DOTA-EB-TATE
Octreotate with an albumin-grabbing dye, built to stay in the blood and the tumour longer
DOTA-EB-TATE is lutetium-177 dotatate's peptide with an extra piece: a fragment of Evans blue, a dye that clings to albumin in the blood. The drug therefore circulates for longer and more of it reaches neuroendocrine tumours, at lower activities than standard treatment. The trade-off seen in patients is a higher dose to the kidneys and bone marrow. Studies in China and a phase 1 in the US have tested it; it is investigational.
Used in human trials: About 3.7 GBq, Per cycle, 8-12 weeks apart, Intravenous (Lutetium-177 DOTA-EB-TATE, 30-patient study) Details ↓
Recommended Dosing
Used in human trials
No manufacturer dose exists for this use: these are amounts given in published trials, not recommendations.
What is it?
Lutetium-177 dotatate is an approved treatment for somatostatin receptor-positive neuroendocrine tumours, but it clears from the body quickly, so much of it is excreted before reaching the tumour, and standard treatment needs up to four doses. DOTA-EB-TATE adds a truncated Evans blue molecule to DOTA-octreotate. Evans blue binds albumin loosely, so the drug rides on albumin through the circulation and has more time to reach receptors.
The first human study, in 2018, gave small doses to five patients and compared them with three given lutetium dotatate. The new drug stayed in the blood far longer and delivered 7.9 times the tumour dose per unit of activity. It also gave 3.2 times the kidney dose and 18.2 times the marrow dose. A pilot with a single 0.66 GBq dose showed tumour responses similar to dotatate at about six times the activity.
Dose-escalation studies followed. In 33 patients, single cycles of 1.85 or 3.7 GBq worked better than 1.11 GBq, and severe blood toxicity appeared only in two patients at the top dose who had had chemotherapy before. With up to three cycles, 1.89 and 3.97 GBq per cycle were tolerated and effective. In 30 patients treated at about 3.7 GBq for up to three cycles and followed a median 46 months, disease control was 85.2% by RECIST, median progression-free survival was 36 months, and no one developed leukaemia, myelodysplasia or kidney damage. A small randomised crossover study found that the usual amino acid infusion to protect the kidneys made no significant difference to kidney dose.
Results outside China are more cautious. An intraindividual comparison in five patients found higher tumour doses than with lutetium DOTATOC in four, but higher kidney, spleen and liver doses in all, so the ratio of tumour to critical-organ dose favoured DOTATOC in four of five. A 2026 US phase 1 in six patients found febrile neutropenia at 3.7 GBq and set the recommended phase 2 activity at 1.85 GBq per cycle for two cycles, with the marrow as the dose-limiting organ.
A modified version with a polyethylene glycol link, LNC1010, is being developed separately. DOTA-EB-TATE itself has no FDA or EMA approval and is given only in nuclear-medicine departments within studies.
Mechanism of Action
Two parts work together: the peptide finds the receptor and the dye keeps the drug in circulation long enough to get there.
Somatostatin receptor 2 agonist
The octreotate part binds the receptor and is internalised, like lutetium dotatate (2018 study).
Albumin binding
Evans blue binds albumin reversibly, extending time in blood and raising tumour dose 7.9-fold in the first patients (2018 study).
Lutetium-177 radiation
Beta radiation from lutetium-177 treats the tumour at lower injected activity than standard dotatate (2020 study).
Marrow and kidney exposure
Longer circulation also raises marrow and kidney doses; marrow was dose-limiting in the US phase 1 (2026 study).
Published Research
These studies were read from their PubMed abstracts on October 29, 2026: eight in patients and two in mice. The copper-67 version in mice is the same DOTA-EB-TATE molecule with another metal.
First in humans: dosimetry
Five patients received 0.35-0.70 GBq and three received lutetium-177 DOTATATE. It was well tolerated, stayed longer in blood and gave 7.9 times the tumour dose. Kidney and marrow doses were 3.2 and 18.2 times higher. Whole-body effective doses were similar (0.205 vs 0.174 mSv per MBq).
Single low-dose treatment pilot
Four patients got one 0.66 GBq dose and three controls got about 3.98 GBq of lutetium dotatate. All four tolerated it and had symptom relief; 72.5% of tumours over 2 cm shrank in uptake by more than 15%. Change in comparable tumours did not differ from dotatate at about one sixth of the activity.
Dose escalation in 33 patients
Groups received about 1.11, 1.85 or 3.7 GBq once, with a dotatate control group. No grade 3-4 toxicity occurred except grade 3 blood toxicity in two previously chemotherapy-treated patients at 3.7 GBq. Partial response rates were 0%, 50% and 50% against 16.7% for dotatate.
Multiple cycles at escalating doses
Thirty-two patients were randomised to 1.17, 1.89 or 3.97 GBq per cycle for up to three cycles. There were no grade 4 events; grade 3 low platelets occurred in one patient in the middle group and three in the top group. Disease control was 66.7%, 83.3% and 71.5%, and no kidney toxicity was seen.
30 patients, long follow-up
Three planned cycles of about 3.7 GBq, 8-12 weeks apart. Grade 3 low platelets in 13.3%, no grade 4 toxicity, no kidney damage and no leukaemia or myelodysplasia over a median 46 months. Response rate 33.3% and disease control 85.2% by RECIST; median progression-free survival 36 months.
Is the kidney-protecting infusion needed?
Ten patients had two 3.7 GBq cycles, one with and one without amino acid infusion, in random order. Kidney effective dose and residence time did not differ significantly, kidney function did not change and no nephrotoxicity was recorded; one patient had grade 3 low platelets.
Compared with lutetium-177 DOTATOC
In five patients given both drugs, tumour dose per activity was higher with DOTA-EB-TATE in four (median 1.7 times), but kidney (3.2 times) and spleen doses were higher in all. The tumour-to-organ ratio favoured DOTATOC in four of five, so the authors advised judging each patient individually.
US phase 1 dose escalation
Six adults with grade 2-3 gastroenteropancreatic tumours received 1.85, 3.70 or 5.55 GBq for two cycles six weeks apart. Kidney dose was a median 4.8 Gy per cycle without kidney toxicity. Febrile neutropenia at 3.7 GBq made the marrow dose-limiting; 1.85 GBq was recommended for phase 2. One partial response and five stable disease at 3 months.
Thyroid cancer models
Alongside receptor staining of 92 thyroid cancers and gallium-68 DOTATATE scans in 25 patients, mouse studies showed DOTA-EB-TATE reached tumours more than DOTA-TATE or DOTA-JR11. Treatment extended survival in a high-receptor model but did nothing in a low-receptor model.
Copper-67 version in mice
Copper-67 DOTA-EB-TATE showed tumour-specific, prolonged uptake on SPECT and projected human effective doses of 0.066-0.085 mSv per MBq. Two 15 MBq doses cleared small tumours in 60% of mice against 20% with the lutetium version; survival was similar.
Dosing Data
DOTA-EB-TATE has no approved label. It is dosed by radioactivity; the rows below are the activities in the carded human studies.
Educational information, not medical advice. Each dose above is tagged with its source: an approved label, a published human study, animal data, or amounts reported by users. None is a recommendation for you. An unapproved compound has no established safe or effective human dose, and products sold for “research use only” are not made or tested for people. Talk to a doctor before acting on anything on this site, including before you start, stop or change any medicine or dose. Full medical disclaimer.
What a Buyer Needs to Know
What is sold, how it is mixed, stored and taken, and what is known about its safety, quality and legal status. Each part names its source. Where we have none, it says unknown.
What is sold
Unknown: we hold no regulator's label that says in what form DOTA-EB-TATE is supplied. It is a radioactive drug: the next part says where it is prepared and given.
Mixing a vial: a worked example
Nothing to mix at home, and no syringe units to work out: DOTA-EB-TATE is a radioactive drug, prepared and given in nuclear-medicine departments, and its dose is an amount of radioactivity (MBq or GBq), not a weight.
This page's dosing note: “The drug is labelled in a hospital radiopharmacy and given by radioactivity; no reconstitution maths applies.”
Source: this page's own note in Dosing Data below; the amount of each dose row in Dosing Data below.
Storage before and after mixing
Unknown: no label on file says how DOTA-EB-TATE is stored. It is a radioactive drug held by the nuclear-medicine department that prepares and gives it (see the part above); the home rules for a mixed vial in the mixing guide do not apply to it.
How it is taken
As it was given in human studies: Intravenous (Per cycle, 8-12 weeks apart; Lutetium-177 DOTA-EB-TATE, 30-patient study).
Source: Used in human trials: the route and frequency of each row in Dosing Data below.
What to expect, and when
How long it stays in the body: not established by a measurement cited on this entry.
How long the doses were given: Lutetium-177 DOTA-EB-TATE, 30-patient study: Up to 3 cycles; Lutetium-177 DOTA-EB-TATE, US phase 1 recommended phase 2 activity: 2 cycles; Lutetium-177 DOTA-EB-TATE, escalation with multiple cycles: Up to 3 cycles.
When effects appear: unknown; no source on this page gives a time to effect for DOTA-EB-TATE. Results reported in the studies are under Published Research.
Source: Used in human trials, the duration of each row in Dosing Data below.
Side effects, and when to stop or get help
From the Side Effects section: Low platelets, the most common severe effect (grade 3 in 13.3% of 30 patients); Febrile neutropenia at 3.7 GBq in the US phase 1, which made marrow the dose-limiting organ; Nausea, fatigue and hair loss (US phase 1); No kidney toxicity reported in the Chinese studies or the US phase 1, despite higher kidney doses. Full list and cautions ↓
When to stop or get help: unknown; no label or trial on file sets rules for stopping DOTA-EB-TATE. Treat a severe or unexpected reaction as a reason to stop and see a doctor.
Source: the Side Effects section below (“From the human studies above”).
Interactions
Unknown: a PubMed search for human interaction studies of DOTA-EB-TATE (reviewed 2026-10-28) found none. Unknown is not the same as safe to combine.
Every peptide's record, with its source: the interaction matrix.
Checking what you bought
Unknown: no published independent test of DOTA-EB-TATE products is in our lab-results database yet, so how products sold under this name measure up is not known.
To read a certificate of analysis, paste it into the COA decoder; it checks the measured mass against DOTA-EB-TATE's expected mass, 2,329.6 Da, from this entry's molecular data. Trust & Verification explains what independent testing can and cannot show.
Legal status
US: In Clinical Trials (Not approved: Drugs@FDA and the EMA medicines list hold no record (searched October 28, 2026)). Sport: Prohibited (S0 catch-all).
Country by country ↓ · Regulatory tracker
Source: this entry's approval status and the WADA Prohibited List, as in Legal Status below.
Side Effects & Contraindications
Reported Side Effects
From the human studies above.
Contraindications & Cautions
No approved label exists, so there are no official contraindications. Points from the studies:
Legal Status
DOTA-EB-TATE is investigational in every jurisdiction checked.
Frequently Asked Questions
?What is DOTA-EB-TATE?
DOTA-octreotate with an Evans blue albumin binder, labelled with lutetium-177 to treat neuroendocrine tumours.
?Why add Evans blue?
It makes the drug ride on albumin, so it stays in the blood longer and more reaches the tumour. Marrow and kidneys also get more radiation.
?How does it compare with lutetium-177 dotatate?
Early studies found similar or better responses at lower activities. An intraindividual comparison found tumour-to-organ dose ratios mostly favoured the standard agonist. There is no large randomised trial.
?Is it approved?
No. It is investigational.
References
- [other] PubChem CID 175678582, DOTA-EB-TATE: formula C105H133N21O30S5, molecular weight 2329.6. Read October 28, 2026. https://pubchem.ncbi.nlm.nih.gov/compound/175678582
- [registry] ClinicalTrials.gov API v2, read October 28, 2026: NCT05475210 (phase 1, completed); NCT03478358 and NCT03308682 (phase 1).
- [clinical-trial] Zhang J, et al. "Safety, Pharmacokinetics, and Dosimetry of a Long-Acting Radiolabeled Somatostatin Analog (177)Lu-DOTA-EB-TATE in Patients with Advanced Metastatic Neuroendocrine Tumors." J Nucl Med, 2018;59(11):1699-1705. PMID: 29653971.
- [clinical-trial] Wang H, et al. "Response to Single Low-dose (177)Lu-DOTA-EB-TATE Treatment in Patients with Advanced Neuroendocrine Neoplasm: A Prospective Pilot Study." Theranostics, 2018;8(12):3308-3316. PMID: 29930731.
- [clinical-trial] Liu Q, et al. "Dose escalation of an Evans blue-modified radiolabeled somatostatin analog (177)Lu-DOTA-EB-TATE in the treatment of metastatic neuroendocrine tumors." Eur J Nucl Med Mol Imaging, 2020;47(4):947-957. PMID: 31832728.
- [clinical-trial] Liu Q, et al. "Peptide Receptor Radionuclide Therapy of Late-Stage Neuroendocrine Tumor Patients with Multiple Cycles of (177)Lu-DOTA-EB-TATE." J Nucl Med, 2021;62(3):386-392. PMID: 32826319.
- [clinical-trial] Jiang Y, et al. "Safety and efficacy of peptide receptor radionuclide therapy with (177)Lu-DOTA-EB-TATE in patients with metastatic neuroendocrine tumors." Theranostics, 2022;12(15):6437-6445. PMID: 36185603.
- [clinical-trial] Jiang Y, et al. "Evaluation of Safety, Biodistribution, and Dosimetry of a Long-Acting Radiolabeled Somatostatin Analog 177 Lu-DOTA-EB-TATE With and Without Amino Acid Infusion." Clin Nucl Med, 2023;48(6):e289-e293. PMID: 37075254.
- [pubmed] Hänscheid H, et al. "Intraindividual comparison of [(177)Lu]Lu-DOTA-EB-TATE and [(177)Lu]Lu-DOTA-TOC." Eur J Nucl Med Mol Imaging, 2021;48(8):2566-2572. PMID: 33452632.
- [clinical-trial] Bodei L, et al. "Next-Generation Peptide Receptor Radionuclide Therapy: A Phase 1 Dose-Escalation and Dosimetry Study of (177)Lu-DOTA-EB-TATE." J Nucl Med, 2026. PMID: 42785949.
- [pubmed] Thakur S, et al. "(177)Lu-DOTA-EB-TATE, a Radiolabeled Analogue of Somatostatin Receptor Type 2, for the Imaging and Treatment of Thyroid Cancer." Clin Cancer Res, 2021;27(5):1399-1409. PMID: 33355247.
- [pubmed] Njotu FN, et al. "Efficacy of [(67)Cu]Cu-EB-TATE Theranostic Against Somatostatin Receptor Subtype-2-Positive Neuroendocrine Tumors." J Nucl Med, 2024;65(4):533-539. PMID: 38485273.
- [pubmed] Guo W, et al. "Safety, dosimetry, and efficacy of an optimized long-acting somatostatin analog for peptide receptor radionuclide therapy in metastatic neuroendocrine tumors: From preclinical testing to first-in-human study." Acta Pharm Sin B, 2025;15(2):707-721. PMID: 40177560.
Sources & Citations
Studies were read from their PubMed records on October 29, 2026. Regulatory status comes from Drugs@FDA and the EMA medicines list (searched October 28, 2026) and trial listings from ClinicalTrials.gov (October 29, 2026). Grey Peptides sells nothing and links to no vendor.
Medical Disclaimer: This content is for educational and informational purposes only. It is not medical advice, and nothing here is an instruction to obtain or use any compound. Talk to a licensed clinician about your own situation.