Tracers / [68Ga]Ga-PSMA-617

[68Ga]Ga-PSMA-617

Also written as 68Ga-PSMA-617; [68Ga]Ga-PSMA-617; [Ga-68]Ga-PSMA-617; PSMA-617
Radionuclide
Ga-68 t½ 67.71 min
Modality
PET
Production route
Stage
Phase II clinical trial
Syntheses indexed
30

What it is

Compound class
PSMA-targeted urea-based small-molecule inhibitor (PSMA-617)
Target / mechanism
Prostate-specific membrane antigen (PSMA) inhibitor PMID 38424422
Clinical application
PET/CT imaging for staging, restaging and detection of biochemical relapse in prostate cancer PMID 35056066
Theranostic pair

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
Scintomics GRP / GRP-3V
Scintomics
vendor cassetteSPE48 % at EOS (decay corr. 79 %)
yes
96 %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. — 68Ga-PSMA-617 was obtained with a yield of 48 % at EOS (decay corr. 79 %)
GAIA
Elysia-Raytest
vendor cassetteSPE<20% with 20 µg; not explicitly stated with 40 µg97.4% ± 1.1% (TLC); 93.6% ± 0.9% (HPLC)PSMA-617
MedChemExpress
38424422
2024 Curr Radiopharm
A GAIA® synthesis module and a GALLIAD® generator were used. — Initial experiments with the automated method described above involving only 20 µg of PSMA-617 were conducted, and were associated with low RCY (<20%).
Manual synthesiscustom manifoldSPE>95
yes
>99%PSMA-61738512591
2024 EJNMMI Radiopharm Chem
the possibility to perform an organic-solvent-free purification represents a major simplification. — SPE work-up afforded a significantly higher recovery of > 95%
custom manifoldnone≥96%PSMA-617
Jenguro Ltd., Moscow, Russia
42653427
2026 Int J Mol Sci
>95%42304982
2026 Ann Med
iQS-TS
ITG (Isotope Technologies Garching)
SPE80.1 ± 6.55%>99%PSMA-617
Tianjin Hengrui Pharmaceutical Co., Ltd.
42222801
2026 ACS Omega
iQS-theranostics synthesizer (iQS-TS, ITG GmbH, Germany) for automated radiolabeling — yield rates of 77.5 ± 7.23% and 80.1 ± 6.55%, respectively
Manual synthesis>94%>94%PSMA-61741510166
2026 Theranostics
Radiolabeling with [177Lu]Lu3+ was completed by the addition of precursor peptides PS1 - PS11 — radiochemical yields of greater than 94% for the 68Ga-labeled and greater than 96% for the 177Lu-labeled compounds
Manual synthesisPSMA-61741407974
2026 Eur J Nucl Med Mol Imaging
1 mL of 68GaCl3 (187 MBq) was added to 90 µL NaOAc (1.5 M) and reacted with 10 µg AP-01 or PSMA-617 at 100 °C for 10 min to acquire 68Ga-AP-01 and 68Ga-PSMA-617, respectively
Manual synthesisover 90%above 95%PSMA-61739563828
2024 ACS Med Chem Lett
[68Ga]Ga, Hepes buffer (0.25 M), pH = 4.0, 95 °C, 30 min. — radiochemical yield was over 90%
39327017
2024 J Nucl Med
GAIA
Elysia-Raytest
vendor cassetteSPEmean RCP by TLC = 97.4% ± 1.1%; mean RCP by HPLC = 93.6% ± 0.9%PSMA-617
MedChemExpress
38424422
2024 Curr Radiopharm
For [68Ga]Ga-PSMA-617 preparation, the automated sequence described above was used unchanged.
38398552
2024 Molecules
36215569
2023 J Nucl Med
Manual synthesisnone>95%>98%PSMA-61736015144
2022 Pharmaceuticals (Basel)
The radiolabeling was performed by incubating PSMA-617 (20 nmol) with 1–1.2 GBq of 68GaCl3 (adjusted to pH 3.8 with 1 M ammonium acetate buffer, pH 4.5) at 95 °C for 12 min. — This tracer [9] is routinely prepared in our center with a radiochemical yield higher than 95%, as determined by UPLC (Figure S9).
35984529
2022 EJNMMI Res
>97%PSMA-61735056066
2021 Pharmaceuticals (Basel)
Scintomics GRP / GRP-3V
Scintomics
vendor cassetteSPE48 % (decay corr. 79 %)
yes
96 %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. — 68Ga-PSMA-617 was obtained with a yield of 48 % at EOS (decay corr. 79 %)
42624106
2026 Cell Stem Cell
42314598
2026 Bioorg Chem
42308923
2026 Biomed Pharmacother
>99%PSMA-61742300211
2026 Org Biomol Chem
Purified PSMA-617 was radiolabelled with 68Ga in >99% radiochemical purity, confirming chemical integrity.
PSMA-61742262712
2026 Ann Nucl Med
42101325
2026 Mol Pharm
41698561
2026 Pharmacol Res
41656418
2026 Eur J Nucl Med Mol Imaging
41611483
2026 J Nucl Med
PSMA-61741521448
2026 Adv Healthc Mater
40518457
2025 Eur J Nucl Med Mol Imaging
39745526
2025 Eur J Nucl Med Mol Imaging
36811661
2023 Eur J Nucl Med Mol Imaging

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Quality control Derived from the published synthesis

Ph. Eur. monograph
USP monograph
AppearancepHRCP HPLCHPLC UVRadionuclidic (HPGe)Half-lifeActivityEndotoxins (LAL)SterilityFilter integrityMolar activityMetal impuritiesGe-68 breakthrough
How this set was arrived at. base set per Ph. Eur. general monograph 0125 (rule); radiometal tracer -> metal impurities (rule); Ga-68, generator-produced per synthesis data (PMID 27090254) -> Ge-68 breakthrough; receptor ligand with a saturable target -> molar activity (rule)

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: 2 corpus articles with Ga-68 PSMA-617 (PMID 40638023, 40441170) were collapsed onto the In-111 anchor. Added. Compound class inferred from precursor name (not stated outright) -- PMID 38424422: 'PSMA-617'. Stage set/updated at stage 23 from PMID 36215569: 'Comparison of 68Ga-PSMA-617 PET/CT and 68Ga-RM2 PET/CT in Patients with Localized Prostate Cancer Who Are Candidates for Radical Prostatectomy: A Prospective, Single-Arm, Single-Center, Phase II Study.'.