol PSMA-617, 12 nmol PSMA-I&T) was added to 0.5 M MES buffer, pH 5.5, and 33 MBq [177Lu]LuCl3 — Radiolabeling of PSMA-617 and PSMA-I&T with [177Lu]LuCl3 resulted in radiochemical yield of > 98%
34887335
2022 J Nucl Med
Manual synthesisnone≥ 95%PSMA-61734402925
2022 Eur J Nucl Med Mol Imaging
The radiolabeling of Ibu-DAB-PSMA and PSMA-617 was performed under standard labeling conditions at pH 4.5 using lutetium-177
33840558
2021 Eur Urol
PSMA-61733778927
2021 Curr Oncol Rep
Manual synthesisPSMA-617
ABX
33579037
2021 Biomolecules
Radiolabeling was conducted as previously described by Kratochwil et al. [34]. 1 GBq of non-carrier added Lutetium-177 (ITG GmbH, Garching, Germany), 30–40 MBq/µL, was mixed with 100 µL sterile 0.4 M sodium acetate solution, pH 5.5, and 1.25 µL 20% w/w ascorbic acid solution; thereafter, 2 µL of a 10 mM solution of PSMA-617 (ABX, Radeberg, Germany) was added.
33465252
2021 Prostate
Manual synthesis>95%>90%PSMA-617
Advanced Biochemical Compounds, ABX, Germany
33094433
2021 Eur J Nucl Med Mol Imaging
Labeling of PSMA-617, PSMA-I&T, and JVZ-007 was performed as previously described — For all labelings, the radiochemical yield was > 95% and the radiochemical purity was > 90%.
31940969
2020 Pharmaceuticals (Basel)
Manual synthesis99%31891883
2020 Nucl Med Biol
labeling yield of [177Lu]Lu-PSMA-617 was measured as a function of reaction time by sampling 2 μL crude product (925 kBq/μL) at different time points and spotting on a TLC plate — high labeling efficiency (99%) can be achieved in just 10 min
Manual synthesisHPLC>98%>99%31399803
2019 Eur J Nucl Med Mol Imaging
All compounds were synthesized using solution-phase chemistry based on our well-established methods — All ligands were radiolabeled with 177Lu in high radiochemical yield (> 98%) and purity (> 99%) using both conventional and microwave-assisted methods.
Manual synthesisPSMA-61731107537
2019 Mutagenesis
177Lu labelling of PSMA-617 was performed as described (11).
Modular-Lab PharmTracer
Eckert & Ziegler
vendor cassetteSPEDOTA-PSMA
ABX
27090254
2016 EJNMMI Res
177Lu-radiolabelling was performed using the cassette-based ModularLab PharmTracer® synthesizer (EZAG, Berlin, Germany)
98%PSMA-61740425733
2026 Nat Protoc
41006727
2025 Med Oncol
40908334
2026 Eur J Nucl Med Mol Imaging
42705104
2026 Biomed Pharmacother
42624649
2026 J Nucl Med
42565339
2026 J Med Econ
42561994
2026 Lancet
42509121
2026 Eur Urol Focus
42472416
2026 Ann Biomed Eng
42437859
2026 Discov Oncol
42418373
2026 J Med Chem
PSMA-61742407347
2026 Bioorg Chem
42320339
2026 Cancer Treat Res Commun
42263768
2026 ACS Nano
42156554
2026 Eur J Nucl Med Mol Imaging
PSMA-61742126983
2026 J Med Chem
42049456
2026 J Nucl Med Technol
41986500
2026 Nat Cancer
41849022
2026 Ann Nucl Med
41748297
2026 J Nucl Med
41575546
2026 Eur J Nucl Med Mol Imaging
99%40494649
2025 Mol Pharm
PSMA-61739332777
2024 J Control Release
35895995
2022 Mol Pharm
RIMS-1 was generated using a convergent synthesis employing solid phase peptide and solution chemistries
34714082
2021 Mol Pharm
33581798
2021 Lancet
31227054
2019 Semin Nucl Med

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Quality control Derived from the published synthesis

Ph. Eur. monograph
no specific monograph
USP monograph
not verified — the USP-NF monograph index is subscription-only and no public confirmation was found
AppearancepHRCP HPLCRCP TLCHPLC UVRadionuclidic (HPGe)Half-lifeActivityEndotoxins (LAL)SterilityFilter integrityOsmolalityMolar activityMetal impuritiesLu-177m
How this set was arrived at. No monograph — base set per Ph. Eur. 0125 + rule-based. Lu-177m content + metal impurities + molar activity + osmolality per rules (therapeutic radiometal, saturable target). HPLC essential for radiolysis products (draft note retained).

Tests listed by reference only. Monograph texts are copyrighted and are not reproduced here. How these are derived

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Notes

Stage 8: PSMA-617 radioligand therapy agent. 7 corpus articles with Lu-177 were collapsed onto the In-111 anchor [111In]In-PSMA-617 by the isotope-blind key (PMID 42287471, 41249585, 41026359, 40908334, 39293462, 38512591, 34964165). Added as its own row. Theranostic hub: also paired (one-way) from f18-psma1007, f18-dcfpyl, in111-psma617 -- ga68-psma11 (Locametz/gozetotide) is the FDA-approved companion diagnostic for Lu-177-PSMA-617 (Pluvicto); the other three are additional PSMA-targeting diagnostics used with the same therapeutic in practice, not tracked back here to avoid a many-valued field. [stage 19] Compound class inferred from precursor name (not stated outright) -- PMID 27090254: 'The ligand PSMA-617 was purchased from ABX.'. Stage set/updated at stage 23 from PMID 38725500: 'Pluvicto™ is a PSMA-targeted radioligand therapeutic (RLT) recently approved by the FDA for the treatment of metastatic castration-resistant prostate cancer (2022 FDA marketing authorization).'.