Tracers / [177Lu]Lu-DOTATATE

[177Lu]Lu-DOTATATE

Also written as 177Lu-DOTA-TATE; [177Lu]Lu-DOTA-TATE; [177Lu]Lu-DOTATATE; [Lu-177]Lu-DOTATATE; DOTA-TATE; lutetium (177Lu) oxodotreotide
Radionuclide
Lu-177 t½ 9585 min
Modality
Therapy
Production route
Stage
approved (FDA-approved)
Syntheses indexed
77

What it is

Compound class
DOTA-conjugated somatostatin analogue (radiolabelled peptide, octreotate)
Target / mechanism
Targets somatostatin receptor subtype 2 (SSTR2) PMID 39142827
Clinical application
Peptide receptor radionuclide therapy (PRRT) for somatostatin receptor-positive tumours, including neuroendocrine tumours and meningiomas PMID 40177560
Theranostic pair
<a href="/tracers/ga68-dotatate/">ga68-dotatate</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-TATE
ABX
27090254
2016 EJNMMI Res
177Lu-radiolabelling was performed using the cassette-based ModularLab PharmTracer® synthesizer (EZAG, Berlin, Germany)
Modular-Lab PharmTracer
Eckert & Ziegler
vendor cassetteSPE80%99.8 ± 0.05% (ITLC); 97.3 ± 1.5% (HPLC)DOTA-(Tyr3)-octreotate
AUSPEP
27408890
2015 Asia Ocean J Nucl Med Biol
Eckert & Ziegler Eurotope’s Modular-Lab Pharm Tracer® automated synthesis system — an estimate of 80% synthesis yield
Manual synthesisDOTATATE
Bachem, Bubendorf, Switzerland
42518020
2026 EJNMMI Res
[177Lu]Lu-DOTATATE was radiolabelled as previously described by Lundsten et al. [28], using the same conditions as mentioned above.
Kit-based preparation
Novartis
42514966
2026 Pharmaceutics
177Lu-DOTATATE (Lutathera®, Novartis, Basel, Switzerland)
42454478
2026 Endocr Relat Cancer
42198448
2026 Pharmaceuticals (Basel)
42177732
2026 EJNMMI Phys
42149369
2026 Ann Nucl Med
42141279
2026 Eur J Nucl Med Mol Imaging
41937276
2026 Med Phys
41887730
2026 J Nucl Med
41806239
2026 Clin Transl Oncol
41798196
2026 Front Endocrinol (Lausanne)
Kit-based preparationDOTATATE (octreotate)41710577
2026 Drug Des Devel Ther
The peptide is conjugated via a DOTA chelator, which securely coordinates the β-emitter radioactive isotope lutetium-177
41693498
2026 Nucl Med Commun
Kit-based preparation41610875
2026 Nuklearmedizin
In-house preparations (using GMP-grade kits and in-house radiolabelling)
DOTATATE41356201
2026 Theranostics
41355961
2026 Theranostics
41342316
2026 Chembiochem
41117982
2026 Eur J Nucl Med Mol Imaging
41083371
2026 Endocr J
40970962
2026 Eur J Nucl Med Mol Imaging
iPHASE MultiSyn
iPHASE Technologies
vendor cassette98 ± 3%
no
95.2 ± 1.3% (0h HPLC)DOTA-TATE
Huayi
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%. — The yield for this radiopharmaceutical was 98 ± 3%.
40634058
2025 Endocr J
40598690
2025 Cancer Imaging
40455253
2025 Eur J Nucl Med Mol Imaging
Kit-based preparation
Advanced Accelerator Applications
40361351
2025 Cancers (Basel)
Lutathera® was obtained commercially from Advanced Accelerator Applications, a Novartis Company (Colleretto Giacosa, Italy).
40302310
2025 J Neuroendocrinol
40186742
2025 Ann Nucl Med
Manual synthesisDOTATATE40177560
2025 Acta Pharm Sin B
177Lu-DOTATATE and 177Lu-EB-TATE were radiolabeled using the same method.
Manual synthesismore than 95%DOTATATE
AUSPEP
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
39351526
2024 Front Endocrinol (Lausanne)
Manual synthesisHPLC>96 %DOTA-TATE
Bachem, Bubendorf, Switzerland
39310112
2024 Theranostics
Radiolabeling with lutetium‑177 and copper‑67 was performed in sodium ascorbate buffer (0.15 mol/L, pH 4.8) for 40 min, at 80 °C and 40 °C, respectively.
DOTATATE39142827
2024 J Nucl Med
Manual synthesisnone>98%DOTATATE
Bachem, Bubendorf, Switzerland
39046521
2024 Eur J Nucl Med Mol Imaging
DOTA-LM3 (CSBio, Silicon Valley Menlo Park, California, United States) and DOTATATE (Bachem, Bubendorf, Switzerland) were labeled with terbium-161 or lutetium-177 at a molar activity of up to 100 MBq/nmol using standard labeling conditions as previously reported
38929531
2024 Medicina (Kaunas)
38324106
2024 Endocrine
38250038
2024 Theranostics
above 97%above 90%DOTA-TATE
Bachem, Bubendorf, Switzerland
36145306
2022 Pharmaceuticals (Basel)
35450421
2022 Front Endocrinol (Lausanne)
34475242
2021 J Nucl Med
33916707
2021 Cancers (Basel)
33037092
2020 J Nucl Med
30854332
2019 Front Oncol
Modular-Lab PharmTracer
Eckert & Ziegler
vendor cassetteSPEDOTA-TATE
ABX
27090254
2016 EJNMMI Res
177Lu-radiolabelling was performed using the cassette-based ModularLab PharmTracer® synthesizer (EZAG, Berlin, Germany)
98%DOTA-TATE40425733
2026 Nat Protoc
41006727
2025 Med Oncol
more than 99%DOTATATE26443981
2016 Nucl Med Commun
novel, self-shielded modular radiosynthesis system for fully automated preparation of PET and therapeutic radiopharmaceuticals
>99%>99%22149590
2012 Cancer Biother Radiopharm
reprogramming and adaptation of a commercially available synthetic module (IBA molecular; Synthera®) allowed high yield, fully automated, in-house radiolabeling — (68)Ga-octreotate and (177)Lu-octreotate were synthesized, resulting in both radiochemical yield and radiochemical purity greater than 99%.
42658097
2026 Health Phys
42579511
2026 Endocr Relat Cancer
42573792
2026 Eur J Nucl Med Mol Imaging
42555490
2026 Hell J Nucl Med
42526976
2026 Clin Lab Med
42517999
2026 Ann Nucl Med
42472334
2026 Hell J Nucl Med
42472319
2026 Hell J Nucl Med
42333414
2026 Clin Nucl Med
42302403
2026 Clin Nucl Med
42234009
2026 Eur J Nucl Med Mol Imaging
42169550
2026 Nucl Med Commun
42167802
2026 J Nucl Med
42097922
2026 PET Clin
41978352
2026 Nucl Med Commun
41932368
2026 J Control Release
41536178
2026 Nucl Med Commun
41533312
2026 Jpn J Radiol
41131958
2025 Nucl Med Rev Cent East Eur
40227439
2025 Radiologie (Heidelb)
32414949
2020 J Nucl Med
32293704
2020 Endokrynol Pol
28588150
2018 J Nucl Med
DOTATATE28450554
2017 J Nucl Med
27890514
2017 Rev Esp Med Nucl Imagen Mol
25771364
2016 Curr Radiopharm
21993546
2012 Oncol Rep
19601842
2009 Curr Pharm Des

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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 Lu-177 monograph — base set per Ph. Eur. 0125 + rule-based (see Ga-68 analogue monograph 3050 for the ligand method). Lu-177m content + metal impurities + molar activity + osmolality per rules.

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: Lutathera / [177Lu]Lu-DOTA-TATE. 2 corpus articles with Lu-177 (PMID 35966589, 35906092) were collapsed onto the Ga-68 anchor [68Ga]Ga-DOTATATE. Added as its own row. Theranostic hub: also paired (one-way) from cu64-dotatate, f18-fet-bag-toca -- ga68-dotatate (NETSPOT) is the FDA-approved companion diagnostic for Lu-177-DOTATATE (Lutathera); the other two are additional diagnostics paired with the same therapeutic in the literature. [stage 19] Compound class inferred from precursor name (not stated outright) -- PMID 27408890: 'DOTATATE, or DOTA-(Tyr3)-octreotate (where DOTA = 1,4,7,10-tetraazacyclododecane– 1,4,7, 10-tetraacetic acid) was obtained from Auspep (Melbourne, Australia)'. Stage set/updated at stage 23 from PMID 40696084: 'Lutetium-177 (177Lu) theranostics have revolutionized personalized cancer treatment, particularly with FDA-approved therapies like [177Lu]Lu-DOTA-TATE for neuroendocrine tumors and [177Lu]Lu-PSMA for prostate cancer.'.