SARTATE
Octreotate in a copper-holding cage: one molecule that can image a tumour with copper-64 and treat it with copper-67
SARTATE joins octreotate, a somatostatin analogue that binds the receptor most neuroendocrine tumours carry, to MeCOSar, a cage-shaped chelator that grips copper very tightly. Because copper has an imaging isotope (copper-64) and a therapy isotope (copper-67), the same molecule can be used to plan a treatment and then to give it. It has been tested in 10 people with neuroendocrine tumours and in a small meningioma study, and in mice. It is not approved.
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Recommended Dosing
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What is it?
Neuroendocrine tumours and meningiomas often carry somatostatin receptor 2. The approved way to image and treat them uses octreotate or octreotide with a DOTA chelator, labelled with gallium-68 for scans and lutetium-177 for therapy, two different metals. Copper offers a matched pair. Copper-64 emits positrons for PET, copper-67 emits beta particles for therapy, and both are chemically identical. The difficulty is that copper tends to leak out of ordinary chelators in the body. MeCOSar, a sarcophagine 'cage', was designed to hold it, and SARTATE is that cage attached to Tyr3-octreotate.
In the 2014 chemistry paper, copper-64 went into SARTATE in about 20 minutes at room temperature at over 99% purity. In mice, tumour uptake two hours after injection was as high as with copper-64 DOTATATE, but at 24 hours SARTATE was still in the tumour while DOTATATE had largely left, and it built up less in the liver and lungs. Copper-67 SARTATE later slowed tumour growth in mice almost as much as lutetium-177 DOTATATE and extended survival equally, and giving the same total activity in two fractions worked better than one.
The first human study gave copper-64 SARTATE to 10 people with neuroendocrine tumours already seen on gallium-68 DOTATATE PET, and scanned them from 30 minutes to 24 hours. Three had mild infusion reactions and none had serious problems. Tumours took up the tracer strongly and kept it, while the liver cleared it, so contrast was best at 24 hours; at 4 hours it found as many lesions as gallium-68 DOTATATE or more, especially in the liver. A meningioma study then imaged five patients with copper-64 SARTATE and treated three with four cycles of copper-67 SARTATE, without serious adverse events, and showed that the two isotopes targeted the tumours almost identically.
That is a small evidence base: 15 patients across two published studies, plus animal work. The authors of the meningioma study say further trials are needed to set the therapeutic dose. The abstracts read do not state the activities given, so this page has no dose rows. SARTATE is prepared in radiopharmacies and given in nuclear-medicine departments within trials; it has no FDA or EMA approval and is not a product for personal use.
At a Glance
Every value in this table is printed from the Grey Peptides dataset, the same record the compound explorer and comparison tool read, so the three can never disagree.
Educational information, not medical advice. The doses on this page come from approved labels, published studies and, where no study exists, 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.
Mechanism of Action
SARTATE carries copper to cells with somatostatin receptor 2. The octreotate part finds the receptor; the cage holds the copper, which is imaged (copper-64) or irradiates the tumour (copper-67).
A cage that keeps copper in
The sarcophagine chelator forms very stable copper complexes, so tracer stayed in tumours at 24 hours and built up less in liver and lungs than copper-64 DOTATATE in mice (2014 study).
SSTR2 targeting
Highly selective for tumour cells carrying somatostatin receptor 2 (2014 study); simulations show its own pattern of contacts with the receptor (2023 study).
Matched imaging and therapy
Copper-64 and copper-67 SARTATE targeted meningiomas almost identically on PET and SPECT in the same patients (2023 study).
Published Research
These are the studies of SARTATE read from their PubMed abstracts on October 29, 2026: two in patients, three in mice, a letter on dosimetry and a computer modelling study. Two records whose titles do not use the name are carded because their abstracts name SARTATE as the agent studied.
First-in-human copper-64 SARTATE PET, 10 patients
Ten people with neuroendocrine tumours were scanned at 30 minutes and 1, 4 and 24 hours. Three had mild infusion-related events. Lesions took up and kept the tracer, the liver cleared over time, and the 24-hour images had the best contrast. At 4 hours it found as many lesions as gallium-68 DOTATATE at 1 hour or more, especially in the liver.
Copper-64 planning and copper-67 therapy in meningioma
Five people with multifocal meningioma had copper-64 SARTATE PET; three then received four cycles of copper-67 SARTATE. No serious adverse events occurred and none stopped treatment. Effective doses were 0.0395 mSv per MBq for copper-64 and 0.0762 for copper-67, highest to the spleen, then kidneys and liver. The two isotopes targeted the tumours almost identically.
Making the conjugate, and mice
The MeCOSar chelator was joined to Tyr3-octreotate and labelled with copper-64 in about 20 minutes at room temperature at over 99% purity. In mice, tumour uptake at 2 hours matched copper-64 DOTATATE, but SARTATE was retained at 24 hours, with less liver and lung uptake; kidney activity cleared by 24 hours.
Copper-67 therapy against lutetium-177 DOTATATE in mice
In mice with rat pancreatic tumours, one 5 MBq dose cut tumour growth by 75% at 7 days, against 89% for lutetium-177 DOTATATE, and both extended survival from 12 to 21 days. Splitting 30 MBq into two doses two weeks apart improved survival over a single dose (47 against 36 days for copper-67 SARTATE).
Neuroblastoma that survives first treatment, in mice
In a mouse model of neuroblastoma spread to the liver, copper-64 SARTATE reached 14.1 to 25.0% of the injected activity per gram in tumours at 24 hours. Copper-67 SARTATE started two weeks after tumour cells were implanted extended survival by about 13 days (30%), but had no clear effect when started at four weeks, when tumours were larger.
Letter: estimating the therapy dose from the scan
A theoretical commentary proposes a shortened equation for estimating the radiation dose of copper-67 SARTATE from the uptake seen on a copper-64 SARTATE scan, for future use in children with neuroblastoma.
Computer simulation of receptor binding
Molecular dynamics simulations of six radiopharmaceuticals bound to somatostatin receptor 2, copper-64 SARTATE among them, found that peptide, chelator and metal each shape the binding, and identified a distinct interaction pattern for each compound.
Side Effects & Contraindications
Reported Side Effects
From the two human studies.
Contraindications & Cautions
No approved label exists, so there are no official contraindications. Points from the studies:
Legal Status
SARTATE is investigational in every jurisdiction checked.
Frequently Asked Questions
?What is SARTATE?
The somatostatin analogue octreotate attached to MeCOSar, a cage-shaped chelator that holds copper tightly, so it can carry copper-64 for PET or copper-67 for therapy.
?Why use copper?
Copper-64 and copper-67 are the same element, so a scan with one predicts how the other will behave. Copper-64's longer half-life also allows imaging up to 24 hours after injection.
?Has it been given to people?
Yes: copper-64 SARTATE PET to 10 people with neuroendocrine tumours, and copper-64 imaging plus four cycles of copper-67 therapy to 3 people with meningioma.
?Is SARTATE approved?
No. It is investigational; the approved copper-64 somatostatin tracer is copper Cu 64 dotatate.
References
- [other] PubChem CID 137347535 (synonyms SarTATE, ucasareotide dasaroxetan): formula C69H103N17O14S2, molecular weight 1458.8. Read October 28, 2026. https://pubchem.ncbi.nlm.nih.gov/compound/137347535
- [clinical-trial] Hicks RJ, et al. "(64)Cu-SARTATE PET Imaging of Patients with Neuroendocrine Tumors Demonstrates High Tumor Uptake and Retention, Potentially Allowing Prospective Dosimetry for Peptide Receptor Radionuclide Therapy." J Nucl Med, 2019;60(6):777-785. PMID: 30442752.
- [clinical-trial] Bailey DL, et al. "(64)Cu Treatment Planning and (67)Cu Therapy with Radiolabeled [(64)Cu/(67)Cu]MeCOSar-Octreotate in Subjects with Unresectable Multifocal Meningioma: Initial Results for Human Imaging, Safety, Biodistribution, and Radiation Dosimetry." J Nucl Med, 2023;64(5):704-710. PMID: 36460344.
- [pubmed] Paterson BM, et al. "PET imaging of tumours with a 64Cu labeled macrobicyclic cage amine ligand tethered to Tyr3-octreotate." Dalton Trans, 2014;43(3):1386-96. PMID: 24202174.
- [pubmed] Cullinane C, et al. "Peptide Receptor Radionuclide Therapy with (67)Cu-CuSarTATE Is Highly Efficacious Against a Somatostatin-Positive Neuroendocrine Tumor Model." J Nucl Med, 2020;61(12):1800-1805. PMID: 32414949.
- [pubmed] Dearling JLJ, et al. "Detection and therapy of neuroblastoma minimal residual disease using [(64/67)Cu]Cu-SARTATE in a preclinical model of hepatic metastases." EJNMMI Res, 2021;11(1):20. PMID: 33630166.
- [pubmed] Laffon E, et al. "An abbreviated therapy-dosimetric equation for the companion diagnostic/therapeutic [(64/67)Cu]Cu-SARTATE." EJNMMI Res, 2021;11(1):75. PMID: 34417898.
- [pubmed] Gervasoni S, et al. "Interaction of Radiopharmaceuticals with Somatostatin Receptor 2 Revealed by Molecular Dynamics Simulations." J Chem Inf Model, 2023;63(15):4924-4933. PMID: 37466559.
- [registry] ClinicalTrials.gov API v2, read October 28, 2026: NCT04438304 (phase 2, diagnostic imaging, completed); NCT03936426 (phase 1/2, copper-67 SARTATE in meningioma, completed); NCT04023331 (phase 1/2, paediatric, terminated).
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. Formula and weight are PubChem's. 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. Consult a licensed healthcare provider before making health decisions.