Tracers / [225Ac]Ac-PSMA-617

[225Ac]Ac-PSMA-617

Also written as PSMA-617; [Ac-225]Ac-PSMA-617; Ac-225-PSMA-617; Pluvicto
Radionuclide
Ac-225 t½ 14284.8 min
Modality
Therapy
Production route
Stage
investigational
Syntheses indexed
21

What it is

Compound class
PSMA-617 – urea-based PSMA-targeting small molecule (DOTA-conjugated peptidomimetic)
Target / mechanism
Targets prostate-specific membrane antigen (PSMA) PMID 34385780
Clinical application
Targeted alpha therapy for metastatic castration-resistant prostate cancer PMID 32802197
Theranostic pair
<a href="/tracers/in111-psma617/">in111-psma617</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
Manual synthesisSPEabout 45%approximately 95%PSMA-617
Novartis
42159963
2026 EJNMMI Radiopharm Chem
For 225Ac labeling of PSMA-617, 225AcCl3 (0.92 MBq) was added to 0.2 M NH4OAc buffer (pH 5.2, 100 µL) in a 0.5 mL Eppendorf tube (LoBind), followed by the addition of PSMA-617 (1.0 nmol, 1.0 µL). — about 45% for [212Pb]Pb-PSMA-617 and [225Ac]Ac-PSMA-617
41783574
2026 Drug Des Devel Ther
38855174
2024 Theranostics
38773983
2024 Theranostics
PSMA-61738577331
2024 Front Oncol
Manual synthesisPSMA-617 precursor
ABX
37797974
2023 J Nucl Med
Radiolabeling was performed as previously described
PSMA-61735177427
2022 J Nucl Med
Manual synthesisSPE85%–87%97%–99%PSMA-617
ABX
34385780
2021 Indian J Nucl Med
Ac-225 PSMA was prepared by adding the required amount (50–150 μg) of the peptidic precursor (PSMA-617) in 1 ml ascorbate buffer. — the radiopeptide was obtained with an adequate yield of 85%–87%
PSMA-61733778927
2021 Curr Oncol Rep
Manual synthesisPSMA-617
CMR, Center of Molecular Research, Moscow, Russia
32802197
2020 Theranostics
A stock solution of 225AcCl3 in 0.01 M HCl was added to the sodium ascorbate buffer-PSMA-617 mixture and heated at 90 °C for 10 min.
31240331
2019 Eur J Nucl Med Mol Imaging
PSMA-617
ABX
31107537
2019 Mutagenesis
PSMA-617
ABX
30232539
2019 Eur J Nucl Med Mol Imaging
42437859
2026 Discov Oncol
PSMA-61740358362
2025 J Med Chem
38218192
2024 Lancet Oncol
PSMA-61734477385
2021 J Med Chem
>99%98 ± 1%PSMA-61734250876
2022 Curr Radiopharm
PSMA-617 precursor was dissolved in 25 μL metal-free water (0.67 mg/mL) and combined with 500 μL 0.05M Tris buffer, pH 9. — high radiochemical yield (57 ± 3 μCi, >99%)
SPEPSMA-61734053430
2022 Curr Radiopharm
PSMA-617, DOTATATE were radiolabelled with 225Actinium in 0.1 M HCl in the presence of ascorbate buffer solution and passed through the C-18 light cartridge for purification
31601699
2020 J Nucl Med
31101746
2020 J Nucl Med

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Notes

Added at stage 21 from therapy-discovered.xlsx (bulk PubMed search by isotope/therapy-type/known-agent, not individually researched yet) -- 35 articles found. Target/mechanism, clinical application, indications, approval and precursor fields still need per-agent research and are intentionally left empty. Diagnostic pair signal at discovery: YES - Ga-68, In-111. Compound class inferred from precursor name (not stated outright) -- PMID 42159963: 'PSMA-617 (1.0 nmol, 1.0 µL)'. Stage set/updated at stage 23 from PMID 38773983: 'At the forefront of clinical trials with 225Ac in PCa are PSMA-targeted TAT agents, notably [225Ac]Ac-PSMA-617, [225Ac]Ac-PSMA-I&T and [225Ac]Ac-J591.'.