Tracer library / [225Ac]Ac-PSMA-617
Structure of PSMA-617 (unlabelled parent compound, from PubChem)
Unlabelled parent compoundPubChem CID 122706786

[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
Clinical research
Syntheses indexed
5

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
[111In]In-PSMA-617

Published syntheses

ModuleCassettePurificationYield %RCP %Precursor / supplierSource
Manual synthesis—SPE~45%~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
Manual synthesis————PSMA-617 precursor
ABX
37797974
2023 J Nucl Med
Radiolabeling was performed as previously described
Manual synthesis—SPE85%–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%
Manual synthesis
n/a
——>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%)
Manual synthesis
n/a
—SPE——PSMA-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

Clinical literature

Clinical studies in the indexed corpus, ordered by design (multicentre, prospective, retrospective, others, case reports last) and then by year. Titles and links only, as published; this is not a summary of the evidence.

  1. Efficacy and safety of 225Ac-PSMA-617 targeted alpha therapy in metastatic castration-resistant Prostate Cancer patients.
    2020 · Theranostics · Prospective
  2. Outcome and Renal Safety of PSMA-Targeted Radioligand Therapy in mCRPC Patients With Preexisting Impaired Renal Function.
    2025 · Clin Nucl Med · Retrospective
  3. Hematologic toxicity profile and efficacy of [225Ac]Ac-PSMA-617 α-radioligand therapy of patients with extensive skeletal metastases of castration-resistant prostate cancer.
    2022 · Eur J Nucl Med Mol Imaging · Retrospective
  4. Molecular imaging and biochemical response assessment after a single cycle of [225Ac]Ac-PSMA-617/[177Lu]Lu-PSMA-617 tandem therapy in mCRPC patients who have progressed on [177Lu]Lu-PSMA-617 monotherapy.
    2021 · Theranostics · Retrospective
  5. Tumor sink effect in PSMA-targeted theranostics: intra-patient evaluation of a cohort receiving 225Ac/177Lu-PSMA tandem radioligand therapy.
    2025 · Q J Nucl Med Mol Imaging · Clinical study
  6. 68 Ga-Prostate-Specific Membrane Antigen PET/CT in Imaging of Hemangiopericytoma.
    2023 · Clin Nucl Med · Clinical study
  7. mCRPC Patients Receiving 225Ac-PSMA-617 Therapy in the Post-Androgen Deprivation Therapy Setting: Response to Treatment and Survival Analysis.
    2022 · J Nucl Med · Clinical study
  8. Patients Resistant Against PSMA-Targeting α-Radiation Therapy Often Harbor Mutations in DNA Damage-Repair-Associated Genes.
    2020 · J Nucl Med · Clinical study
  9. Predictors of Overall and Disease-Free Survival in Metastatic Castration-Resistant Prostate Cancer Patients Receiving 225Ac-PSMA-617 Radioligand Therapy.
    2020 · J Nucl Med · Clinical study
  10. Correction to: 225Ac-PSMA-617 in chemotherapy-naive patients with advanced prostate cancer: a pilot study.
    2019 · Eur J Nucl Med Mol Imaging · Clinical study
Show all 13 clinical studies
  1. Treatment of brain metastases of castration-resistant prostate cancer with 225Ac-PSMA-617.
    2019 · Eur J Nucl Med Mol Imaging · Clinical study
  2. DNA damage in human whole blood caused by radiopharmaceuticals evaluated by the comet assay.
    2019 · Mutagenesis · Clinical study
  3. 225Ac-PSMA-617 in chemotherapy-naive patients with advanced prostate cancer: a pilot study.
    2019 · Eur J Nucl Med Mol Imaging · Clinical study

Precursor

Common precursor
—
Suppliers seen in the literature
—
Cited suppliers in indexed syntheses
ABX, Novartis
Typical final purification
—

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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.'. | Stage 30 (2026-09-18): Stage was 'investigational'; normalised to 'Clinical research', original wording kept here.
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