Tracers / [177Lu]Lu-DOTA-TOC

[177Lu]Lu-DOTA-TOC

Also written as [177Lu]Lu-DOTATOC; [Lu-177]Lu-DOTATOC; DOTA-TOC; DOTATOC; edotreotide; Lu-177 DOTATOC
Radionuclide
Lu-177 t½ 9585 min
Modality
Therapy
Production route
Stage
Syntheses indexed
28

What it is

Compound class
DOTA-conjugated somatostatin analog peptide (DOTA-TOC)
Target / mechanism
Somatostatin receptor (SSTR) targeting agonist PMID 32859703
Clinical application
Peptide receptor radionuclide therapy (PRRT) for neuroendocrine tumors PMID 40148509
Theranostic pair
<a href="/tracers/ga68-dotatoc/">ga68-dotatoc</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 EAZY
Eckert & Ziegler
vendor cassettenone93.4 ± 3.999.7 ± 0.2 (radio-HPLC)DOTA-TOC
ABX
37233924
2023 EJNMMI Radiopharm Chem
ModularLab EAZY (Eckert & Ziegler Eurotope GmbH, Berlin, Germany) — we achieved an improved balanced radiochemical yield of 93.4 ± 3.9% with a decreased precursor load of 10–17 µg
Manual synthesiscustom manifoldnone98.3 ± 0.6%>99% TLC, >97% HPLCDOTATOC
Gamma Servizi s.r.l., Pavia, Italy
29097938
2017 Contrast Media Mol Imaging
a manually assembled system consisting of tubes, valves, and syringes — 98.3 ± 0.6% (n = 43) for ... 177Lu-DOTATOC
ADD-2
Amercare
custom manifoldnone90.8 ± 8.3%>98%DOTATOC
Gamma Servizi s.r.l., Pavia, Italy
29097938
2017 Contrast Media Mol Imaging
The radiolabelling was performed by using an ADD-2 (Amercare, Thame, UK), a prototype of a semiautomatic dose dispenser device — 90.8 ± 8.3% (n = 88) for 177Lu-DOTATOC
Modular-Lab EAZY
Eckert & Ziegler
vendor cassetteSPE83.1 ± 5.7%>97%DOTATOC
Gamma Servizi s.r.l., Pavia, Italy
29097938
2017 Contrast Media Mol Imaging
Modular-Lab Eazy automatic synthesizer, disposable cassettes (C0-YDOTAPEP-CM, C0-LUDOTAPEP-CM, C0-YDOTAPSMA-CM, and C0-LUDOTAPSMA-CM), hardware, and reagent kits were supplied by Eckert & Ziegler Eurotope GmbH (Berlin, Germany) — 83.1 ± 5.7% (n = 26) for ... 177Lu-DOTATOC, respectively, were achieved
42073521
2026 Cancers (Basel)
41937276
2026 Med Phys
Kit-based preparation41610875
2026 Nuklearmedizin
In-house preparations (using GMP-grade kits and in-house radiolabelling)
Kit-based preparation
ITM
at least 95%DOTATOC41381241
2026 J Nucl Med
[177Lu]Lu-DOTATOC was produced in a kit-labeling procedure, by adding 240 µg of DOTATOC dissolved in sodium ascorbate buffer (pH 5) to a vial containing 1 GBq of no-carrier-added [177Lu]LuCl3 (EndolucinBeta; ITM GmbH), and subsequently heated at 95 °C for 30 min.
DOTATOC41356201
2026 Theranostics
40455253
2025 Eur J Nucl Med Mol Imaging
40186126
2025 BMC Cancer
>95%40148509
2025 Eur J Nucl Med Mol Imaging
Manual synthesismore than 95%DOTATOC
ABX
40147849
2025 J Nucl Med
Radiolabeling of the DOTA compounds was done at 85°C for 25 min, using ascorbic acid buffer and no-carrier-added [177Lu]LuCl3
ITM
>97%39023784
2024 Eur J Nucl Med Mol Imaging
38324106
2024 Endocrine
Modular-Lab EAZY
Eckert & Ziegler
vendor cassettenone93.4 ± 3.999.7 ± 0.2DOTA-TOC
ABX
37233924
2023 EJNMMI Radiopharm Chem
All three radiopharmaceuticals were successfully synthesized in high radiochemical purities and yields on the ML Eazy. — we achieved an improved balanced radiochemical yield of 93.4 ± 3.9% with a decreased precursor load of 10–17 µg
Manual synthesis≥ 98%DOTATOC34625828
2022 Eur J Nucl Med Mol Imaging
Radiolabeling and quality control of the SST analogues were performed as previously reported [43].
Manual synthesisnone>97%DOTA-TOC (50 μg)33452632
2021 Eur J Nucl Med Mol Imaging
the labeling and release procedure was identical for [177Lu]Lu-DOTA-TOC — the radiochemical yield was > 97% in all cases
32859703
2021 J Nucl Med
noneDOTATOC
Perkin Elmer, USA
30939449
2019 Endocr Connect
noneDOTATOC
Perkin Elmer, USA
30939449
2019 Endocr Connect
30854332
2019 Front Oncol
Manual synthesis98.3 ± 0.6>99% TLC, >97% HPLCDOTATOC
Gamma Servizi s.r.l., Pavia, Italy
29097938
2017 Contrast Media Mol Imaging
Manual labelling was carried out using telescopic tongs and dedicated poly(methyl methacrylate) (PMMA) shielding for syringes and vials. — for 177Lu-DOTATOC they were 98.3% ± 0.6
ADD-2
Amercare
custom manifold90.8 ± 8.3>98%DOTATOC
Gamma Servizi s.r.l., Pavia, Italy
29097938
2017 Contrast Media Mol Imaging
The radiolabelling was performed by using an ADD-2 (Amercare, Thame, UK), a prototype of a semiautomatic dose dispenser device — 90.8% ± 8.3, and 83.1 ± 5.7%
Modular-Lab EAZY
Eckert & Ziegler
vendor cassetteSPE83.1 ± 5.7>97%DOTATOC
Gamma Servizi s.r.l., Pavia, Italy
29097938
2017 Contrast Media Mol Imaging
Modular-Lab Eazy automatic synthesizer, disposable cassettes (C0-YDOTAPEP-CM, C0-LUDOTAPEP-CM, C0-YDOTAPSMA-CM, and C0-LUDOTAPSMA-CM), hardware, and reagent kits were supplied by Eckert & Ziegler Eurotope GmbH (Berlin, Germany). — average RCYs of 82.0 ± 8.4% (n = 24) and 83.1 ± 5.7% (n = 26) for 90Y- and 177Lu-DOTATOC, respectively
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
Modular-Lab Eazy automatic synthesizer, disposable cassettes (C0-YDOTAPEP-CM, C0-LUDOTAPEP-CM, C0-YDOTAPSMA-CM, and C0-LUDOTAPSMA-CM), hardware, and reagent kits were supplied by Eckert & Ziegler Eurotope GmbH (Berlin, Germany). — average RCYs of 76.4 ± 2.2% (n = 5) and 90.1 ± 0.8% (n = 5), for yttrium-90 and lutetium-177, respectively, were achieved
42581163
2026 Eur J Nucl Med Mol Imaging
28588150
2018 J Nucl Med

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Quality control Derived from the published synthesis

Ph. Eur. monograph
USP monograph
AppearancepHRCP HPLCHPLC UVRadionuclidic (HPGe)Half-lifeActivityEndotoxins (LAL)SterilityFilter integrityOsmolalityMolar activityMetal impuritiesLu-177m
How this set was arrived at. base set per Ph. Eur. general monograph 0125 (rule); radiometal tracer -> metal impurities (rule); Lu-177 preparation -> Lu-177m content (rule); therapeutic radiopharmaceutical -> osmolality (rule); 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

Added from reverse module search (stage 6); 3 article(s) with Lu-177. Compound class inferred from precursor name (not stated outright) -- PMID 37233924: 'DOTA-TOC (GMP quality, product no. 9702) was purchased from ABX, Radeberg, Germany'. | Stage 28: added indication(s) onc-ppgl from consolidated missing-rubric review.